DNA/RNA合成

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S1166	Cisplatin	<1 mg/mL	60 mg/mL	'<1 mg/mL
S1149	Gemcitabine HCl	19 mg/mL	<1 mg/mL	<1 mg/mL
S1135	Pemetrexed	94 mg/mL	<1 mg/mL	<1 mg/mL
S1215	Carboplatin	14 mg/mL	<1 mg/mL	<1 mg/mL
S3360	Bis(2-ethylhexyl) phthalate			' mg/mL
S3356	Phosphonoacetic acid	28 mg/mL	28 mg/mL	'''28 mg/mL
S3009	Menthone			' mg/mL
S9718	TK216	<1 mg/mL	75 mg/mL	50 mg/mL
S9649	Acelarin (NUC-1031)	<1 mg/mL	100 mg/mL	'20 mg/mL
S8977	BCH001	<1 mg/mL	84 mg/mL	5 mg/mL
S8850	JH-RE-06	<1 mg/mL	12 mg/mL	<1 mg/mL
S7418	Cycloheximide	15 mg/mL	56 mg/mL	''56 mg/mL
S6848	3'-Fluoro-3'-deoxythymidine (Alovudine)	20 mg/mL	49 mg/mL	'40 mg/mL
S0816	Brr2 Inhibitor C9	<1 mg/mL	89 mg/mL	''2 mg/mL
S0780	Oncrasin-1			' mg/mL
S0469	ML216	˂1 mg/mL	38 mg/mL	˂1 mg/mL
S0280	Madrasin	<1 mg/mL	1 mg/mL	3 mg/mL
S0102	L 189	˂1 mg/mL	49 mg/mL	˂1 mg/mL
S0063	RG3039	<1 mg/mL	3 mg/mL	'''<1 mg/mL
S0054	D-I03	<1 mg/mL	86 mg/mL	10 mg/mL
S2600	Fexinidazole	<1 mg/mL	56 mg/mL	<1 mg/mL
S8932	Remdesivir (GS-5734)	<1 mg/mL	100 mg/mL	'''16 mg/mL
S1491	Fludarabine	<1 mg/mL	57 mg/mL	<1 mg/mL
S1224	Oxaliplatin	3 mg/mL	-1 mg/mL	0.01 mg/mL
S2684	CX-5461	<1 mg/mL	0.02 mg/mL	<1 mg/mL
S1209	Fluorouracil (5-Fluorouracil, 5-FU)	<1 mg/mL	26 mg/mL	<1 mg/mL
S1156	Capecitabine	6 mg/mL	72 mg/mL	72 mg/mL
S1229	Fludarabine Phosphate	2 mg/mL	73 mg/mL	<1 mg/mL
S1117	Triciribine	<1 mg/mL	64 mg/mL	<1 mg/mL
S1516	Cidofovir	12 mg/mL	2 mg/mL	<1 mg/mL
S1648	Cytarabine	48 mg/mL	1 mg/mL	<1 mg/mL
S1714	Gemcitabine	52 mg/mL	52 mg/mL	<1 mg/mL
S1213	Nelarabine	3 mg/mL	60 mg/mL	<1 mg/mL
S1373	Daptomycin	100 mg/mL	100 mg/mL	<1 mg/mL
S3035	Daunorubicin HCl	100 mg/mL	100 mg/mL	<1 mg/mL
S1199	Cladribine	<1 mg/mL	57 mg/mL	<1 mg/mL
S1192	Raltitrexed	<1 mg/mL	91 mg/mL	<1 mg/mL
S1218	Clofarabine	<1 mg/mL	60 mg/mL	<1 mg/mL
S1302	Ifosfamide	52 mg/mL	52 mg/mL	52 mg/mL
S2678	NSC 207895	<1 mg/mL	0.4 mg/mL	<1 mg/mL
S1221	Dacarbazine	2 mg/mL	12 mg/mL	1 mg/mL
S1896	Hydroxyurea	15 mg/mL	15 mg/mL	<1 mg/mL
S1807	Aciclovir	<1 mg/mL	45 mg/mL	<1 mg/mL
S1299	Floxuridine	49 mg/mL	49 mg/mL	10 mg/mL
S1305	Mercaptopurine (6-MP)	<1 mg/mL	30 mg/mL	<1 mg/mL
S1384	Mizoribine	51 mg/mL	1 mg/mL	<1 mg/mL
S1949	Menadione	<1 mg/mL	34 mg/mL	34 mg/mL
S2239	Tubacin	<1 mg/mL	100 mg/mL	<1 mg/mL
S1289	Carmofur	<1 mg/mL	52 mg/mL	10 mg/mL
S4227	Fidaxomicin	<1 mg/mL	100 mg/mL	<1 mg/mL
S1907	Metronidazole	<1 mg/mL	34 mg/mL	<1 mg/mL
S1760	Rifapentine	<1 mg/mL	100 mg/mL	17 mg/mL
S1778	Trifluridine	59 mg/mL	59 mg/mL	'59 mg/mL
S1790	Rifaximin	<1 mg/mL	47 mg/mL	3 mg/mL
S1995	Procarbazine HCl	52 mg/mL	<1 mg/mL	52 mg/mL
S1784	Vidarabine	3 mg/mL	53 mg/mL	<1 mg/mL
S1764	Rifampin	<1 mg/mL	100 mg/mL	<1 mg/mL
S3001	Clevudine	52 mg/mL	52 mg/mL	4 mg/mL
S1300	Tegafur (FT-207)	8 mg/mL	40 mg/mL	7 mg/mL
S1826	Nedaplatin	18 mg/mL	<1 mg/mL	<1 mg/mL
S7470	Triapine	<1 mg/mL	20 mg/mL	<1 mg/mL
S7757	6-Thio-dG	<1 mg/mL	56 mg/mL	<1 mg/mL
S4297	Mupirocin	46 mg/mL	100 mg/mL	100 mg/mL
S8376	Rbin-1	<1 mg/mL	23 mg/mL	'1 mg/mL
S9521	Pentostatin	54 mg/mL	54 mg/mL	<1 mg/mL
S5552	Amenamevir			' mg/mL
S8095	Tubercidin	<1 mg/mL	53 mg/mL	<1 mg/mL
S4035	Vitamin D2	<1 mg/mL	20 mg/mL	80 mg/mL
S7975	Favipiravir (T-705)	5 mg/mL	31 mg/mL	22 mg/mL
S8328	CeMMEC1 HCl	<1 mg/mL	23 mg/mL	1 mg/mL
S5484	Rimantadine Hydrochloride	-1 mg/mL	43 mg/mL	-1 mg/mL
S4504	6-Mercaptopurine (6-MP) Monohydrate	<1 mg/mL	34 mg/mL	'<1 mg/mL
S7742	SCR7	<1 mg/mL	66 mg/mL	3 mg/mL
S4737	Psoralen	<1 mg/mL	37 mg/mL	'<1 mg/mL
S8146	Mitomycin C	<1 mg/mL	66 mg/mL	<1 mg/mL
S1973	Cyclocytidine HCl	44 mg/mL	10 mg/mL	<1 mg/mL
S3641	Osalmid	<1 mg/mL	45 mg/mL	45 mg/mL
S7449	CRT0044876	<1 mg/mL	41 mg/mL	1 mg/mL
S7445	E3330	<1 mg/mL	75 mg/mL	75 mg/mL
S5293	Nimustine Hydrochloride	-1 mg/mL	61 mg/mL	-1 mg/mL
S5297	Vidarabine monohydrate	-1 mg/mL	57 mg/mL	''-1 mg/mL
S2794	Sofosbuvir (GS-7977)	11 mg/mL	100 mg/mL	100 mg/mL
S8434	B02	<1 mg/mL	67 mg/mL	20 mg/mL
S8539	TAS-102	15 mg/mL	100 mg/mL	100 mg/mL
S7637	DTP3	100 mg/mL	100 mg/mL	100 mg/mL
S8144	Halofuginone	<1 mg/mL	20 mg/mL	<1 mg/mL
S7679	YK-4-279	<1 mg/mL	73 mg/mL	51 mg/mL
S4236	Proflavine Hemisulfate	22 mg/mL	<1 mg/mL	<1 mg/mL
S7718	BMH-21	<1 mg/mL	5 mg/mL	2 mg/mL
S4239	Bergapten	<1 mg/mL	5 mg/mL	<1 mg/mL
S4782	5-methoxyflavone	-1 mg/mL	50 mg/mL	-1 mg/mL
S4537	Oxolinic acid	<1 mg/mL	0.5 mg/mL	''<1 mg/mL
S7546	Pritelivir (BAY 57-1293)	<1 mg/mL	80 mg/mL	'<1 mg/mL
S8329	CeMMEC13	<1 mg/mL	67 mg/mL	6 mg/mL
S5582	Cytarabine hydrochloride	-1 mg/mL	55 mg/mL	-1 mg/mL
S7419	Blasticidin S HCl	91 mg/mL	<1 mg/mL	<1 mg/mL
S4288	Chloroambucil	<1 mg/mL	60 mg/mL	'60 mg/mL
S8246	RK-33	<1 mg/mL	85 mg/mL	<1 mg/mL
S3168	cis-Resveratrol	<1 mg/mL	46 mg/mL	'''46 mg/mL
S6893	PIN1 inhibitor API-1	<1 mg/mL	73 mg/mL	2 mg/mL
S2427	Triglycidyl Isocyanurate (Teroxirone)	<1 mg/mL	59 mg/mL	'<1 mg/mL
S8326	Saccharin 1-methylimidazole (SMI)	53 mg/mL	53 mg/mL	53 mg/mL
S1334	Flupirtine maleate	<1 mg/mL	84 mg/mL	2 mg/mL
S1214	Bleomycin Sulfate	100 mg/mL	100 mg/mL	'''<1 mg/mL
S6854	Triazavirin	20 mg/mL	57 mg/mL	<1 mg/mL
S1237	Temozolomide	<1 mg/mL	38 mg/mL	<1 mg/mL
S1212	Bendamustine HCl	2 mg/mL	78 mg/mL	17 mg/mL
S1840	Lomustine	<1 mg/mL	46 mg/mL	<1 mg/mL
S7918	Bromodeoxyuridine (BrdU)	<1 mg/mL	61 mg/mL	2 mg/mL
S4888	Guanine	<1 mg/mL	0.1 mg/mL	<1 mg/mL
S5505	2’-deoxyuridine	-1 mg/mL	45 mg/mL	-1 mg/mL
S6359	Purine	-1 mg/mL	24 mg/mL	-1 mg/mL
S4194	Azaguanine-8	<1 mg/mL	6 mg/mL	<1 mg/mL
S4803	Thymidine	-1 mg/mL	48 mg/mL	-1 mg/mL
S1981	Adenine	<1 mg/mL	<1 mg/mL	'<1 mg/mL
S1983	Adenine HCl	4 mg/mL	8 mg/mL	<1 mg/mL
S1982	Adenine sulfate	2 mg/mL	<1 mg/mL	<1 mg/mL
S6077	Cytidine 5′-triphosphate (disodium salt)	-1 mg/mL	18 mg/mL	-1 mg/mL
S5374	5'-Cytidylic acid	64 mg/mL	<1 mg/mL	-1 mg/mL
S5384	UTP Trisodium Salt	100 mg/mL	<1 mg/mL	-1 mg/mL
S3190	N6-methyladenosine (m6A)	14 mg/mL	47 mg/mL	2 mg/mL
S2029	Uridine	49 mg/mL	49 mg/mL	<1 mg/mL
S9382	Thymine	-1 mg/mL	25 mg/mL	-1 mg/mL

