トポイソメラーゼ

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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
S1208	Doxorubicin (Adriamycin) HCl	20 mg/mL	100 mg/mL	''''''<1 mg/mL
S1225	Etoposide (VP-16)	<1 mg/mL	100 mg/mL	''<1 mg/mL
S1288	Camptothecin (NSC-100880)	<1 mg/mL	3 mg/mL	'''<1 mg/mL
S1231	Topotecan (NSC609699) HCl	91 mg/mL	91 mg/mL	'<1 mg/mL
S1198	Irinotecan (CPT-11)	<1 mg/mL	7 mg/mL	''<1 mg/mL
E2516	Doxorubicin	50 mg/mL	100 mg/mL	<1 mg/mL
E0459	Robinetin	<1 mg/mL	60 mg/mL	3 mg/mL
S1228	Idarubicin HCl	5 mg/mL	100 mg/mL	<1 mg/mL
S1223	Epirubicin (IMI 28) HCl	100 mg/mL	100 mg/mL	'<1 mg/mL
S2485	Mitoxantrone (NSC-301739) 2HCl	89 mg/mL	89 mg/mL	'<1 mg/mL
S3035	Daunorubicin (RP 13057) HCl	100 mg/mL	100 mg/mL	''<1 mg/mL
S1465	Moxifloxacin (BAY12-8039) HCl	60 mg/mL	87 mg/mL	''<1 mg/mL
S2217	Irinotecan (CPT-11) HCl Trihydrate	1 mg/mL	100 mg/mL	'7 mg/mL
S4908	SN-38	<1 mg/mL	21 mg/mL	'<1 mg/mL
S1367	Amonafide	<1 mg/mL	57 mg/mL	4 mg/mL
S1787	Teniposide	<1 mg/mL	40 mg/mL	<1 mg/mL
S1340	Gatifloxacin	<1 mg/mL	7 mg/mL	<1 mg/mL
S1222	Dexrazoxane HCl (ICRF-187)	60 mg/mL	60 mg/mL	<1 mg/mL
S1342	Genistein (NPI 031L)	<1 mg/mL	54 mg/mL	''2 mg/mL
S1940	Levofloxacin	11 mg/mL	24 mg/mL	9 mg/mL
S1393	Pirarubicin (NSC-333054)	<1 mg/mL	7 mg/mL	'<1 mg/mL
S1464	Marbofloxacin	<1 mg/mL	3 mg/mL	<1 mg/mL
S2027	Ciprofloxacin	<1 mg/mL	<1 mg/mL	<1 mg/mL
S2492	Novobiocin Sodium (NSC 2382)	100 mg/mL	100 mg/mL	''100 mg/mL
S1756	Enoxacin	<1 mg/mL	32 mg/mL	<1 mg/mL
S1463	Ofloxacin	<1 mg/mL	0.4 mg/mL	<1 mg/mL
S1509	Norfloxacin	<1 mg/mL	3 mg/mL	<1 mg/mL
S1327	Ellagic acid	<1 mg/mL	3 mg/mL	<1 mg/mL
S2328	Nalidixic acid	<1 mg/mL	6 mg/mL	<1 mg/mL
S7261	Beta-Lapachone	<1 mg/mL	33 mg/mL	'10 mg/mL
S4006	Clinafloxacin	<1 mg/mL	0.03 mg/mL	<1 mg/mL
S6747	SW-044248	<1 mg/mL	14 mg/mL	<1 mg/mL
S5008	Ciprofloxacin hydrochloride	74 mg/mL	7 mg/mL	'<1 mg/mL
S4119	Pefloxacin Mesylate Dihydrate	67 mg/mL	9 mg/mL	<1 mg/mL
S5964	Gatifloxacin hydrochloride	20 mg/mL	4 mg/mL	'<1 mg/mL
S2064	Balofloxacin	<1 mg/mL	5 mg/mL	<1 mg/mL
S5026	Irinotecan hydrochloride	<1 mg/mL	100 mg/mL	'''<1 mg/mL
S2271	Berberine chloride (NSC 646666)	<1 mg/mL	40 mg/mL	<1 mg/mL
S4604	Levofloxacin hydrate	5 mg/mL	74 mg/mL	10 mg/mL
S0093	Genz-644282	<1 mg/mL	<1 mg/mL	<1 mg/mL
S2423	(S)-10-Hydroxycamptothecin	<1 mg/mL	8 mg/mL	<1 mg/mL
S6790	Ellipticine hydrochloride	˂1 mg/mL	3 mg/mL	˂1 mg/mL
S9321	Topotecan	-1 mg/mL	84 mg/mL	-1 mg/mL
S7518	Voreloxin (SNS-595) hydrochloride	1 mg/mL	1 mg/mL	'<1 mg/mL
S5059	Pixantrone Maleate	100 mg/mL	100 mg/mL	1 mg/mL
S3603	Betulinic acid	<1 mg/mL	20 mg/mL	10 mg/mL
S5111	7-Ethylcamptothecin	-1 mg/mL	20 mg/mL	-1 mg/mL
S2653	9-amino-CPT (9-Aminocamptothecin)	<1 mg/mL	25 mg/mL	<1 mg/mL
S3898	Hydroxy Camptothecine	-1 mg/mL	29 mg/mL	'-1 mg/mL
S2288	Rubitecan	<1 mg/mL	58 mg/mL	<1 mg/mL
S6631	Belotecan (CKD-602) hydrochloride	4 mg/mL	47 mg/mL	<1 mg/mL
S3181	Flumequine	<1 mg/mL	3 mg/mL	<1 mg/mL
S9634	Phenoxodiol (Haginin E)	<1 mg/mL	48 mg/mL	48 mg/mL

亜型選択性的な製品

Topoisomerase製品

All (56) Topoisomerase阻害剤(55) Topoisomerase活性剤(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
S1208	Doxorubicin (Adriamycin) HCl Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage, mitophagy and apoptosis in tumor cells. Doxorubicin reduces basal phosphorylation of AMPK. Doxorubicin is used in the concomitant treatment of HIV-infected patients but is found to be at high risk of HBV reactivation.	Adv Sci (Weinh), 2022, e2103332 Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 Bioact Mater, 2022, 18:459-470	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.
S1225	Etoposide (VP-16) Etoposide (VP-16, VP-16213) is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity. Etoposide induces autophagy, mitophagy and apoptosis.	Mol Cell, 2022, S1097-2765(22)00085-5 Nat Commun, 2022, 13(1):1714 Dev Cell, 2022, 57(5):638-653.e5	Cellular biomarker responses in HT29 cells exposed to various cytotoxic chemotherapeutic agents in combination with the Chk1 inhibitor V158411. HT29 cells were exposed to the combination GI80 of gemcitabine (0.2 uM), camptothecin (0.44 uM), cisplatin (68 uM), oxaliplatin (131 uM), doxorubicin (1.2 uM) or etoposide (59 uM) for 18 hours followed by DMSO (-) or 400 nM V158411 (+) for a further 24 hours. Protein expression was characterized by immunoblotting.
S1288	Camptothecin (NSC-100880) Camptothecin (NSC-100880, CPT, Campathecin, (S)-(+)-Camptothecin) is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM in a cell-free assay. Camptothecin induces apoptosis in cancer cells via microRNA-125b-mediated mitochondrial pathways. Phase 2.	Sci Adv, 2022, 8(3):eabj8357 Cell Rep, 2022, 38(12):110536 Elife, 2022, 11e70726	Growth suppression by UBE2M silencing is enhanced by DNA damaging agents. Growth sensitivity of HEY cells in the presence of Camptothecin(CPT) was monitored using clonogenic assay.
S1231	Topotecan (NSC609699) HCl Topotecan HCl (NSC609699, Nogitecan, SKFS 104864A) is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively. Topotecan HCl induces autophagy and apoptosis.	Clin Transl Med, 2022, 12(5):e881 Int J Mol Sci, 2022, 23(10)5532 Hum Cell, 2022, 10.1007/s13577-022-00671-y	Pax3:Foxo1a knockdown increases select chemotherapy sensitivities. MTS assay was performed for Pax3:Foxo1a knockdown mouse aRMS tumor cells treated with DNA damaging agents and microtubule inhibitors. Pax3:Foxo1a knockdown reduced the concentration at which viability was impaired by 50% (IC50) of topotecan by 4.8 fold, respectively, yet did not affect the IC50 of mafosfamide.
S1198	Irinotecan (CPT-11) Irinotecan (CPT-11, (+)-Irinotecan) is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.	Cancers (Basel), 2022, 14(5)1230 Cancer Cell, 2021, 39(4):566-579.e7 J Cachexia Sarcopenia Muscle, 2021, 10.1002/jcsm.12703	In vitro cell uptake data showing the HA coating on HAC-PFP-DC nanoparticles significantly improves drug delivery into prostasphere and mammosphere cells enriched with CSCs. Fluorescence micrographs of mammosphere cells after incubated with the simple mixture of free DOX&CPT, PFP-DC nanoparticles, and HAC-PFPDC nanoparticles for 3 h at 37℃.