DNA/RNA Synthesis製品

All (126) DNA/RNA Synthesis阻害剤(100) DNA/RNA Synthesis活性剤(4) DNA/RNA Synthesis拮抗剤(1) DNA/RNA Synthesisモジュレータ(1)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1166	Cisplatin Cisplatin (cisplatinum, cis-diamminedichloroplatinum II, CDDP) is an inorganic platinum complex, which is able to inhibit DNA synthesis by conforming DNA adducts in tumor cells. Cisplatin activates ferroptosis and induces autophagy. Solutions are best fresh-prepared.	Theranostics, 2021, 11(6):2860-2875 Mol Cancer, 2021, 20(1):17 Acta Pharmacol Sin, 2021, 10.1038/s41401-020-00577-1	Cell viabilities with increasing concentrations of cisplatin (CP) and doxorubicin (DOXO) under normoxic and hypoxic condition for 48 hours were determined by MTT assay. IC50 values are presented as the means ?SDs (n=4) and * denotes p<0.05.
S1149	Gemcitabine HCl Gemcitabine HCl (LY188011) is a DNA synthesis inhibitor with IC50 of 50 nM, 40 nM, 18 nM and 12 nM in PANC1, MIAPaCa2, BxPC3 and Capan2 cells, respectively.	Oncogene, 2021, 10.1038/s41388-020-01634-z Cell Death Dis, 2021, 12(1):72 Invest New Drugs, 2021, 10.1007/s10637-020-01003-3	RNA incorporating drugs induce SG assembly. HeLa cells were treated with the RNA incorporating agents 5-azacytidine (50 uM) and 6-thioguanine (10 uM), or the DNA incorporating agents trifluorothymidine (10 uM) and gemcitabine (100 nM) for 72 h. Subsequently, the cellular localization of the SG marker protein TIAR (green) and the P-body marker protein DCP1 (red) was analyzed. Nuclei were stained with Hoechst. Scale bars represent 20 um.
S1135	Pemetrexed Pemetrexed (LY-231514) is a novel antifolate and antimetabolite for TS, DHFR and GARFT with K_i of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.	Nat Commun, 2020, 14;11(1):1825 J Hematol Oncol, 2020, 1;13(1):40 Cell Death Dis, 2020, 11(11):945	Role of PARP and BER in the synergy between PTX and GMX in A549 cells. Cells were pretreated ±1 umol/L olaparib (2 hours) then sequentially ±150 nmol/L PTX (24 hours), then ± GMX 12 nmol/L (48 hours). PAR modification of proteins and γ-H2AX levels were measured in extracts treated as in A by Western blotting.
S1215	Carboplatin Carboplatin (JM-8, CBDCA, NSC 241240) is a DNA synthesis inhibitor by binding to DNA and interfering with the cell's repair mechanism in A2780, SKOV-3, IGROV-1, and HX62 cells. Solutions are best fresh-prepared.	Eur J Pharmacol, 2021, 895:173887 Nat Commun, 2020, 24;11(1):1975 Nat Commun, 2020, 22;11(1):2573	Detection of apoptotic responses was found to increase in epimorphin-treated A1847 with increasing concentrations of carboplatin compared to those of the untreated controls. Data were normalized to the controls and are represented as means ± S.D. [*p<0.05 compared with control]. Images of apoptotic cells were captured at 10X magnification, with at least 3 images per well, using an upright phase-contrast microscope (T3.15A; Fisher Scientific).
S3360^新	Bis(2-ethylhexyl) phthalate Bis(2-ethylhexyl) phthalate (Dioctyl phthalate, DOP, Diplast O, ESBO-D 82, Ergoplast FDO, Ergoplast FDO-S, Etalon) induces DNA strand breaks and gene expression alterations in larval zebrafish Danio rerio.
S3356^新	Phosphonoacetic acid Phosphonoacetic acid (PAA) is an active endogenous metabolite that possesses a restricted potential to block DNA biosynthesis. Phosphonoacetic acid exhibits anti-viral activities.
S3009^新	Menthone Menthone is one of the main volatile components of the essential oil of peppermint (Mentha piperita L.). Menthone is used as antioxidant agent and has a good compensatory effect with significant reduction in DNA damages in sperm cells.
S9718^新	TK216 TK216 is a potent inhibitor targeting E26 transformation specific (ETS) factors via blocking the protein-protein interaction with RNA helicases. TK216 exhibits antilymphoma activity.
S9649^新	Acelarin (NUC-1031) Acelarin (NUC-1031, Fosgemcitabine palabenamide, CPF-31, MTL-007, GTPL7389), a prodrug based on an aryloxy phosphoramidate derivative of gemcitabine, is a DNA synthesis inhibitor with EC50 of 0.2 nM.
S8977^新	BCH001 BCH001 is a specific PAPD5 inhibitor that restores telomerase activity and telomere length in dyskeratosis congenita (DC) patient induced pluripotent stem cells. PAPD5 is a noncanonical poly(A) polymerase with an unusual RNA-binding motif.
S8850^新	JH-RE-06 JH-RE-06 is a potent REV1-REV7 interface inhibitor with an IC50 of 0.78 μM and Kd value of 0.42 μM, disrupting REV1-POL ζ-mediated mutagenic translesion synthesis (TLS).
S7418^新	Cycloheximide Cycloheximide (Actidione, Naramycin A, CHX), an antifungal antibiotic, is an eukaryote protein synthesis inhibitor with IC50 of 532.5 nM and 2880 nM for protein synthesis and RNA synthesis in vivo, respectively. Cycloheximide suppresses ferroptosis and inhibits autophagy.	Theranostics, 2021, 11(2):700-714 Theranostics, 2021, 11(6):2655-2669 ACS Nano, 2020, 10.1021/acsnano.0c08947
S6848^新	3'-Fluoro-3'-deoxythymidine (Alovudine) 3'-Fluoro-3'-deoxythymidine (Alovudine, CL 184824, FddThd, FLT, MIV-310) is a potent inhibitor of polymerase γ and reverse transcriptase that can be used in the treatment of HIV infection. 3'-Fluoro-3'-deoxythymidine (Alovudine) is also a marker of DNA synthesis that can be used as an early response biomarker in the chemotherapy of pancreatic cancer.
S0816^新	Brr2 Inhibitor C9 Brr2 inhibitor C9 (Brr2 Inhibitor 9) is an allosteric inhibitor of the spliceosomal RNA helicase Brr2. Brr2 is implicated in autosomal-dominant retinitis pigmentosa a group of progressive retinal degenerative disorders.
S0780^新	Oncrasin-1 Oncrasin-1 (Onc-1) is a potent RNA polymerase II inhibitor with antitumor activity that kills various human lung cancer cells with K-Ras mutations. Oncrasin-1 drives abnormal aggregation of protein kinase C iota (PKCι) in nucleus of sensitive cells but not in resistant cells.
S0469^新	ML216 ML216 (CID-49852229) is a potent and selective inhibitor of the DNA unwinding activity of BLM(Bloom’s syndrome protein) with antitumor activity. ML216 inhibits helicases with IC50 of 0.97 μM and 2.98 μM for BLM^636-1298 and BLM^full-length, respectively.
S0280^新	Madrasin Madrasin (DDD00107587) is a potent and cell-penetrant pre-mRNA splicing inhibitor. Madrasin interferes with the early stages of spliceosome assembly and stalls spliceosome assembly at the A complex.
S0102^新	L 189 L 189 is a novel human DNA ligase inhibitor with IC50 of 5 μM, 9 μM and 5 μM for hLigI, hLigIII and hLigIV, respectively. L 189 inhibits base excision repair (BER) and non-homologous end joining (NHEJ). L 189 specifically sensitizes cancer cells to DNA damage.
S0063^新	RG3039 RG3039 (PF-06687859, PF 6687859, Quinazoline 495) is an orally bioavailable and brain-penetrant inhibitor of the mRNA decapping enzyme DcpS with IC50 of 4.2 nM and IC90 of 40 nM, respectively.
S0054^新	D-I03 D-I03 is a selective inhibitor of RAD52 with Kd of 25.8 µM. D-I03 inhibits ssDNA annealing by RAD52 and D-loop formation with IC50 of 5 µM and 8 µM, respectively.
S2600^新	Fexinidazole Fexinidazole (HOE-239, Fexinidazole Winthrop) is a 5-nitroimidazole derivative. Fexinidazole is a DNA synthesis inhibitor and the only, all-oral agent for Human African Trypanosomiasis(HAT or sleeping sickness).
S8932^新	Remdesivir (GS-5734) Remdesivir (GS-5734), a monophosphoramidate prodrug of an adenosine analog, is an investigational broad-spectrum antiviral agent with in vitro activity against multiple RNA viruses, including Ebola and CoV.	Nat Commun, 2021, 12(1):668 mBio, 2021, 12(1)e02754-20 Antiviral Res, 2021, 187:105015
S1491	Fludarabine Fludarabine (FaraA, Fludarabinum) is a STAT1 activation inhibitor which causes a specific depletion of STAT1 protein (and mRNA) but not of other STATs. Also a DNA synthesis inhibitor in vascular smooth muscle cells. Fludarabine induces apoptosis.	Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19 Cell Metab, 2020, 31(3):564-579	Normal human KC pretreated with STAT1 inhibitor (fludarabine [10 uM]) or STAT3 inhibitor (STA-21 [2 uM]) for 24 h. The mRNA levels of hBD2 and hBD3 were assessed by qRT-PCR.
S1224	Oxaliplatin Oxaliplatin (L-OHP) is a DNA alkylating agent that activates autophagy. Oxaliplatin inhibits DNA synthesis by conforming DNA adducts in RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2, and HT-144 cells. DMF is recommended for dissolution. Solutions are best fresh-prepared.	Nat Microbiol, 2021, 10.1038/s41564-020-00831-6 Mol Cancer, 2021, 20(1):10 Adv Biol Regul, 2021, S2212-4926(20)30091-9	Immunocytochemical staining of SW620 (metastatic) cells after treatment with 10 uM oxaliplatin (F) or 10 uM ginsenosides 20(S)-Rg 3 (G) and negative staining (H). Cells demonstrated differential expression of histone H4.
S2684	CX-5461 CX-5461 is an inhibitor of rRNA synthesis, selectively inhibits Pol I-driven transcription of rRNA with IC50 of 142 nM in HCT-116, A375, and MIA PaCa-2 cells, has no effect on Pol II, and possesses 250- to 300-fold selectivity for inhibition of rRNA transcription versus DNA replication and protein translation.	Sci Rep, 2021, 11(1):360 Nat Commun, 2020, 11(1):4287 Nucleic Acids Res, 2020, 18;gkaa344	The specific Pol I inhibitor CX-5461 causes nucleolar disruption, blocks LTP maintenance and Fsk-induced synthesis of new rRNA. DAPI staining (blue; A, B,C) shows the area of the nucleus. Nomarski images (grey; G, H,I) show the area of the nuclei and nucleoli (arrowheads). Application of Pol I specific inhibitor CX-5461 (200 nM) causes nucleolar disruption as indicated by the distribution of fibrillarin (green); compare A, D to B, E and C, F.
S1209	Fluorouracil (5-Fluorouracil, 5-FU) Fluorouracil (5-Fluorouracil, 5-FU, NSC 19893) is a DNA/RNA synthesis inhibitor, which interrupts nucleotide synthetic by inhibiting thymidylate synthase (TS) in tumor cells. Fluorouracil induces apoptosis and can be used in the treatment of HIV.	Molecules, 2021, 26(2)E334 Biosci Rep, 2021, BSR20200842 Int J Radiat Biol, 2021, 1-16	DNA-PKcs suppression mediated ROS production and GSH content in HepG2 cells exposed to CDDP and 5-Fu. a DNA-PKcs inhibition promoted ROS production in HepG2 cells treated with indicated concentrations of CDDP and 5-Fu. DCFH-DA fluorescent analysis was performed to assess the ROS level. Data presented were mean ?SD of three independent experiments.
S1156	Capecitabine Capecitabine (RO 09-1978) is a tumor-selective fluoropyrimidine carbamate, which achieves higher intratumoral 5-FU level with lower toxicity than 5-FU. Capecitabine treatment of HCT-15 cells causes condensation of DNA and induces apoptosis.	Cancer Lett, 2020, 28;476:67-74 Acta Biomater, 2020, S1742-7061(20)30751-0 Cancer Cell Int, 2020, 19;20:58	Growth curve of human colon cancer xenografts in nude mice treated with orally administered vehicle or capecitabine at 360 mg/kg (n = 10–12 per cell line).
S1229	Fludarabine Phosphate Fludarabine Phosphate (F-ara-A, NSC 312887) is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.	Exp Neurol, 2020, S0014-4886(20)30337-X Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8	Imatinib mesylate (IM) in combination of F-AMP significantly inhibits Ki67 and c-KIT expression in GIST-T1 tumor xenografts. Tumors were collected on the day after the last treatment and were then subjected to H&E staining and immunohistochemical detection of Ki67, c-KIT, and cleaved caspase-3 expression. Representative images of H&E staining and immunohistochemical staining of Ki67, c-KIT, and cleaved caspase-3 in mice tumors. Arrows indicate the decrease in cellularity and the increase in stromal fibrosis. Magnification, x 400.
S1117	Triciribine Triciribine (NSC 154020, VD-0002, vqd-002, API-2) is a DNA synthesis inhibitor, also inhibits Akt in PC3 cell line and HIV-1 in CEM-SS, H9, H9IIIB, U1 cells with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. Phase 1/2.	Mol Cancer Ther, 2020, molcanther.0369.2020 Cell Oncol (Dordr), 2020, 8 Molecules, 2020, 25(19)E4505	Effect of triciribine on the migration of (A) FaDu and (B) Hep2 cells. The cells were treated with 5 µM triciribine for different periods of time. *P<0.05 vs. control. Hpf, high-power field.
S1516	Cidofovir Cidofovir (HPMPC) suppresses virus replication by selective inhibition of viral DNA synthesis.	Nat Biotechnol, 2019, 37(3):303-313 J Virol, 2019, 93(4) Antiviral Res, 2019, 162:178-185	The copy numbers of the intracellular viral DNA were directly extracted from cells and were quantified by qPCR using primers specific for the KSHV ORF73 gene. Then each sample was normalized to the amount of the GAPDH gene (C), CDV (20 µM) was used as a positive control. CDV:Cidofovir.
S1648	Cytarabine Cytarabine (Cytarabin, Ara-C, Arabinofuranosyl Cytidine) is an antimetabolic agent and DNA synthesis inhibitor with IC50 of 16 nM in wild-type CCRF-CEM cells. Cytarabine induces autophagy and apoptosis.	Cell Death Dis, 2021, 12(1):9 Cytometry A, 2021, 10.1002/cyto.a.24308 Haematologica, 2020, haematol.2020.246843	Viability and CI vs Fa after 24-h exposure to cytarabine alone or in combination with ABT-199 in Riva, U2932 and VavP-Bcl2/c-MYC murine tumor cells. Viability shown at 500 nM (500 ng/ml for cytarabine; quadruplicates±s.e.m.).
S1714	Gemcitabine Gemcitabine (LY-188011, NSC 613327), a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy. Gemcitabine induces a potent p53-dependent apoptosis.	Cell Death Dis, 2021, 12(1):72 Invest New Drugs, 2021, 10.1007/s10637-020-01003-3 Int J Radiat Biol, 2021, 1-16	RNA incorporating drugs induce SG assembly. HeLa cells were treated with the RNA incorporating agents 5-azacytidine (50 uM) and 6-thioguanine (10 uM), or the DNA incorporating agents trifluorothymidine (10 uM) and gemcitabine (100 nM) for 72 h. Subsequently, the cellular localization of the SG marker protein TIAR (green) and the P-body marker protein DCP1 (red) was analyzed. Nuclei were stained with Hoechst. Scale bars represent 20 um.
S1213	Nelarabine Nelarabine (506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.	Nat Cell Biol, 2020, 20 Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8	b) Western blot analysis documenting cleavage of caspase-8, caspase-9, caspase-3, and PARP by nelarabine. Cells were treated with nelarabine (5 μM for JURKAT, P12-ICHIKAWA, and DND-41 cells, 2 μM MOLT-4 cells) for the indicated times, collected, and then lysed. Fifty micrograms of each lysate were electrophoresed on SDS-PAGE gels followed by transfer onto a nitrocellulose membrane. c) Nelarabine induces a decrease in the phosphorylation status of critical components of the PI3K/AKT/mTOR signaling pathway, as well as p-ERK (Thr202) levels in T-ALL sensitive cell lines. Western blot analysis documenting the reduction of p-AKT (Ser473), p-S6RP, p-GSK3β (Ser9), and p-ERK (Thr202). Antibody to β-actin served as a loading control. Molecular weights are indicated on the right
S1373	Daptomycin Daptomycin (LY146032) is a novel antibiotic with rapid in vitro bactericidal activity against gram-positive organisms.	Sci Adv, 2020, 6(34):eaba8968 Front Microbiol, 2020, 21;11:646 PLoS One, 2020, 15(2):e0228509	Same experiment as in Figure 2 with fluorescent daptomycin shown as confocal images. A 7/3 DOPC/DOPG GUV (including 1% Rh-PE) was introduced at time zero into a solution containing 1 uM daptomycin with 0.5 uM BODIPY-daptomycin and 1 mM Ca2+. To show colocalization of lipid and peptide in aggregates, confocal images were taken: red for RH-PE and green for BODIPY-daptomycin. As the protrusion length decreased, aggregates appeared on the GUV surface containing both lipid and peptide. The scale bar is 10 um.
S3035	Daunorubicin HCl Daunorubicin HCl (Daunomycin) inhibits both DNA and RNA synthesis and inhibits DNA synthesis with K_i of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis.	Int J Radiat Oncol Biol Phys, 2021, 109(1):60-72 Haematologica, 2020, 12;haematol.2019.233445 Cancer Cell Int, 2020, 19;20:58	A) MV411 or B) Kasumi 1 cells were incubated with YM155 (0.25 x IC50) in the presence or absence of i) 0.5 x IC50 or ii) 1 x IC50 of Daunorubicin or iii) 0.5 x IC50 or iv) 1 x IC50 of Cytarabine for 72h. Following 72h treatment, cells were subject to a resazurin reduction assay. Percentages were normalised to DMSO controls. Column, mean of 3 independent experiments; Bars, SEM. p<0.05, p<0.01, **p<0.005. Students t-test. Similar trends were observed with 0.5 x and 1 x IC50 of YM155 in combination with Daunorubicin or Cytarabine (data not shown).
S1199	Cladribine Cladribine (2-CdA, 2-chlorodeoxyadenosine) is an adenosine deaminase inhibitor for U266, RPMI8226, and MM1.S cells with IC50 of approximately 2.43 μM, 0.75 μM, and 0.18 μM, respectively.	Nat Commun, 2020, 29;11(1):2086 PLoS Pathog, 2020, 16;16(3):e1008341 Front Immunol, 2020, 11:616570
S1192	Raltitrexed Raltitrexed (ZD-1694) is a thymidylate synthase inhibitor with an IC50 of 9 nM for the inhibition of L1210 cell growth.	Anal Chem, 2020, 10.1021/acs.analchem.0c02756 Int J Mol Sci, 2020, 21(12):E4452 EBioMedicine, 2019, 48:289-300	Fig. 1. Raltitrexed dose-response curve. HEK293 parental and MRP5 transfected cells were plated in a 96-well plate at a density of 4000 cells/well in complete DMEM (10% FBS, 1% Pencillin/streptomycin) and allowed to incubate for 24h at 37°C, 5% CO2. Raltirexed was added and the cells allowed to incubate for 72h. Total DNA present in each well was then quantified using Cyquant® cell proliferation assay. Results show Total DNA as % of the DMSO-only control wells. Experiment was done in triplicate.
S1218	Clofarabine Clofarabine inhibits the enzymatic activities of ribonucleotide reductase (RNR) (IC50 = 65 nM) and DNA polymerase. Clofarabine induces autophagy and apoptosis.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8 Hum Cell, 2020, 10.1007/s13577-020-00420-z	Immunoblot analysis of cell lysates of NCI-H929 cells treated with CLO (5 μM, 3-48 h) GAPDH served as the loading control for each membrane, and data are representative of at least two independent experiments
S1302	Ifosfamide Ifosfamide (NSC109724, Isophosphamide) is a nitrogen mustard alkylating agent used in the treatment of cancer.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8 Hum Cell, 2020, 10.1007/s13577-020-00420-z	Chemotherapeutic response. Ifosfamide was applied at different concentrations on Lipo-DUE1, Lipo246, and PLS-1 for 72 h. Subsequently, cell viability was determined by MTS assay at a wavelength of 490 nm. Values represent the mean±S.D. of triplicates
S2678	NSC 207895 NSC 207895 (XI-006) suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase.	Genes Dev, 2020, 34(7-8):526-543 Oncotarget, 2020, 11(46):4224-4242 Sci Rep, 2019, 9(1):1897	Median overall survival of mice (n = 5 mice in vehicle and PYR-41; n = 4 mice in NSC group) inoculated with IOWA-1T xenografts were increased to 43 ± 0.5 and 39 ± 2 days with PYR-41 (PYR) and NSC-207895 (NSC), respectively, compared with a vehicle-treated control group 33 ± 1 days (*p < 0.05).
S1221	Dacarbazine Dacarbazine (DTIC-Dome) is a triazene derivative with antineoplastic activity. Dacarbazine alkylates and cross-links DNA during all phases of the cell cycle, resulting in disruption of DNA function, cell cycle arrest, and apoptosis; used in the treatment of various cancers.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S1896	Hydroxyurea Hydroxyurea (nci-c04831, nsc32065) is an antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase. Hydroxyurea activates apoptosis and autophagy. Hydroxyurea is used to treat HIV infection.	Carcinogenesis, 2021, bgab002 Haematologica, 2020, 12;haematol.2019.233445 Cancer Cell Int, 2020, 19;20:58	Lethally irradiated C57BL/6 recipient mice were injected with a 1:1 mixture of GFP+JAK2(V671F) and wild-type bone marrow cells. Five weeks later, mice were treated with vehicle (C), hydroxyurea (H; 30 mg/kg twice daily IP), ruxolitinib (R; 30 mg/kg twice daily oral gavage), BMN673 (B; 0.33 mg/kg IV), H+R, H+B, R+B, and H+R+B for 3 weeks. Percentage of GFP+JAK2(V617F) was measured in (panel B) bone marrow cells, (panel C) splenocytes, and (panel D) peripheral blood leukocytes; (panel E) number of GFP+JAK2(V617F) Lin−Sca1+c-Kit+ (LSK) cells per 106 bone marrow cells was calculated, too. P < .05, P < .05, and **P < .05 when compared with control, single treatment, and double treatment, respectively, from 6 to 7 mice using the Student t test.
S1807	Aciclovir Acyclovir (Acyclovir, Acycloguanosine, Zovirax) is a synthetic nucleoside analogue active against herpesviruses. Acyclovir induces cell cycle perturbation and apoptosis in Jurkat leukemia cells.	Sci Adv, 2020, 6(49)eabd9443 ACS Infect Dis, 2020, 6(11):2926-2937 Antimicrob Agents Chemother, 2020, AAC.00245-20	(A) HONE1 and (B) HK1-EBV cells were treated with TPA (40 ng/ml) and SB (3 mM) for EBV induction. After 3 h, uninduced and induced HONE1 and HK1-EBV cells were treated with the vehicle control (0.006% DMSO) or indicated concentrations of berberine for 48 h. Subsequently, the culture medium was harvested for quantitative-PCR analysis with EBNA1 primers. Each sample was normalized to the amount of the GAPDH gene; *p<0.05, compared with the control group.
S1299	Floxuridine Floxuridine (Deoxyfluorouridine, FUDR, NSC 27640) is an antineoplastic antimetabolite, used in the treatment of colon carcinoma and colorectal cancer that has metastasized to the liver.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S1305	Mercaptopurine (6-MP) Mercaptopurine is a widely used antileukemic agent and immunosuppressive drug that inhibits de novo purine synthesis through incorporation of thiopurine methyltransferase metabolites into DNA and RNA.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S1384	Mizoribine Mizoribine (Bredinin, NSC 289637) is an imidazole nucleoside and an immunosuppressant that inhibits HCV RNA replication with IC50 of ~ 100 μM for anti-HCV activity. Mizoribine is a selective inhibitor of inosine-5'-monophosphate dehydrogenase (IMPDH) and guanosine monophosphate synthetase. Mizoribine also inhibits SARS-CoV.	JCI Insight, 2020, 9;5(7):e135071 Cancer Cell, 2017, 32(5):624-638
S1949	Menadione Menadione(Vitamin K3), a fat-soluble compound, is an inhibitor of Cdc25 phosphatase and mitochondrial DNA polymerase γ (pol γ), used as a nutritional supplement.	Cell Mol Immunol, 2020, 10.1038/s41423-020-00545-z Am J Cancer Res, 2020, 1;10(5):1442-1454 Life Sci, 2020, 242:117159
S2239	Tubacin Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM in a cell-free assay, approximately 350-fold selectivity over HDAC1. Tubacin reduces the replication of the Japanese Encephalitis Virus via the decrease of viral RNA synthesis.	Cancers (Basel), 2020, 12(11)E3172 FASEB J, 2020, 10.1096/fj.202001508R Int J Mol Sci, 2020, 22(1)E142	Verification of Hdac6 deletion in knockout MEFs. Expression of HDAC6 and acetylation of tubulin were analyzed by immunoblotting.
S1289	Carmofur Carmofur (HCFU) is a highly potent acid ceramidase inhibitor, used in the treatment of breast and colorectal cancer.	Nat Struct Mol Biol, 2020, 7 Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S4227	Fidaxomicin Fidaxomicin (OPT-80, PAR-101) is a narrow spectrum macrocyclic antibiotic that inhibits RNA polymerase sigma subunit.	Sci Rep, 2020, 18;10(1):8159 PLoS One, 2020, 15(2):e0228509 Antiviral Res, 2019, 170:104570
S1907	Metronidazole Metronidazole, a synthetic antibacterial and antiprotozoal agent of the nitroimidazole class, is used against protozoa.	Bone Joint Res, 2020, 16;9(4):152-161
S1760	Rifapentine Rifapentine (MDL473) is an antibiotic, which inhibits DNA-dependent RNA polymerase activity, used to treat tuberculosis.	Front Microbiol, 2020, 10:2936 mSphere, 2018, 3(5)
S1778	Trifluridine Trifluridine (NSC 529182, NSC 75520) is an anti-herpesvirus antiviral agent by interacting viral DNA replication, used primarily on the eye.	Sci Adv, 2020, 6(49)eabd9443 Ocul Surf, 2019, 10.1016/j.jtos.2019.11.011 Oncol Lett, 2018, 15(5):6107-6114
S1790	Rifaximin Rifaximin is a RNA synthesis inhibitor by binding the β subunit of the bacterial DNA-dependent RNA polymerase, used to treat traveler's diarrhea caused by certain bacteria.
S1995	Procarbazine HCl Procarbazine HCl (NSC-77213) is a hydrochloride salt form of procarbazine which is a polyfunctional alkylating compound, used for the treatment of Hodgkin's lymphoma.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z Hum Cell, 2020, 10.1007/s13577-020-00425-8
S1784	Vidarabine Vidarabine is an antiviral drug by interfering with the synthesis of viral DNA, used to treat herpes simplex and varicella zoster viruses.	Neuron, 2017, 96(6):1290-1302 ACS Appl Mater Interfaces, 2016, 8(39):25818-25824 Biogerontology, 2016, 17(5-6):907-920
S1764	Rifampin Rifampin (Rimactane, Rifampicin) is a DNA-dependent RNA polymerase inhibitor, used to treat a number of bacterial infections.	Pharmacogenomics J, 2020, 10.1038/s41397-020-0160-7 Front Microbiol, 2020, 10:2936 Pharmacotherapy, 2019, 39(1):67-76
S3001	Clevudine Clevudine is an antiviral drug for the treatment of hepatitis B.
S1300	Tegafur (FT-207) Tegafur (FT-207, NSC 148958) is a substance being used in the treatment of some types of cancer.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z Hum Cell, 2020, 10.1007/s13577-020-00425-8
S1826	Nedaplatin Nedaplatin is a derivative of cisplatin and DNA damage agent for tumor colony forming units with IC50 of 94 μM.	Nat Commun, 2019, 10(1):5654 Cancer Res, 2018, 78(19):5694-5705 Oncol Lett, 2016, 12(5):4195-4202
S7470	Triapine Triapine (3-AP) is a potent ribonucleotide reductase (RNR) inhibitor with broad spectrum antitumor activity by inhibiting DNA synthesis. Phase 2.	Nat Commun, 2020, 11(1):3214 Cancer Chemother Pharmacol, 2020, 10.1007/s00280-020-04154-5 Onco Targets Ther, 2020, 13:6523-6537	(a) Quantification of p-RPA/ Rad51, 53BP1 and γH2AX in GBM01 cells treated with DMSO or triapine. (b) Quantification of p-RPA/Rad51, 53BP1 and γH2AX in GBM02 cells treated with DMSO or triapine.
S7757	6-Thio-dG 6-thio-dG is a nucleoside analog and telomerase substrate.	Clin Sci (Lond), 2020, 10.1042/CS20190890
S4297	Mupirocin Mupirocin is an isoleucyl t-RNA synthetase inhibitor, used in the treatment of bacterial skin infections.	Anaerobe, 2020, 62:102169 Life Sci, 2019, 224:51-57 Biogerontology, 2016, 17(5-6):907-920
S8376	Rbin-1 Rbin-1 (Ribozinoindole-1) is a potent chemical inhibitor of eukaryotic ribosome assembly. It inhibits recombinant full-length Mdn1's ATPase activity in vitro.
S9521	Pentostatin Pentostatin is a potent inhibitor of adenosine deaminase. The drug is effective in the treatment of many lymphoproliferative malignancies, particularly hairy-cell leukemia. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.	Nat Metab, 2020, 10.1038/s42255-020-0227-4
S5552	Amenamevir Amenamevir (ASP2151) is a potent helicase-primase inhibitor and a novel class of antiviral agent.	J Biomol Struct Dyn, 2020, 1-14
S8095	Tubercidin Tubercidin (7-deaza-adenosine), an adenosine analogue, is a nucleoside antibiotic. It is incorporated into DNA and inhibits polymerases, thereby inhibiting DNA replication and RNA and protein synthesis. This agent also exhibits antifungal and antiviral activities.	Mol Cell, 2020, 80(6):1104-1122.e9
S4035	Vitamin D2 Vitamin D2 (Ergocalciferol) is a selective inhibitor of mammalian DNA polymerase A (pol A) with IC50 of 123 μM.	Aging (Albany NY), 2020, 12
S7975	Favipiravir (T-705) Favipiravir (T-705) is a potent and selective RNA-dependent RNA polymerase inhibitor, used to treat influenza virus infections.	mBio, 2021, 12(1)e02754-20 Viruses, 2020, 22;12(3) pii: E351 Antiviral Res, 2020, 182:104902	(A) BoDV-1 infection was measured by IFA. BoDV-1 P40 was detected with a primary monoclonal antibody (red), nuclei were stained with DAPI (blue), merged image (scale bars: 50 μm). Favipiravir: T-705
S8328	CeMMEC1 HCl CeMMEC1 is an N-methylisoquinolinone derivative that inhibits the second bromodomain of TAF1 (IC50=0.9 μM).
S5484	Rimantadine Hydrochloride Rimantadine is an RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza. It works by inhibiting a viral protein called M2, which normally mediates the transport of acid ions across the influenza virion shell.	bioRxiv, 2020, 2020.08.12.246389
S4504	6-Mercaptopurine (6-MP) Monohydrate 6-Mercaptopurine (6-MP) Monohydrate is a widely used antileukemic agent and immunosuppressive drug that inhibits de novo purine synthesis through incorporation of thiopurine methyltransferase metabolites into DNA and RNA.
S7742	SCR7 SCR7 is a specific DNA Ligase IV inhibitor, which blocks nonhomologous end-joining (NHEJ).	Proc Natl Acad Sci U S A, 2020, 22;201918845 Cell Rep, 2020, 14;31(2):107518 Cell Rep, 2020, 33(2):108240	The start codon CUG of PTEN-long was mutated to AUG and PTENlong expression is significantly increased. gRNA1 and gRNA2 have similar efficiency in driving PTEN-long expression (lanes 1 and 2). Combined gRNA1 and gRNA2 (lane 3) did not enhance PTEN-long expression compared to lane 1 and 2. The ssODN is required for mutation of CTG to ATG through HDR and without which PTEN-long is not expressed (lane 4). PTEN-long cDNA cloned into pcDNA3.1 with CTG to ATG mutation was highly expressed in transfected HEK293T cells (lane 5). Lane 6 is protein ladder. Lanes 7–10 indicate that the combination of gRNA and ssODN is required to facilitate HDR occurrence and double-strand DNA break.
S4737	Psoralen Psoralen (Psoralene, Ficusin, Furocoumarin) is a naturally occurring furocoumarin that intercalates with DNA, inhibiting DNA synthesis and cell division.