E2516^新	Doxorubicin Adriamycin (Doxorubicin, Hydroxydaunorubicin), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent, inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication, and induces apoptosis, also inhibits human DNA topoisomerase I with an IC50 of 0.8 μM.
S8942^新	Suramin sodium salt Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatase (PTPases) inhibitor, also is the potent inhibitor of sirtuins, purified topoisomerase II and SARS-CoV-2 RNA-dependent RNA polymerase (RdRp).
E0459^新	Robinetin Robinetin inhibits HIV integrase cleavage and integration in a dose-dependent manne, inhibits the DNA synthesis in Proteus vulgaris, and the RNA synthesis in S. aureus, also inhibits egg yolk phosphatidylcholine (EYPC) membrane lipid peroxidation and hemoglobin A (HbA) glycosylation with high efficiency.
S8999^新	Exatecan Mesylate Exatecan Mesylate (DX-8951f) is a water-soluble and non-pro-drug analog of camptothecin and shows significant topoisomerase I inhibition with IC50 of 0.975 μg/ml.
S1228	Idarubicin HCl Idarubicin HCl (4-demethoxydaunorubicin, NSC256439, 4-DMDR) is a hydrochloride salt form of Idarubicin which is an anthracycline antibiotic and a DNA topoisomerase II (topo II) inhibitor for MCF-7 cells with IC50 of 3.3 ng/mL in a cell-free assay. Idarubicin induces mTOR-dependent cytotoxic autophagy.	Hum Cell, 2022, 10.1007/s13577-022-00671-y Cancers (Basel), 2021, 13(14)3586 Biomolecules, 2021, 11(8)1128	Sensitivity of AML cells to conventional induction treatment and small-molecule p53 activators. Cell viability in OCI-AML3 cells treated for 24 hours with cytarabin/idarubicin (CI) and Nultin-3A (Nut; A), CI and Leptomycin-B (LMB; B), or Nut and LMB (D), respectively. CI was tested at 0, 100, 200, and 300 nmol/L CI; Nutlin-3A at 0, 2.5, 5, 7.5; and LMB at 0, 2, 8, 32 ng/mL in dosages 0, 1, 2, and 3, respectively. Cell viability in normal and AML bone marrow cells.
S1223	Epirubicin (IMI 28) HCl Epirubicin HCl (IMI 28, NSC 256942, 4'-epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase. Epirubicin induces apoptosis.	Mol Med, 2022, 28(1):49 Bioengineered, 2022, 13(5):12888-12898 Hum Cell, 2022, 10.1007/s13577-022-00671-y	Growth inhibitory effects of Epirubicin human pancreatic cancer cells. MiaPaCa-2 cells were plated in triplicates into 48-well plates at a density of 10,000 cells/ml. After 24 hours, complete culture medium was changed into fresh low-serum-containing medium (0.5% FBS) containing DMSO (control) or indicated doses of Epirubicin (Selleckchem). Cell viability 48 hours after treatment was determined by AlamarBlue assay (Invitrogen) according to manufacturer's instructions. Results are expressed as percentages of control, which was arbitrarily assigned 100% viability, and represented as the mean ± standard deviation (SD) of the tripicate wells.
S2485	Mitoxantrone (NSC-301739) 2HCl Mitoxantrone 2HCl (NSC-301739) is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis.	J Cell Biochem, 2022, 10.1002/jcb.30213 Hum Cell, 2022, 10.1007/s13577-022-00671-y Cancers (Basel), 2021, 13(8)1954	Immunohistochemistry and quantification of cleaved caspase 3 expression in DU145-DR tumor xenografts from (D). Scale bar, 100 mm. Data represent the mean ± SD. *p < 0.05.
S3035	Daunorubicin (RP 13057) HCl Daunorubicin HCl (Daunomycin, RP 13057, Rubidomycin) 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.	Nat Cell Biol, 2022, 10.1038/s41556-021-00814-7 Cell Rep, 2022, 39(1):110643 J Cell Biochem, 2022, 10.1002/jcb.30213	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).