S8146	Mitomycin C Mitomycin C is an antineoplastic antibiotic by inhibiting DNA synthesis, used to treat different cancers. Mitomycin C induces apoptosis in a caspases-dependent and Fas/CD95-independent manner.	Int J Radiat Biol, 2021, 1-16 Cell, 2020, 18;S0092-8674(20)30623-1. Cell Stem Cell, 2020, S1934-5909(20)30544-0	MTT results of three HCC cell lines at 72 h after indicated treatments. Three independent experiments were carried out.
S1973	Cyclocytidine HCl Cyclocytidine (NSC 145668) is the prodrug of cytarabine, which is a pyrimidine nucleoside analog that inhibits the DNA synthesis and used mainly in the treatment of leukemia.	Acta Biochim Biophys Sin (Shanghai), 2020, 14 pii: gmaa017 J Med Virol, 2019, 91(8):1440-1447 Int J Mol Sci, 2018, 19(6)
S3641	Osalmid Osalmid suppresses ribonucleotide reductase (RR) activity in a concentration-dependent manner, with a 50% RR activity-inhibitory concentration (IC50) of 8.23 μM.
S7449	CRT0044876 CRT0044876 (NSC 69877, 7-NO2-ICA) is a potent and selective APE1 inhibitor with IC50 of ~3 μM.	Nat Biotechnol, 2017, 35(5):463-474
S7445	E3330 E3330 is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.
S5293	Nimustine Hydrochloride Nimustine Hydrochloride (Nidran) is the hydrochloride salt of nimustine, a nitrosourea with antineoplastic activity that alkylates and crosslinks DNA, thereby causing DNA fragmentation, inhibition of protein synthesis, and cell death.
S5297	Vidarabine monohydrate Vidarabine (Spongoadenosine, Vira-A) is a nucleoside antibiotic with antiviral acitivity that interferes with the synthesis of viral DNA. It is used to treat herpes simplex and varicella zoster viruses.
S2794	Sofosbuvir (GS-7977) Sofosbuvir (PSI-7977, GS-7977) is a HCV NS5B polymerase inhibitor for the treatment of chronic hepatitis C virus (HCV) infection.	Cells, 2020, 17;9(4) pii: E1003 Antiviral Res, 2020, 185:104974 Sci Rep, 2020, 18;10(1):8159	Representative confocal microscope image showing phosphorylated Drp1 translocation to mitochondria and mitochondrial fission in the presence of Sofosbuvir. At 24 hours after treatment with Sofosbuvir (100 nM), Huh7 cells were immunostained with antibodies against TOM20 (red) and p-Drp1 (S616) (green). Nuclei are demarcated with white dotted circles. Treated (+) and untreated (–) cells are marked. In the zoomed images, the arrows indicate the colocalization of TOM20 and p-Drp1 (S616) in Sofosbuvir-treated cells (yellow spots).
S6115	Pyridoxal 5′-phosphate hydrate Pyridoxal 5′-phosphate (pyridoxal phosphate, Vitamin B6 phosphate, PAL-P, PLP), a vitamin B6 phosphate, is a coenzyme in a variety of enzymatic reactions.
S8434	B02 B02 is a small-molecule inhibitor of human RAD51 with an IC50 of 27.4 μM, but does not inhibit its E. coli homologue RecA (IC50 > 250 μM).	G3 (Bethesda), 2020, 4;10(5):1585-1597 Nat Commun, 2019, 10(1):1412 Neurooncol Adv, 2019,	HEK 293T cells were transfected with a total of 6 μg of plasmid DNA (2 μg pSG-I-SceI-HA, 2 μg pcDNA-HBZ-Myc-His or empty vector, and 2 μg the pDR-GFP reporter) and treated with 20 μM B02 for 48 h where indicated. Data shown are averages of results from three independent experiments, and error bars represent SEM (*, P ≤ 0.05 by Student's t test).
S8539	TAS-102 TAS-102 is an orally administered combination of a thymidine-based nucleic acid analogue, trifluridine, and a thymidine phosphorylase inhibitor, tipiracil hydrochloride.
S7637	DTP3 DTP3 is a selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor and is able to restore MKK7/JNK activation. DTP3 inhibits cancer-selective NF-κB survival pathway.
S8144	Halofuginone Halofuginone is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in mammal.	Sci Rep, 2020, 10(1):19723 Oncol Lett, 2020, 20(6):385 Res Sq, 2020, rs.3.rs-48659
S3669	Carmustine Carmustine (bis-chloroethylnitrosourea, BCNU, BiCNU) is a cell-cycle phase nonspecific alkylating antineoplastic agent and used in the treatment of brain tumors and various other malignant neoplasms.
S7679	YK-4-279 YK-4-279 is a potent inhibitor of EWS-FLI1 binding to RNA helicase A (RHA).	Clin Cancer Res, 2020, 21;clincanres35732019 Cancers (Basel), 2020, 12(11)E3205 Cancer Cell, 2019, 36(2):179-193	YK-4-279-induced cell apoptosis of NB cells by Western blot assay. SH-SY5Y cells were treated with YK-4-279 (0, 0.1 μM, 0.3 μM, 1 μM, 3 μM) for 24 h. Whole cell lysates were subjected to SDS-PAGE and immunoblotted with antibodies against PARP and Caspase 3 to detect apoptosis. β-actin was detected as loading control. YK-4-279-induced apoptosis of NB cell line SH-SY5Y by FACS. Cells were treated with YK-4-279 (0, 1 μM, 3 μM) for 24 h, and then stained by PI and analyzed by FACS.
S4236	Proflavine Hemisulfate Proflavine Hemisulfate is a topical antiseptic by interchelating DNA, thereby disrupting DNA synthesis and leading to high levels of mutation in the copied DNA strands.
S7718	BMH-21 BMH-21 is a DNA intercalator, which binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription.	Front Genet, 2020, 11:43 Biochem Biophys Res Commun, 2019, 10.1016/j.bbrc.2019.06.057 Cancer Invest, 2019, 37(6):242-252	Pharmacological and siRNA perturbations in HEK293 cells suggest that mTORC1 also modulates cytoplasmic rheology through ribosome crowding in mammals.
S4239	Bergapten Bergapten is a psoralen that can be photoactivated and is capable of crossing-linking DNA, covalently modifying proteins and lipids, and consequently inhibiting cell replication.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z Hum Cell, 2020, 10.1007/s13577-020-00425-8
S4782	5-methoxyflavone 5-methoxyflavone is a novel DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity.
S4537	Oxolinic acid Oxolinic acid (Urinox, NSC 110364) is a quinolone antibiotic, inhibiting the enzyme DNA gyrase and DNA synthesis.It also acts as a dopamine reuptake inhibitor.
S7546	Pritelivir (BAY 57-1293) Pritelivir (BAY 57-1293, AIC316) is a potent helicase primase inhibitor, exhibiting antiviral effect on herpes simplex virus (HSV) with IC50 of 20 nM for both HSV-1 and HSV-2.
S8329	CeMMEC13 CeMMEC13 is an isoquinolinone that selectively inhibits the second bromodomain of TAF1 (IC50 = 2.1 µM).
S5582	Cytarabine hydrochloride Cytarabine is a pyrimidine nucleoside analog that is used mainly in the treatment of leukemia. It is an antimetabolite antineoplastic agent that inhibits the synthesis of DNA.	Cell Death Dis, 2021, 12(1):9 Cytometry A, 2021, 10.1002/cyto.a.24308 Am J Cancer Res, 2020, 10(10):3302-3315
S7419	Blasticidin S HCl Blasticidin S HCl is a nucleoside antibiotic isolated from Stretomyces girseochromogenes, and acts as a DNA and protein synthesis inhibitor, used to select transfected cells carrying bsr or BSD resistance genes.	Theranostics, 2021, 11(6):2966-2986 Nat Commun, 2020, 11(1):5842 Cells, 2020, 9(1)
S4288	Chloroambucil Chloroambucil (Chlorambucil) is a nitrogen mustard alkylating agent, used in the treatment of chronic lymphocytic leukemia.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S8246	RK-33 RK-33 is a first-in-class small molecule inhibitor of DDX3 (a RNA helicase) and causes G1 cell cycle arrest, induces apoptosis, and promotes radiation sensitization in DDX3-overexpressing cells.	Mol Cell, 2020, 80(6):1104-1122.e9 Proc Natl Acad Sci U S A, 2020, 117(45):28092-28101 J Virol, 2020, 6;94(2):e01679-19
S3168^新	cis-Resveratrol cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively.
S6893^新	PIN1 inhibitor API-1 PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor with IC50 of 72.3 nM. PIN1 inhibitor API-1 targets Pin1 peptidyl-prolyl isomerase domain and inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 up-regulates miRNA biogenesis by retaining active XPO5 conformation and suppresses HCC development.
S2427^新	Triglycidyl Isocyanurate (Teroxirone) Triglycidyl Isocyanurate (Teroxirone, Tris(2,3-epoxypropyl) Isocyanurate, TGI, TGIC) is a triazene triepoxide with antineoplastic activity. It inhibits growth of human non-small cell lung cancer cells by activating p53. Triglycidyl Isocyanurate alkylates and cross-links DNA, thereby inhibiting DNA replication. Triglycidyl Isocyanurate is also used in various polyester powder coatings in the metal finishing industry.
S8326	Saccharin 1-methylimidazole (SMI) Saccharin 1-methylimidazole (SMI) is considered a general-purpose activator for DNA and RNA synthesis.
S1334	Flupirtine maleate Flupirtine maleate is the salt form of Flupirtine, which is a centrally acting non-opioid analgesia, is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties.	Assay Drug Dev Technol, 2019, 17(7):310-321
S9603^新	Lurbinectedin Lurbinectedin (PM01183, PM-1183, LY-01017, Tryptamicidin, Zepsyre, ZEPZELCA), a DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity. Lurbinectedin inhibits RMG1 and RMG2 cell growth with IC50 of 1.25 nM and 1.16 nM, respectively.
S1214	Bleomycin Sulfate Bleomycin Sulfate (NSC125066) is a glycopeptide antibiotic and an anticancer agent for squamous cell carcinomas (SCC) with IC50 of 4 nM in UT-SCC-19A cells.	Sci Transl Med, 2020, 12(530) Mol Cell, 2020, 22 pii: S1097-2765(20)30231-8 Nat Commun, 2020, 29;11(1):2086
S6854^新	Triazavirin Triazavirin (TZV, Riamilovir) is a novel antiviral drug, a nucleoside analogue of nucleic acid that inhibits the synthesis of viral RNA and DNA and replication of genomic fragments. Triazavirin is active against influenza and a number of other viruses. Triazavirin is an effective protective agent on the transmission stage of influenza.
S1237	Temozolomide Temozolomide (CCRG81045, NSC 362856, TMZ) is a monofunctional SN-1 alkylating agent that can modify nitrogen atoms in the DNA ring and the extracyclic oxygen group, chemically converted to MTIC and degrades to methyldiazonium cation, which transfers methyl groups to DNA at physiologic pH. A DNA damage inducer in L-1210 and L-1210/BCNU cells. Temozolomide induces apoptosis and exhibits antitumor activity.	Theranostics, 2021, 11(4):1991-2005 Hum Mol Genet, 2021, ddab009 Exp Ther Med, 2021, 21(2):175	C57BL/6 mice were implanted in the striatum with citrine-GL26-Cherry-HMGB1, which were stably transfected to express the YFP citrine and HMGB1 fused to red fluorescent protein cherry. Fourteen days later, they were treated with saline, Ad-TK+Ad-Flt3L, or Ad-TK+Ad-Flt3L+TMZ (temozolomide). Five days after treatment, the cellular location of cherry-HMGB1 in these cells was assessed by confocal microscopy. Arrows, tumor cells (green) with cytoplasmic HMGB1 (red).
S1212	Bendamustine HCl Bendamustine (SDX-105, Cytostasane) HCl is a DNA-damaging agent with IC50 of 50 μM in cell-free assay.	Oncoimmunology, 2020, 30;9(1):1758011 Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z	Fractional Analysis of Combination Therapy of SGI-1776 With Bendamustine in B-Cell Lymphoma.
S1840	Lomustine Lomustine (nsc79037, Gleostine, CeeNU, CCNU) inhibits cancer cells by damaging the DNA and stops cells from dividing.	Nature, 2020, 580(7804):517-523. Cancer Cell Int, 2020, 19;20:58 Vet Comp Oncol, 2020, 10.1111/vco.12656	Initial range finding concentration response analysis of the cytotoxic effects of (A) lomustine (IC50 = 12 μM) and (B) vincristine (IC50 = 1.5 nM) on D283 Med in a clonogenic assay of cell survival
S7918	Bromodeoxyuridine (BrdU) Bromodeoxyuridine (BrdU) is a nucleoside analog that competes with thymidine for incorporation into DNA, and used in the detection of proliferating cells.	Cell Prolif, 2020, 28;e12818 Biomed Pharmacother, 2019, 109:1951-1959 Biomedicine & Pharmacotherapy, 2018, 10.1016/j.biopha.2018.11.029	Immunofluorescence microphotographs of proliferating ARPE-19 cell with BrdU (red) and DAPI (blue) staining after ARPE-19 cells were untreated or treated with AF (1.0 μM) in the absence or presence of EGF (100ng/ml) for 24 hours and then subjected to BrdU labeling for 4 hours, followed by immunostaining with anti-BrdU antibody and DAPI. Scale bar = 20μm.
S4888	Guanine Guanine is one of the four main nucleobases found in the nucleic acids DNA and RNA.
S5505	2’-deoxyuridine 2'-deoxyuridine (dU, 2'-dU) is frequently halogenated to create thymidine analogues useful for studies of DNA synthesis and degradation mechanisms.
S6359	Purine Purine is a heterocyclic aromatic organic compound which plays crucial roles in DNA and RNA. It is also significant components in a number of other important biomolecules, such as ATP, GTP, cyclic AMP, NADH, and coenzyme A.
S4194	Azaguanine-8 Azaguanine-8 (NSC-749, SF-337, SK 1150) is a purine analogs showing antineoplastic activity by competing with guanine in the metabolism.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z Hum Cell, 2020, 10.1007/s13577-020-00425-8
S4803	Thymidine Thymidine (Deoxythymidine, 2'-Deoxythymidine, 5-Methyldeoxyuridine) is a pyrimidine nucleoside that is composed of the pyrimidine base thymine attached to the sugar deoxyribose. As a constituent of DNA, thymidine pairs with adenine in the DNA double helix.
S1981	Adenine Adenine is a purine derivative and a nucleobase with a variety of roles in biochemistry.	PLoS Pathog, 2020, 16;16(3):e1008341
S1983	Adenine HCl Adenine HCl is a hydrochloride salt form of adenine which is a purine derivative and a nucleobase with a variety of roles in biochemistry.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z Hum Cell, 2020, 10.1007/s13577-020-00425-8
S1982	Adenine sulfate Adenine sulfate is a sulfate salt form of adenine which is a purine derivative and a nucleobase with a variety of roles in biochemistry.
S6077	Cytidine 5′-triphosphate (disodium salt) Cytidine 5'-triphosphate is a pyrimidine nucleoside triphosphate that is involved in a variety of biochemical reactions. It is used in the synthesis of RNA by RNA polymerases.
S5374	5'-Cytidylic acid 5'-Cytidylic acid (Cytidine monophosphate, Cytidine 5'-phosphate) is a nucleotide that is used as a monomer in RNA.
S5384	UTP Trisodium Salt Uridine-5'-triphosphate (UTP) is a pyrimidine nucleoside triphosphate and a substrate for the synthesis of RNA during transcription.
S3190	N6-methyladenosine (m6A) N6-methyladenosine (m6A, NSC-29409) is a base modified analog of adenosine and is found as a minor nucleoside in natural RNAs.	Nat Genet, 2020, 10.1038/s41588-020-0677-3 Nat Cell Biol, 2019, 21(5):651-661 Nat Commun, 2019, 10(1):5126	(A) Comparison of ribose modification across the RNA species. Modified nucleosides of MRC-5 cells were aligned in terms of modification type and then RNA species. Data are presented as means ± STD, n = 3. (B) tRNA modification profiles of cancer tissues. Data are presented as means ± STD, n = 5.
S2029	Uridine Uridine (NSC 20256) is a nucleoside, contains a uracil attached to a ribose ring via a β-N1-glycosidic bond.
S9382	Thymine Thymine (5-methyluracil) is one of the four nucleobases in the nucleic acid of DNA.

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S1166	Cisplatin Cisplatin (cisplatinum, cis-diamminedichloroplatinum II, CDDP) is an inorganic platinum complex, which is able to inhibit DNA synthesis by conforming DNA adducts in tumor cells. Cisplatin activates ferroptosis and induces autophagy. Solutions are best fresh-prepared.	Theranostics, 2021, 11(6):2860-2875 Mol Cancer, 2021, 20(1):17 Acta Pharmacol Sin, 2021, 10.1038/s41401-020-00577-1	Cell viabilities with increasing concentrations of cisplatin (CP) and doxorubicin (DOXO) under normoxic and hypoxic condition for 48 hours were determined by MTT assay. IC50 values are presented as the means ?SDs (n=4) and * denotes p<0.05.
S1149	Gemcitabine HCl Gemcitabine HCl (LY188011) is a DNA synthesis inhibitor with IC50 of 50 nM, 40 nM, 18 nM and 12 nM in PANC1, MIAPaCa2, BxPC3 and Capan2 cells, respectively.	Oncogene, 2021, 10.1038/s41388-020-01634-z Cell Death Dis, 2021, 12(1):72 Invest New Drugs, 2021, 10.1007/s10637-020-01003-3	RNA incorporating drugs induce SG assembly. HeLa cells were treated with the RNA incorporating agents 5-azacytidine (50 uM) and 6-thioguanine (10 uM), or the DNA incorporating agents trifluorothymidine (10 uM) and gemcitabine (100 nM) for 72 h. Subsequently, the cellular localization of the SG marker protein TIAR (green) and the P-body marker protein DCP1 (red) was analyzed. Nuclei were stained with Hoechst. Scale bars represent 20 um.
S1135	Pemetrexed Pemetrexed (LY-231514) is a novel antifolate and antimetabolite for TS, DHFR and GARFT with K_i of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.	Nat Commun, 2020, 14;11(1):1825 J Hematol Oncol, 2020, 1;13(1):40 Cell Death Dis, 2020, 11(11):945	Role of PARP and BER in the synergy between PTX and GMX in A549 cells. Cells were pretreated ±1 umol/L olaparib (2 hours) then sequentially ±150 nmol/L PTX (24 hours), then ± GMX 12 nmol/L (48 hours). PAR modification of proteins and γ-H2AX levels were measured in extracts treated as in A by Western blotting.
S1215	Carboplatin Carboplatin (JM-8, CBDCA, NSC 241240) is a DNA synthesis inhibitor by binding to DNA and interfering with the cell's repair mechanism in A2780, SKOV-3, IGROV-1, and HX62 cells. Solutions are best fresh-prepared.	Eur J Pharmacol, 2021, 895:173887 Nat Commun, 2020, 24;11(1):1975 Nat Commun, 2020, 22;11(1):2573	Detection of apoptotic responses was found to increase in epimorphin-treated A1847 with increasing concentrations of carboplatin compared to those of the untreated controls. Data were normalized to the controls and are represented as means ± S.D. [*p<0.05 compared with control]. Images of apoptotic cells were captured at 10X magnification, with at least 3 images per well, using an upright phase-contrast microscope (T3.15A; Fisher Scientific).
S3360^新	Bis(2-ethylhexyl) phthalate Bis(2-ethylhexyl) phthalate (Dioctyl phthalate, DOP, Diplast O, ESBO-D 82, Ergoplast FDO, Ergoplast FDO-S, Etalon) induces DNA strand breaks and gene expression alterations in larval zebrafish Danio rerio.
S3356^新	Phosphonoacetic acid Phosphonoacetic acid (PAA) is an active endogenous metabolite that possesses a restricted potential to block DNA biosynthesis. Phosphonoacetic acid exhibits anti-viral activities.
S3009^新	Menthone Menthone is one of the main volatile components of the essential oil of peppermint (Mentha piperita L.). Menthone is used as antioxidant agent and has a good compensatory effect with significant reduction in DNA damages in sperm cells.
S9718^新	TK216 TK216 is a potent inhibitor targeting E26 transformation specific (ETS) factors via blocking the protein-protein interaction with RNA helicases. TK216 exhibits antilymphoma activity.
S9649^新	Acelarin (NUC-1031) Acelarin (NUC-1031, Fosgemcitabine palabenamide, CPF-31, MTL-007, GTPL7389), a prodrug based on an aryloxy phosphoramidate derivative of gemcitabine, is a DNA synthesis inhibitor with EC50 of 0.2 nM.
S8977^新	BCH001 BCH001 is a specific PAPD5 inhibitor that restores telomerase activity and telomere length in dyskeratosis congenita (DC) patient induced pluripotent stem cells. PAPD5 is a noncanonical poly(A) polymerase with an unusual RNA-binding motif.
S8850^新	JH-RE-06 JH-RE-06 is a potent REV1-REV7 interface inhibitor with an IC50 of 0.78 μM and Kd value of 0.42 μM, disrupting REV1-POL ζ-mediated mutagenic translesion synthesis (TLS).
S7418^新	Cycloheximide Cycloheximide (Actidione, Naramycin A, CHX), an antifungal antibiotic, is an eukaryote protein synthesis inhibitor with IC50 of 532.5 nM and 2880 nM for protein synthesis and RNA synthesis in vivo, respectively. Cycloheximide suppresses ferroptosis and inhibits autophagy.	Theranostics, 2021, 11(2):700-714 Theranostics, 2021, 11(6):2655-2669 ACS Nano, 2020, 10.1021/acsnano.0c08947
S6848^新	3'-Fluoro-3'-deoxythymidine (Alovudine) 3'-Fluoro-3'-deoxythymidine (Alovudine, CL 184824, FddThd, FLT, MIV-310) is a potent inhibitor of polymerase γ and reverse transcriptase that can be used in the treatment of HIV infection. 3'-Fluoro-3'-deoxythymidine (Alovudine) is also a marker of DNA synthesis that can be used as an early response biomarker in the chemotherapy of pancreatic cancer.
S0816^新	Brr2 Inhibitor C9 Brr2 inhibitor C9 (Brr2 Inhibitor 9) is an allosteric inhibitor of the spliceosomal RNA helicase Brr2. Brr2 is implicated in autosomal-dominant retinitis pigmentosa a group of progressive retinal degenerative disorders.
S0780^新	Oncrasin-1 Oncrasin-1 (Onc-1) is a potent RNA polymerase II inhibitor with antitumor activity that kills various human lung cancer cells with K-Ras mutations. Oncrasin-1 drives abnormal aggregation of protein kinase C iota (PKCι) in nucleus of sensitive cells but not in resistant cells.
S0469^新	ML216 ML216 (CID-49852229) is a potent and selective inhibitor of the DNA unwinding activity of BLM(Bloom’s syndrome protein) with antitumor activity. ML216 inhibits helicases with IC50 of 0.97 μM and 2.98 μM for BLM^636-1298 and BLM^full-length, respectively.
S0280^新	Madrasin Madrasin (DDD00107587) is a potent and cell-penetrant pre-mRNA splicing inhibitor. Madrasin interferes with the early stages of spliceosome assembly and stalls spliceosome assembly at the A complex.
S0102^新	L 189 L 189 is a novel human DNA ligase inhibitor with IC50 of 5 μM, 9 μM and 5 μM for hLigI, hLigIII and hLigIV, respectively. L 189 inhibits base excision repair (BER) and non-homologous end joining (NHEJ). L 189 specifically sensitizes cancer cells to DNA damage.
S0063^新	RG3039 RG3039 (PF-06687859, PF 6687859, Quinazoline 495) is an orally bioavailable and brain-penetrant inhibitor of the mRNA decapping enzyme DcpS with IC50 of 4.2 nM and IC90 of 40 nM, respectively.
S0054^新	D-I03 D-I03 is a selective inhibitor of RAD52 with Kd of 25.8 µM. D-I03 inhibits ssDNA annealing by RAD52 and D-loop formation with IC50 of 5 µM and 8 µM, respectively.
S2600^新	Fexinidazole Fexinidazole (HOE-239, Fexinidazole Winthrop) is a 5-nitroimidazole derivative. Fexinidazole is a DNA synthesis inhibitor and the only, all-oral agent for Human African Trypanosomiasis(HAT or sleeping sickness).
S8932^新	Remdesivir (GS-5734) Remdesivir (GS-5734), a monophosphoramidate prodrug of an adenosine analog, is an investigational broad-spectrum antiviral agent with in vitro activity against multiple RNA viruses, including Ebola and CoV.	Nat Commun, 2021, 12(1):668 mBio, 2021, 12(1)e02754-20 Antiviral Res, 2021, 187:105015
S1491	Fludarabine Fludarabine (FaraA, Fludarabinum) is a STAT1 activation inhibitor which causes a specific depletion of STAT1 protein (and mRNA) but not of other STATs. Also a DNA synthesis inhibitor in vascular smooth muscle cells. Fludarabine induces apoptosis.	Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19 Cell Metab, 2020, 31(3):564-579	Normal human KC pretreated with STAT1 inhibitor (fludarabine [10 uM]) or STAT3 inhibitor (STA-21 [2 uM]) for 24 h. The mRNA levels of hBD2 and hBD3 were assessed by qRT-PCR.
S1224	Oxaliplatin Oxaliplatin (L-OHP) is a DNA alkylating agent that activates autophagy. Oxaliplatin inhibits DNA synthesis by conforming DNA adducts in RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2, and HT-144 cells. DMF is recommended for dissolution. Solutions are best fresh-prepared.	Nat Microbiol, 2021, 10.1038/s41564-020-00831-6 Mol Cancer, 2021, 20(1):10 Adv Biol Regul, 2021, S2212-4926(20)30091-9	Immunocytochemical staining of SW620 (metastatic) cells after treatment with 10 uM oxaliplatin (F) or 10 uM ginsenosides 20(S)-Rg 3 (G) and negative staining (H). Cells demonstrated differential expression of histone H4.
S2684	CX-5461 CX-5461 is an inhibitor of rRNA synthesis, selectively inhibits Pol I-driven transcription of rRNA with IC50 of 142 nM in HCT-116, A375, and MIA PaCa-2 cells, has no effect on Pol II, and possesses 250- to 300-fold selectivity for inhibition of rRNA transcription versus DNA replication and protein translation.	Sci Rep, 2021, 11(1):360 Nat Commun, 2020, 11(1):4287 Nucleic Acids Res, 2020, 18;gkaa344	The specific Pol I inhibitor CX-5461 causes nucleolar disruption, blocks LTP maintenance and Fsk-induced synthesis of new rRNA. DAPI staining (blue; A, B,C) shows the area of the nucleus. Nomarski images (grey; G, H,I) show the area of the nuclei and nucleoli (arrowheads). Application of Pol I specific inhibitor CX-5461 (200 nM) causes nucleolar disruption as indicated by the distribution of fibrillarin (green); compare A, D to B, E and C, F.
S1209	Fluorouracil (5-Fluorouracil, 5-FU) Fluorouracil (5-Fluorouracil, 5-FU, NSC 19893) is a DNA/RNA synthesis inhibitor, which interrupts nucleotide synthetic by inhibiting thymidylate synthase (TS) in tumor cells. Fluorouracil induces apoptosis and can be used in the treatment of HIV.	Molecules, 2021, 26(2)E334 Biosci Rep, 2021, BSR20200842 Int J Radiat Biol, 2021, 1-16	DNA-PKcs suppression mediated ROS production and GSH content in HepG2 cells exposed to CDDP and 5-Fu. a DNA-PKcs inhibition promoted ROS production in HepG2 cells treated with indicated concentrations of CDDP and 5-Fu. DCFH-DA fluorescent analysis was performed to assess the ROS level. Data presented were mean ?SD of three independent experiments.
S1156	Capecitabine Capecitabine (RO 09-1978) is a tumor-selective fluoropyrimidine carbamate, which achieves higher intratumoral 5-FU level with lower toxicity than 5-FU. Capecitabine treatment of HCT-15 cells causes condensation of DNA and induces apoptosis.	Cancer Lett, 2020, 28;476:67-74 Acta Biomater, 2020, S1742-7061(20)30751-0 Cancer Cell Int, 2020, 19;20:58	Growth curve of human colon cancer xenografts in nude mice treated with orally administered vehicle or capecitabine at 360 mg/kg (n = 10–12 per cell line).
S1229	Fludarabine Phosphate Fludarabine Phosphate (F-ara-A, NSC 312887) is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.	Exp Neurol, 2020, S0014-4886(20)30337-X Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8	Imatinib mesylate (IM) in combination of F-AMP significantly inhibits Ki67 and c-KIT expression in GIST-T1 tumor xenografts. Tumors were collected on the day after the last treatment and were then subjected to H&E staining and immunohistochemical detection of Ki67, c-KIT, and cleaved caspase-3 expression. Representative images of H&E staining and immunohistochemical staining of Ki67, c-KIT, and cleaved caspase-3 in mice tumors. Arrows indicate the decrease in cellularity and the increase in stromal fibrosis. Magnification, x 400.
S1117	Triciribine Triciribine (NSC 154020, VD-0002, vqd-002, API-2) is a DNA synthesis inhibitor, also inhibits Akt in PC3 cell line and HIV-1 in CEM-SS, H9, H9IIIB, U1 cells with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. Phase 1/2.	Mol Cancer Ther, 2020, molcanther.0369.2020 Cell Oncol (Dordr), 2020, 8 Molecules, 2020, 25(19)E4505	Effect of triciribine on the migration of (A) FaDu and (B) Hep2 cells. The cells were treated with 5 µM triciribine for different periods of time. *P<0.05 vs. control. Hpf, high-power field.
S1516	Cidofovir Cidofovir (HPMPC) suppresses virus replication by selective inhibition of viral DNA synthesis.	Nat Biotechnol, 2019, 37(3):303-313 J Virol, 2019, 93(4) Antiviral Res, 2019, 162:178-185	The copy numbers of the intracellular viral DNA were directly extracted from cells and were quantified by qPCR using primers specific for the KSHV ORF73 gene. Then each sample was normalized to the amount of the GAPDH gene (C), CDV (20 µM) was used as a positive control. CDV:Cidofovir.