S1465	Moxifloxacin (BAY12-8039) HCl Moxifloxacin (BAY12-8039) is a fourth-generation synthetic fluoroquinolone antibacterial agent.	Clin Transl Sci, 2019, 12(6):687-697 Front Microbiol, 2018, 6:336 J Pharmacol Toxicol Methods, 2017, 90:39-47
S2217	Irinotecan (CPT-11) HCl Trihydrate Irinotecan (CPT-11) prevents DNA from unwinding by inhibition of topoisomerase 1.	Stem Cell Res Ther, 2022, 13(1):219 Cancers (Basel), 2022, 14(8)1968 Cancers (Basel), 2022, 14(5)1230	Growth inhibitory effects of Irinotecan in human pancreatic cancer cells. Panc1 cells were plated in triplicates into 48-well plates at a density of 10,000 cells/ml. After 24 hours, complete culture medium was changed into fresh low-serum-containing medium (1% FBS) containing DMSO (control) or indicated doses of Irinotecan (Selleckchem). Cell viability 72 hours after treatment was determined by AlamarBlue assay (Invitrogen) according to manufacturer's instructions. Results are expressed as percentages of control, which was arbitrarily assigned 100% viability, and represented as the mean ± standard deviation (SD) of the tripicate wells.
S4908	SN-38 SN-38 (NK012) is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy.	Adv Healthc Mater, 2022, e2102816 Clin Transl Med, 2022, 12(5):e881 Biomedicines, 2022, 10(3)638	HCT116 cells were pretreated with tested compounds for 1 hour and then cotreated with 1 μM SN-38 for 2 hours. Cell lysates were then subjected to Western blot analysis. Data shown are representative of three independent experiments. Con, concentration.
S1367	Amonafide Amonafide (NSC308847, AS1413) produces protein-associated DNA-strand breaks through a topoisomerase II-mediated reaction, but does not produce topoisomerase I-mediated DNA cleavage. Phase 3.	Nat Commun, 2019, 10(1):4217 Front Oncol, 2019, 9:1406 Theranostics, 2015, 5(5):477-88
S1787	Teniposide Teniposide (NSC 122819, VM-26) is a chemotherapeutic medication mainly used in the treatment of childhood acute lymphocytic leukemia (ALL).	Hum Cell, 2022, 10.1007/s13577-022-00671-y Cancer Cell, 2021, S1535-6108(21)00659-0 Nat Commun, 2021, 12(1):6813
S1340	Gatifloxacin Gatifloxacin (AM-1155, CG5501, BMS-206584) is an antibiotic of the fourth-generation fluoroquinolone family, and inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.	Cancer Discov, 2020, CD-20-0160 Biochem Pharmacol, 2015, 95(4):227-37	Cleavable complex formation with nuclear DNA in P. falciparum treated with topoisomerase poisons. Parasites were metabolically labeled with [3H]hypoxanthine, treated with etoposide (■), gatifloxacin (●), levofloxacin(▲), ciprofloxacin (□), fleroxacin (○), or nalidixic acid (△) at the indicated concentrations for 18-22 h, lysed with SDS and digested with RNases. SDS and protein-bound DNA were precipitated with potassium. The fold increase in nuclear DNA capture as compared to solvent controls (mean of triplicate determinations) was plotted against concentration. Coefficient of variation for each data point was 19%.
S1222	Dexrazoxane HCl (ICRF-187) Dexrazoxane HCl (ICRF-187, ADR-529) is an intracellular iron chelator, which decreases the formation of superoxide radicals, used as a cardioprotective agent; also an inhibitor of topoisomerase II	PLoS Genet, 2019, 15(2):e1007925 J Virol, 2019, 93(11) EMBO Rep, 2017, 18(8):1412-1428
S1342	Genistein (NPI 031L) Genistein (NPI 031L), a phytoestrogen found in soy products, is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM or by insulin with IC50 of 19 μM.	ACS Appl Mater Interfaces, 2022, 14(21):24144-24159 Hum Cell, 2022, 10.1007/s13577-022-00671-y Adv Sci (Weinh), 2021, e2103360
S1940	Levofloxacin Levofloxacin (Fluoroquinolone) is a broad-spectrum antibiotic topoisomerase II and topoisomerase IV inhibitor, used to treat respiratory, urinary tract, gastrointestinal, and abdominal infections.	Adv Healthc Mater, 2022, e2102117 Exp Ther Med, 2021, 21(4):332 Mol Cell, 2020, 80(6):1104-1122.e9
S1393	Pirarubicin (NSC-333054) Pirarubicin (NSC-333054) is an anthracycline antibiotic, and also a DNA/RNA synthesis inhibitor by intercalating into DNA and interacts with topoisomerase II, used as an antineoplastic agent.	Cell Death Dis, 2022, 13(5):492 Int J Nanomedicine, 2021, 16:951-976 Pharmaceuticals (Basel), 2020, 14(1)E22
S1464	Marbofloxacin Marbofloxacin is a potent antibiotic inhibiting bacterial DNA replication.