S1648	Cytarabine Cytarabine (Cytarabin, Ara-C, Arabinofuranosyl Cytidine) is an antimetabolic agent and DNA synthesis inhibitor with IC50 of 16 nM in wild-type CCRF-CEM cells. Cytarabine induces autophagy and apoptosis.	Cell Death Dis, 2021, 12(1):9 Cytometry A, 2021, 10.1002/cyto.a.24308 Haematologica, 2020, haematol.2020.246843	Viability and CI vs Fa after 24-h exposure to cytarabine alone or in combination with ABT-199 in Riva, U2932 and VavP-Bcl2/c-MYC murine tumor cells. Viability shown at 500 nM (500 ng/ml for cytarabine; quadruplicates±s.e.m.).
S1714	Gemcitabine Gemcitabine (LY-188011, NSC 613327), a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy. Gemcitabine induces a potent p53-dependent apoptosis.	Cell Death Dis, 2021, 12(1):72 Invest New Drugs, 2021, 10.1007/s10637-020-01003-3 Int J Radiat Biol, 2021, 1-16	RNA incorporating drugs induce SG assembly. HeLa cells were treated with the RNA incorporating agents 5-azacytidine (50 uM) and 6-thioguanine (10 uM), or the DNA incorporating agents trifluorothymidine (10 uM) and gemcitabine (100 nM) for 72 h. Subsequently, the cellular localization of the SG marker protein TIAR (green) and the P-body marker protein DCP1 (red) was analyzed. Nuclei were stained with Hoechst. Scale bars represent 20 um.
S1213	Nelarabine Nelarabine (506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.	Nat Cell Biol, 2020, 20 Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8	b) Western blot analysis documenting cleavage of caspase-8, caspase-9, caspase-3, and PARP by nelarabine. Cells were treated with nelarabine (5 μM for JURKAT, P12-ICHIKAWA, and DND-41 cells, 2 μM MOLT-4 cells) for the indicated times, collected, and then lysed. Fifty micrograms of each lysate were electrophoresed on SDS-PAGE gels followed by transfer onto a nitrocellulose membrane. c) Nelarabine induces a decrease in the phosphorylation status of critical components of the PI3K/AKT/mTOR signaling pathway, as well as p-ERK (Thr202) levels in T-ALL sensitive cell lines. Western blot analysis documenting the reduction of p-AKT (Ser473), p-S6RP, p-GSK3β (Ser9), and p-ERK (Thr202). Antibody to β-actin served as a loading control. Molecular weights are indicated on the right
S1373	Daptomycin Daptomycin (LY146032) is a novel antibiotic with rapid in vitro bactericidal activity against gram-positive organisms.	Sci Adv, 2020, 6(34):eaba8968 Front Microbiol, 2020, 21;11:646 PLoS One, 2020, 15(2):e0228509	Same experiment as in Figure 2 with fluorescent daptomycin shown as confocal images. A 7/3 DOPC/DOPG GUV (including 1% Rh-PE) was introduced at time zero into a solution containing 1 uM daptomycin with 0.5 uM BODIPY-daptomycin and 1 mM Ca2+. To show colocalization of lipid and peptide in aggregates, confocal images were taken: red for RH-PE and green for BODIPY-daptomycin. As the protrusion length decreased, aggregates appeared on the GUV surface containing both lipid and peptide. The scale bar is 10 um.
S3035	Daunorubicin HCl Daunorubicin HCl (Daunomycin) inhibits both DNA and RNA synthesis and inhibits DNA synthesis with K_i of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis.	Int J Radiat Oncol Biol Phys, 2021, 109(1):60-72 Haematologica, 2020, 12;haematol.2019.233445 Cancer Cell Int, 2020, 19;20:58	A) MV411 or B) Kasumi 1 cells were incubated with YM155 (0.25 x IC50) in the presence or absence of i) 0.5 x IC50 or ii) 1 x IC50 of Daunorubicin or iii) 0.5 x IC50 or iv) 1 x IC50 of Cytarabine for 72h. Following 72h treatment, cells were subject to a resazurin reduction assay. Percentages were normalised to DMSO controls. Column, mean of 3 independent experiments; Bars, SEM. p<0.05, p<0.01, **p<0.005. Students t-test. Similar trends were observed with 0.5 x and 1 x IC50 of YM155 in combination with Daunorubicin or Cytarabine (data not shown).
S1199	Cladribine Cladribine (2-CdA, 2-chlorodeoxyadenosine) is an adenosine deaminase inhibitor for U266, RPMI8226, and MM1.S cells with IC50 of approximately 2.43 μM, 0.75 μM, and 0.18 μM, respectively.	Nat Commun, 2020, 29;11(1):2086 PLoS Pathog, 2020, 16;16(3):e1008341 Front Immunol, 2020, 11:616570
S1192	Raltitrexed Raltitrexed (ZD-1694) is a thymidylate synthase inhibitor with an IC50 of 9 nM for the inhibition of L1210 cell growth.	Anal Chem, 2020, 10.1021/acs.analchem.0c02756 Int J Mol Sci, 2020, 21(12):E4452 EBioMedicine, 2019, 48:289-300	Fig. 1. Raltitrexed dose-response curve. HEK293 parental and MRP5 transfected cells were plated in a 96-well plate at a density of 4000 cells/well in complete DMEM (10% FBS, 1% Pencillin/streptomycin) and allowed to incubate for 24h at 37°C, 5% CO2. Raltirexed was added and the cells allowed to incubate for 72h. Total DNA present in each well was then quantified using Cyquant® cell proliferation assay. Results show Total DNA as % of the DMSO-only control wells. Experiment was done in triplicate.
S1218	Clofarabine Clofarabine inhibits the enzymatic activities of ribonucleotide reductase (RNR) (IC50 = 65 nM) and DNA polymerase. Clofarabine induces autophagy and apoptosis.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8 Hum Cell, 2020, 10.1007/s13577-020-00420-z	Immunoblot analysis of cell lysates of NCI-H929 cells treated with CLO (5 μM, 3-48 h) GAPDH served as the loading control for each membrane, and data are representative of at least two independent experiments
S1302	Ifosfamide Ifosfamide (NSC109724, Isophosphamide) is a nitrogen mustard alkylating agent used in the treatment of cancer.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8 Hum Cell, 2020, 10.1007/s13577-020-00420-z	Chemotherapeutic response. Ifosfamide was applied at different concentrations on Lipo-DUE1, Lipo246, and PLS-1 for 72 h. Subsequently, cell viability was determined by MTS assay at a wavelength of 490 nm. Values represent the mean±S.D. of triplicates
S2678	NSC 207895 NSC 207895 (XI-006) suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase.	Genes Dev, 2020, 34(7-8):526-543 Oncotarget, 2020, 11(46):4224-4242 Sci Rep, 2019, 9(1):1897	Median overall survival of mice (n = 5 mice in vehicle and PYR-41; n = 4 mice in NSC group) inoculated with IOWA-1T xenografts were increased to 43 ± 0.5 and 39 ± 2 days with PYR-41 (PYR) and NSC-207895 (NSC), respectively, compared with a vehicle-treated control group 33 ± 1 days (*p < 0.05).
S1221	Dacarbazine Dacarbazine (DTIC-Dome) is a triazene derivative with antineoplastic activity. Dacarbazine alkylates and cross-links DNA during all phases of the cell cycle, resulting in disruption of DNA function, cell cycle arrest, and apoptosis; used in the treatment of various cancers.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S1896	Hydroxyurea Hydroxyurea (nci-c04831, nsc32065) is an antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase. Hydroxyurea activates apoptosis and autophagy. Hydroxyurea is used to treat HIV infection.	Carcinogenesis, 2021, bgab002 Haematologica, 2020, 12;haematol.2019.233445 Cancer Cell Int, 2020, 19;20:58	Lethally irradiated C57BL/6 recipient mice were injected with a 1:1 mixture of GFP+JAK2(V671F) and wild-type bone marrow cells. Five weeks later, mice were treated with vehicle (C), hydroxyurea (H; 30 mg/kg twice daily IP), ruxolitinib (R; 30 mg/kg twice daily oral gavage), BMN673 (B; 0.33 mg/kg IV), H+R, H+B, R+B, and H+R+B for 3 weeks. Percentage of GFP+JAK2(V617F) was measured in (panel B) bone marrow cells, (panel C) splenocytes, and (panel D) peripheral blood leukocytes; (panel E) number of GFP+JAK2(V617F) Lin−Sca1+c-Kit+ (LSK) cells per 106 bone marrow cells was calculated, too. P < .05, P < .05, and **P < .05 when compared with control, single treatment, and double treatment, respectively, from 6 to 7 mice using the Student t test.
S1807	Aciclovir Acyclovir (Acyclovir, Acycloguanosine, Zovirax) is a synthetic nucleoside analogue active against herpesviruses. Acyclovir induces cell cycle perturbation and apoptosis in Jurkat leukemia cells.	Sci Adv, 2020, 6(49)eabd9443 ACS Infect Dis, 2020, 6(11):2926-2937 Antimicrob Agents Chemother, 2020, AAC.00245-20	(A) HONE1 and (B) HK1-EBV cells were treated with TPA (40 ng/ml) and SB (3 mM) for EBV induction. After 3 h, uninduced and induced HONE1 and HK1-EBV cells were treated with the vehicle control (0.006% DMSO) or indicated concentrations of berberine for 48 h. Subsequently, the culture medium was harvested for quantitative-PCR analysis with EBNA1 primers. Each sample was normalized to the amount of the GAPDH gene; *p<0.05, compared with the control group.
S1299	Floxuridine Floxuridine (Deoxyfluorouridine, FUDR, NSC 27640) is an antineoplastic antimetabolite, used in the treatment of colon carcinoma and colorectal cancer that has metastasized to the liver.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S1305	Mercaptopurine (6-MP) Mercaptopurine is a widely used antileukemic agent and immunosuppressive drug that inhibits de novo purine synthesis through incorporation of thiopurine methyltransferase metabolites into DNA and RNA.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S1384	Mizoribine Mizoribine (Bredinin, NSC 289637) is an imidazole nucleoside and an immunosuppressant that inhibits HCV RNA replication with IC50 of ~ 100 μM for anti-HCV activity. Mizoribine is a selective inhibitor of inosine-5'-monophosphate dehydrogenase (IMPDH) and guanosine monophosphate synthetase. Mizoribine also inhibits SARS-CoV.	JCI Insight, 2020, 9;5(7):e135071 Cancer Cell, 2017, 32(5):624-638
S1949	Menadione Menadione(Vitamin K3), a fat-soluble compound, is an inhibitor of Cdc25 phosphatase and mitochondrial DNA polymerase γ (pol γ), used as a nutritional supplement.	Cell Mol Immunol, 2020, 10.1038/s41423-020-00545-z Am J Cancer Res, 2020, 1;10(5):1442-1454 Life Sci, 2020, 242:117159
S2239	Tubacin Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM in a cell-free assay, approximately 350-fold selectivity over HDAC1. Tubacin reduces the replication of the Japanese Encephalitis Virus via the decrease of viral RNA synthesis.	Cancers (Basel), 2020, 12(11)E3172 FASEB J, 2020, 10.1096/fj.202001508R Int J Mol Sci, 2020, 22(1)E142	Verification of Hdac6 deletion in knockout MEFs. Expression of HDAC6 and acetylation of tubulin were analyzed by immunoblotting.
S1289	Carmofur Carmofur (HCFU) is a highly potent acid ceramidase inhibitor, used in the treatment of breast and colorectal cancer.	Nat Struct Mol Biol, 2020, 7 Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S4227	Fidaxomicin Fidaxomicin (OPT-80, PAR-101) is a narrow spectrum macrocyclic antibiotic that inhibits RNA polymerase sigma subunit.	Sci Rep, 2020, 18;10(1):8159 PLoS One, 2020, 15(2):e0228509 Antiviral Res, 2019, 170:104570
S1907	Metronidazole Metronidazole, a synthetic antibacterial and antiprotozoal agent of the nitroimidazole class, is used against protozoa.	Bone Joint Res, 2020, 16;9(4):152-161
S1760	Rifapentine Rifapentine (MDL473) is an antibiotic, which inhibits DNA-dependent RNA polymerase activity, used to treat tuberculosis.	Front Microbiol, 2020, 10:2936 mSphere, 2018, 3(5)
S1778	Trifluridine Trifluridine (NSC 529182, NSC 75520) is an anti-herpesvirus antiviral agent by interacting viral DNA replication, used primarily on the eye.	Sci Adv, 2020, 6(49)eabd9443 Ocul Surf, 2019, 10.1016/j.jtos.2019.11.011 Oncol Lett, 2018, 15(5):6107-6114
S1790	Rifaximin Rifaximin is a RNA synthesis inhibitor by binding the β subunit of the bacterial DNA-dependent RNA polymerase, used to treat traveler's diarrhea caused by certain bacteria.
S1995	Procarbazine HCl Procarbazine HCl (NSC-77213) is a hydrochloride salt form of procarbazine which is a polyfunctional alkylating compound, used for the treatment of Hodgkin's lymphoma.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z Hum Cell, 2020, 10.1007/s13577-020-00425-8
S1784	Vidarabine Vidarabine is an antiviral drug by interfering with the synthesis of viral DNA, used to treat herpes simplex and varicella zoster viruses.	Neuron, 2017, 96(6):1290-1302 ACS Appl Mater Interfaces, 2016, 8(39):25818-25824 Biogerontology, 2016, 17(5-6):907-920
S1764	Rifampin Rifampin (Rimactane, Rifampicin) is a DNA-dependent RNA polymerase inhibitor, used to treat a number of bacterial infections.	Pharmacogenomics J, 2020, 10.1038/s41397-020-0160-7 Front Microbiol, 2020, 10:2936 Pharmacotherapy, 2019, 39(1):67-76
S3001	Clevudine Clevudine is an antiviral drug for the treatment of hepatitis B.
S1300	Tegafur (FT-207) Tegafur (FT-207, NSC 148958) is a substance being used in the treatment of some types of cancer.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z Hum Cell, 2020, 10.1007/s13577-020-00425-8
S1826	Nedaplatin Nedaplatin is a derivative of cisplatin and DNA damage agent for tumor colony forming units with IC50 of 94 μM.	Nat Commun, 2019, 10(1):5654 Cancer Res, 2018, 78(19):5694-5705 Oncol Lett, 2016, 12(5):4195-4202
S7470	Triapine Triapine (3-AP) is a potent ribonucleotide reductase (RNR) inhibitor with broad spectrum antitumor activity by inhibiting DNA synthesis. Phase 2.	Nat Commun, 2020, 11(1):3214 Cancer Chemother Pharmacol, 2020, 10.1007/s00280-020-04154-5 Onco Targets Ther, 2020, 13:6523-6537	(a) Quantification of p-RPA/ Rad51, 53BP1 and γH2AX in GBM01 cells treated with DMSO or triapine. (b) Quantification of p-RPA/Rad51, 53BP1 and γH2AX in GBM02 cells treated with DMSO or triapine.
S7757	6-Thio-dG 6-thio-dG is a nucleoside analog and telomerase substrate.	Clin Sci (Lond), 2020, 10.1042/CS20190890
S4297	Mupirocin Mupirocin is an isoleucyl t-RNA synthetase inhibitor, used in the treatment of bacterial skin infections.	Anaerobe, 2020, 62:102169 Life Sci, 2019, 224:51-57 Biogerontology, 2016, 17(5-6):907-920
S8376	Rbin-1 Rbin-1 (Ribozinoindole-1) is a potent chemical inhibitor of eukaryotic ribosome assembly. It inhibits recombinant full-length Mdn1's ATPase activity in vitro.
S9521	Pentostatin Pentostatin is a potent inhibitor of adenosine deaminase. The drug is effective in the treatment of many lymphoproliferative malignancies, particularly hairy-cell leukemia. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.	Nat Metab, 2020, 10.1038/s42255-020-0227-4
S5552	Amenamevir Amenamevir (ASP2151) is a potent helicase-primase inhibitor and a novel class of antiviral agent.	J Biomol Struct Dyn, 2020, 1-14
S8095	Tubercidin Tubercidin (7-deaza-adenosine), an adenosine analogue, is a nucleoside antibiotic. It is incorporated into DNA and inhibits polymerases, thereby inhibiting DNA replication and RNA and protein synthesis. This agent also exhibits antifungal and antiviral activities.	Mol Cell, 2020, 80(6):1104-1122.e9
S4035	Vitamin D2 Vitamin D2 (Ergocalciferol) is a selective inhibitor of mammalian DNA polymerase A (pol A) with IC50 of 123 μM.	Aging (Albany NY), 2020, 12
S7975	Favipiravir (T-705) Favipiravir (T-705) is a potent and selective RNA-dependent RNA polymerase inhibitor, used to treat influenza virus infections.	mBio, 2021, 12(1)e02754-20 Viruses, 2020, 22;12(3) pii: E351 Antiviral Res, 2020, 182:104902	(A) BoDV-1 infection was measured by IFA. BoDV-1 P40 was detected with a primary monoclonal antibody (red), nuclei were stained with DAPI (blue), merged image (scale bars: 50 μm). Favipiravir: T-705
S8328	CeMMEC1 HCl CeMMEC1 is an N-methylisoquinolinone derivative that inhibits the second bromodomain of TAF1 (IC50=0.9 μM).
S5484	Rimantadine Hydrochloride Rimantadine is an RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza. It works by inhibiting a viral protein called M2, which normally mediates the transport of acid ions across the influenza virion shell.	bioRxiv, 2020, 2020.08.12.246389
S4504	6-Mercaptopurine (6-MP) Monohydrate 6-Mercaptopurine (6-MP) Monohydrate is a widely used antileukemic agent and immunosuppressive drug that inhibits de novo purine synthesis through incorporation of thiopurine methyltransferase metabolites into DNA and RNA.
S7742	SCR7 SCR7 is a specific DNA Ligase IV inhibitor, which blocks nonhomologous end-joining (NHEJ).	Proc Natl Acad Sci U S A, 2020, 22;201918845 Cell Rep, 2020, 14;31(2):107518 Cell Rep, 2020, 33(2):108240	The start codon CUG of PTEN-long was mutated to AUG and PTENlong expression is significantly increased. gRNA1 and gRNA2 have similar efficiency in driving PTEN-long expression (lanes 1 and 2). Combined gRNA1 and gRNA2 (lane 3) did not enhance PTEN-long expression compared to lane 1 and 2. The ssODN is required for mutation of CTG to ATG through HDR and without which PTEN-long is not expressed (lane 4). PTEN-long cDNA cloned into pcDNA3.1 with CTG to ATG mutation was highly expressed in transfected HEK293T cells (lane 5). Lane 6 is protein ladder. Lanes 7–10 indicate that the combination of gRNA and ssODN is required to facilitate HDR occurrence and double-strand DNA break.
S4737	Psoralen Psoralen (Psoralene, Ficusin, Furocoumarin) is a naturally occurring furocoumarin that intercalates with DNA, inhibiting DNA synthesis and cell division.
S8146	Mitomycin C Mitomycin C is an antineoplastic antibiotic by inhibiting DNA synthesis, used to treat different cancers. Mitomycin C induces apoptosis in a caspases-dependent and Fas/CD95-independent manner.	Int J Radiat Biol, 2021, 1-16 Cell, 2020, 18;S0092-8674(20)30623-1. Cell Stem Cell, 2020, S1934-5909(20)30544-0	MTT results of three HCC cell lines at 72 h after indicated treatments. Three independent experiments were carried out.
S1973	Cyclocytidine HCl Cyclocytidine (NSC 145668) is the prodrug of cytarabine, which is a pyrimidine nucleoside analog that inhibits the DNA synthesis and used mainly in the treatment of leukemia.	Acta Biochim Biophys Sin (Shanghai), 2020, 14 pii: gmaa017 J Med Virol, 2019, 91(8):1440-1447 Int J Mol Sci, 2018, 19(6)
S3641	Osalmid Osalmid suppresses ribonucleotide reductase (RR) activity in a concentration-dependent manner, with a 50% RR activity-inhibitory concentration (IC50) of 8.23 μM.
S7449	CRT0044876 CRT0044876 (NSC 69877, 7-NO2-ICA) is a potent and selective APE1 inhibitor with IC50 of ~3 μM.	Nat Biotechnol, 2017, 35(5):463-474
S7445	E3330 E3330 is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.
S5293	Nimustine Hydrochloride Nimustine Hydrochloride (Nidran) is the hydrochloride salt of nimustine, a nitrosourea with antineoplastic activity that alkylates and crosslinks DNA, thereby causing DNA fragmentation, inhibition of protein synthesis, and cell death.
S5297	Vidarabine monohydrate Vidarabine (Spongoadenosine, Vira-A) is a nucleoside antibiotic with antiviral acitivity that interferes with the synthesis of viral DNA. It is used to treat herpes simplex and varicella zoster viruses.
S2794	Sofosbuvir (GS-7977) Sofosbuvir (PSI-7977, GS-7977) is a HCV NS5B polymerase inhibitor for the treatment of chronic hepatitis C virus (HCV) infection.	Cells, 2020, 17;9(4) pii: E1003 Antiviral Res, 2020, 185:104974 Sci Rep, 2020, 18;10(1):8159	Representative confocal microscope image showing phosphorylated Drp1 translocation to mitochondria and mitochondrial fission in the presence of Sofosbuvir. At 24 hours after treatment with Sofosbuvir (100 nM), Huh7 cells were immunostained with antibodies against TOM20 (red) and p-Drp1 (S616) (green). Nuclei are demarcated with white dotted circles. Treated (+) and untreated (–) cells are marked. In the zoomed images, the arrows indicate the colocalization of TOM20 and p-Drp1 (S616) in Sofosbuvir-treated cells (yellow spots).
S6115	Pyridoxal 5′-phosphate hydrate Pyridoxal 5′-phosphate (pyridoxal phosphate, Vitamin B6 phosphate, PAL-P, PLP), a vitamin B6 phosphate, is a coenzyme in a variety of enzymatic reactions.
S8434	B02 B02 is a small-molecule inhibitor of human RAD51 with an IC50 of 27.4 μM, but does not inhibit its E. coli homologue RecA (IC50 > 250 μM).	G3 (Bethesda), 2020, 4;10(5):1585-1597 Nat Commun, 2019, 10(1):1412 Neurooncol Adv, 2019,	HEK 293T cells were transfected with a total of 6 μg of plasmid DNA (2 μg pSG-I-SceI-HA, 2 μg pcDNA-HBZ-Myc-His or empty vector, and 2 μg the pDR-GFP reporter) and treated with 20 μM B02 for 48 h where indicated. Data shown are averages of results from three independent experiments, and error bars represent SEM (*, P ≤ 0.05 by Student's t test).
S8539	TAS-102 TAS-102 is an orally administered combination of a thymidine-based nucleic acid analogue, trifluridine, and a thymidine phosphorylase inhibitor, tipiracil hydrochloride.
S7637	DTP3 DTP3 is a selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor and is able to restore MKK7/JNK activation. DTP3 inhibits cancer-selective NF-κB survival pathway.
S8144	Halofuginone Halofuginone is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in mammal.	Sci Rep, 2020, 10(1):19723 Oncol Lett, 2020, 20(6):385 Res Sq, 2020, rs.3.rs-48659
S3669	Carmustine Carmustine (bis-chloroethylnitrosourea, BCNU, BiCNU) is a cell-cycle phase nonspecific alkylating antineoplastic agent and used in the treatment of brain tumors and various other malignant neoplasms.
S7679	YK-4-279 YK-4-279 is a potent inhibitor of EWS-FLI1 binding to RNA helicase A (RHA).	Clin Cancer Res, 2020, 21;clincanres35732019 Cancers (Basel), 2020, 12(11)E3205 Cancer Cell, 2019, 36(2):179-193	YK-4-279-induced cell apoptosis of NB cells by Western blot assay. SH-SY5Y cells were treated with YK-4-279 (0, 0.1 μM, 0.3 μM, 1 μM, 3 μM) for 24 h. Whole cell lysates were subjected to SDS-PAGE and immunoblotted with antibodies against PARP and Caspase 3 to detect apoptosis. β-actin was detected as loading control. YK-4-279-induced apoptosis of NB cell line SH-SY5Y by FACS. Cells were treated with YK-4-279 (0, 1 μM, 3 μM) for 24 h, and then stained by PI and analyzed by FACS.
S4236	Proflavine Hemisulfate Proflavine Hemisulfate is a topical antiseptic by interchelating DNA, thereby disrupting DNA synthesis and leading to high levels of mutation in the copied DNA strands.
S7718	BMH-21 BMH-21 is a DNA intercalator, which binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription.	Front Genet, 2020, 11:43 Biochem Biophys Res Commun, 2019, 10.1016/j.bbrc.2019.06.057 Cancer Invest, 2019, 37(6):242-252	Pharmacological and siRNA perturbations in HEK293 cells suggest that mTORC1 also modulates cytoplasmic rheology through ribosome crowding in mammals.
S4239	Bergapten Bergapten is a psoralen that can be photoactivated and is capable of crossing-linking DNA, covalently modifying proteins and lipids, and consequently inhibiting cell replication.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z Hum Cell, 2020, 10.1007/s13577-020-00425-8
S4782	5-methoxyflavone 5-methoxyflavone is a novel DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity.
S4537	Oxolinic acid Oxolinic acid (Urinox, NSC 110364) is a quinolone antibiotic, inhibiting the enzyme DNA gyrase and DNA synthesis.It also acts as a dopamine reuptake inhibitor.
S7546	Pritelivir (BAY 57-1293) Pritelivir (BAY 57-1293, AIC316) is a potent helicase primase inhibitor, exhibiting antiviral effect on herpes simplex virus (HSV) with IC50 of 20 nM for both HSV-1 and HSV-2.
S8329	CeMMEC13 CeMMEC13 is an isoquinolinone that selectively inhibits the second bromodomain of TAF1 (IC50 = 2.1 µM).
S5582	Cytarabine hydrochloride Cytarabine is a pyrimidine nucleoside analog that is used mainly in the treatment of leukemia. It is an antimetabolite antineoplastic agent that inhibits the synthesis of DNA.	Cell Death Dis, 2021, 12(1):9 Cytometry A, 2021, 10.1002/cyto.a.24308 Am J Cancer Res, 2020, 10(10):3302-3315
S7419	Blasticidin S HCl Blasticidin S HCl is a nucleoside antibiotic isolated from Stretomyces girseochromogenes, and acts as a DNA and protein synthesis inhibitor, used to select transfected cells carrying bsr or BSD resistance genes.	Theranostics, 2021, 11(6):2966-2986 Nat Commun, 2020, 11(1):5842 Cells, 2020, 9(1)
S4288	Chloroambucil Chloroambucil (Chlorambucil) is a nitrogen mustard alkylating agent, used in the treatment of chronic lymphocytic leukemia.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S8246	RK-33 RK-33 is a first-in-class small molecule inhibitor of DDX3 (a RNA helicase) and causes G1 cell cycle arrest, induces apoptosis, and promotes radiation sensitization in DDX3-overexpressing cells.	Mol Cell, 2020, 80(6):1104-1122.e9 Proc Natl Acad Sci U S A, 2020, 117(45):28092-28101 J Virol, 2020, 6;94(2):e01679-19

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S3168^新	cis-Resveratrol cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively.
S6893^新	PIN1 inhibitor API-1 PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor with IC50 of 72.3 nM. PIN1 inhibitor API-1 targets Pin1 peptidyl-prolyl isomerase domain and inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 up-regulates miRNA biogenesis by retaining active XPO5 conformation and suppresses HCC development.
S2427^新	Triglycidyl Isocyanurate (Teroxirone) Triglycidyl Isocyanurate (Teroxirone, Tris(2,3-epoxypropyl) Isocyanurate, TGI, TGIC) is a triazene triepoxide with antineoplastic activity. It inhibits growth of human non-small cell lung cancer cells by activating p53. Triglycidyl Isocyanurate alkylates and cross-links DNA, thereby inhibiting DNA replication. Triglycidyl Isocyanurate is also used in various polyester powder coatings in the metal finishing industry.
S8326	Saccharin 1-methylimidazole (SMI) Saccharin 1-methylimidazole (SMI) is considered a general-purpose activator for DNA and RNA synthesis.

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S1334	Flupirtine maleate Flupirtine maleate is the salt form of Flupirtine, which is a centrally acting non-opioid analgesia, is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties.	Assay Drug Dev Technol, 2019, 17(7):310-321

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S1334

Flupirtine maleate

Flupirtine maleate is the salt form of Flupirtine, which is a centrally acting non-opioid analgesia, is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties.

Assay Drug Dev Technol, 2019, 17(7):310-321

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S9603^新	Lurbinectedin Lurbinectedin (PM01183, PM-1183, LY-01017, Tryptamicidin, Zepsyre, ZEPZELCA), a DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity. Lurbinectedin inhibits RMG1 and RMG2 cell growth with IC50 of 1.25 nM and 1.16 nM, respectively.

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S9603^新

Lurbinectedin

Lurbinectedin (PM01183, PM-1183, LY-01017, Tryptamicidin, Zepsyre, ZEPZELCA), a DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity. Lurbinectedin inhibits RMG1 and RMG2 cell growth with IC50 of 1.25 nM and 1.16 nM, respectively.

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S1214	Bleomycin Sulfate Bleomycin Sulfate (NSC125066) is a glycopeptide antibiotic and an anticancer agent for squamous cell carcinomas (SCC) with IC50 of 4 nM in UT-SCC-19A cells.	Sci Transl Med, 2020, 12(530) Mol Cell, 2020, 22 pii: S1097-2765(20)30231-8 Nat Commun, 2020, 29;11(1):2086
S6854^新	Triazavirin Triazavirin (TZV, Riamilovir) is a novel antiviral drug, a nucleoside analogue of nucleic acid that inhibits the synthesis of viral RNA and DNA and replication of genomic fragments. Triazavirin is active against influenza and a number of other viruses. Triazavirin is an effective protective agent on the transmission stage of influenza.
S1237	Temozolomide Temozolomide (CCRG81045, NSC 362856, TMZ) is a monofunctional SN-1 alkylating agent that can modify nitrogen atoms in the DNA ring and the extracyclic oxygen group, chemically converted to MTIC and degrades to methyldiazonium cation, which transfers methyl groups to DNA at physiologic pH. A DNA damage inducer in L-1210 and L-1210/BCNU cells. Temozolomide induces apoptosis and exhibits antitumor activity.	Theranostics, 2021, 11(4):1991-2005 Hum Mol Genet, 2021, ddab009 Exp Ther Med, 2021, 21(2):175	C57BL/6 mice were implanted in the striatum with citrine-GL26-Cherry-HMGB1, which were stably transfected to express the YFP citrine and HMGB1 fused to red fluorescent protein cherry. Fourteen days later, they were treated with saline, Ad-TK+Ad-Flt3L, or Ad-TK+Ad-Flt3L+TMZ (temozolomide). Five days after treatment, the cellular location of cherry-HMGB1 in these cells was assessed by confocal microscopy. Arrows, tumor cells (green) with cytoplasmic HMGB1 (red).
S1212	Bendamustine HCl Bendamustine (SDX-105, Cytostasane) HCl is a DNA-damaging agent with IC50 of 50 μM in cell-free assay.	Oncoimmunology, 2020, 30;9(1):1758011 Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z	Fractional Analysis of Combination Therapy of SGI-1776 With Bendamustine in B-Cell Lymphoma.
S1840	Lomustine Lomustine (nsc79037, Gleostine, CeeNU, CCNU) inhibits cancer cells by damaging the DNA and stops cells from dividing.	Nature, 2020, 580(7804):517-523. Cancer Cell Int, 2020, 19;20:58 Vet Comp Oncol, 2020, 10.1111/vco.12656	Initial range finding concentration response analysis of the cytotoxic effects of (A) lomustine (IC50 = 12 μM) and (B) vincristine (IC50 = 1.5 nM) on D283 Med in a clonogenic assay of cell survival
S7918	Bromodeoxyuridine (BrdU) Bromodeoxyuridine (BrdU) is a nucleoside analog that competes with thymidine for incorporation into DNA, and used in the detection of proliferating cells.	Cell Prolif, 2020, 28;e12818 Biomed Pharmacother, 2019, 109:1951-1959 Biomedicine & Pharmacotherapy, 2018, 10.1016/j.biopha.2018.11.029	Immunofluorescence microphotographs of proliferating ARPE-19 cell with BrdU (red) and DAPI (blue) staining after ARPE-19 cells were untreated or treated with AF (1.0 μM) in the absence or presence of EGF (100ng/ml) for 24 hours and then subjected to BrdU labeling for 4 hours, followed by immunostaining with anti-BrdU antibody and DAPI. Scale bar = 20μm.
S4888	Guanine Guanine is one of the four main nucleobases found in the nucleic acids DNA and RNA.
S5505	2’-deoxyuridine 2'-deoxyuridine (dU, 2'-dU) is frequently halogenated to create thymidine analogues useful for studies of DNA synthesis and degradation mechanisms.
S6359	Purine Purine is a heterocyclic aromatic organic compound which plays crucial roles in DNA and RNA. It is also significant components in a number of other important biomolecules, such as ATP, GTP, cyclic AMP, NADH, and coenzyme A.
S4194	Azaguanine-8 Azaguanine-8 (NSC-749, SF-337, SK 1150) is a purine analogs showing antineoplastic activity by competing with guanine in the metabolism.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z Hum Cell, 2020, 10.1007/s13577-020-00425-8
S4803	Thymidine Thymidine (Deoxythymidine, 2'-Deoxythymidine, 5-Methyldeoxyuridine) is a pyrimidine nucleoside that is composed of the pyrimidine base thymine attached to the sugar deoxyribose. As a constituent of DNA, thymidine pairs with adenine in the DNA double helix.
S1981	Adenine Adenine is a purine derivative and a nucleobase with a variety of roles in biochemistry.	PLoS Pathog, 2020, 16;16(3):e1008341
S1983	Adenine HCl Adenine HCl is a hydrochloride salt form of adenine which is a purine derivative and a nucleobase with a variety of roles in biochemistry.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z Hum Cell, 2020, 10.1007/s13577-020-00425-8
S1982	Adenine sulfate Adenine sulfate is a sulfate salt form of adenine which is a purine derivative and a nucleobase with a variety of roles in biochemistry.
S6077	Cytidine 5′-triphosphate (disodium salt) Cytidine 5'-triphosphate is a pyrimidine nucleoside triphosphate that is involved in a variety of biochemical reactions. It is used in the synthesis of RNA by RNA polymerases.
S5374	5'-Cytidylic acid 5'-Cytidylic acid (Cytidine monophosphate, Cytidine 5'-phosphate) is a nucleotide that is used as a monomer in RNA.
S5384	UTP Trisodium Salt Uridine-5'-triphosphate (UTP) is a pyrimidine nucleoside triphosphate and a substrate for the synthesis of RNA during transcription.
S3190	N6-methyladenosine (m6A) N6-methyladenosine (m6A, NSC-29409) is a base modified analog of adenosine and is found as a minor nucleoside in natural RNAs.	Nat Genet, 2020, 10.1038/s41588-020-0677-3 Nat Cell Biol, 2019, 21(5):651-661 Nat Commun, 2019, 10(1):5126	(A) Comparison of ribose modification across the RNA species. Modified nucleosides of MRC-5 cells were aligned in terms of modification type and then RNA species. Data are presented as means ± STD, n = 3. (B) tRNA modification profiles of cancer tissues. Data are presented as means ± STD, n = 5.
S2029	Uridine Uridine (NSC 20256) is a nucleoside, contains a uracil attached to a ribose ring via a β-N1-glycosidic bond.
S9382	Thymine Thymine (5-methyluracil) is one of the four nucleobases in the nucleic acid of DNA.

研究分野別

製品類型

DNA/RNA合成

シグナル伝達経路

研究分野

阻害剤の選択性比較

DNA/RNA Synthesis製品