S2027	Ciprofloxacin Ciprofloxacin (Bay o 9867) is a fluoroquinolone antibiotic, shows broad and potent antibacterial activity, with MIC90 of 0.024-6 μM.	Environ Mol Mutagen, 2019, 60(6):513-533	Ciprofoxacin (Cipro) reduces cancer cell survival in combination with chemotherapy. A and B, colony formation was conducted with A549 and SW48 cells treated with the clinically relevant chemotherapeutics cisplatin or 5-FU in the presence or absence of 2 μmol/L cipro ﬂoxacin. C, cipro ﬂ oxacin at 2 μmol/L decreased proliferation of KG-1 cells and slightly enhanced the effect of etoposide (Etop). , P < 0.05; *, P < 0.01 ( t tests).
S2492	Novobiocin Sodium (NSC 2382) Novobiocin Sodium (NSC 2382, Albamycin, Cathomycin) is an aminocoumarin antibiotic that targets bacterial DNA gyrase (TopoIV), used to treat susceptible gram positive bacteria.	Mol Cancer Ther, 2021, 10.1158/1535-7163.MCT-21-0215 Nat Cancer, 2021, 2(6):598-610 Mol Syst Biol, 2018, 14(3):e7858	Cell viability and caspase 3/7 activity in MDA-MB-231 cells co-treated with carbenoxolone, novobiocin, ibrutinib and bisphosphonates. Cell viability (A) and caspase 3/7 activity (B) was determined after treatment with ZA (zoledronic acid), RIS (risedronate), IBN (ibandronate), ALN (alendronate) in combination with carbenoxolone, novobiocin and ibrutinib. All data are expressed as means of three different measure points of three independent experiments ± SEM and were normalized to BP treatment alone. Significances were calculated with the Mann Whitney U test (p < 0.05; *p < 0.005).
S1756	Enoxacin Enoxacin (AT-2266, CI919, Pd107779, NSC 629661) is an oral broad-spectrum fluoroquinolone antibacterial agent by inhibiting bacterial DNA gyrase and topoisomerase IV, used to treat a wide variety of infections.	J Virol, 2020, 17;94(3) pii: e01233-19
S1463	Ofloxacin Ofloxacin (DL8280) is a synthetic broad-spectrum antimicrobial agent.
S1509	Norfloxacin Norfloxacin (MK-0366) is a broad-spectrum antibiotic. Norfloxacin (MK-0366) targets bacterial gyrase and topoisomerase IV enzymes.
S1327	Ellagic acid Ellagic acid (Elagostasine, Gallogen) has antiproliferative and antioxidant property.	Mol Cell, 2020, 80(6):1104-1122.e9 Kaohsiung J Med Sci, 2020, 6 Nutr Cancer, 2017, 69(7):1088-1098
S2328	Nalidixic acid Nalidixic acid (NSC-82174) is a synthetic 1,8-naphthyridine antimicrobial agent with a limited bacteriocidal spectrum. It is an inhibitor of the A subunit of bacterial DNA gyrase.	Hum Mol Genet, 2020, ddaa244 Int J Mol Sci, 2018, 19(6)
S7261	Beta-Lapachone Beta-Lapachone (β-Lapachone, ARQ-501) is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2.	Comput Struct Biotechnol J, 2022, 20:2442-2454 Free Radic Biol Med, 2021, 173:64-69 Front Pharmacol, 2021, 12:766909
S4006	Clinafloxacin Clinafloxacin (CI-960, PD127391, AM-1091) is a fluoroquinolone that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumoniae.
S6747	SW-044248 SW-044248 is a non-canonical Top1 inhibitor with a pattern of selective toxicity for NSCLC cells.
S5008	Ciprofloxacin hydrochloride Ciprofloxacin (CPX, Cetraxal, Ciloxan, Cipro, Bay-09867) hydrochloride, a fluorinated quinolone, is a β-diketone antibiotic with a broad spectrum antibacterial activity. Ciprofloxacin is an inhibitor of bacterial DNA gyrase (a subclass of Type II topoisomerases).
S4119	Pefloxacin Mesylate Dihydrate Pefloxacin Mesylate Dihydrate (1589 RB) is the third generation of fluoroquinolone class of antibacterials, which inhibits Topoisomerase II activity and DNA replication.
S5627	Amsacrine hydrochloride Amsacrine hydrochloride (m-AMSA, acridinyl anisidide) is the hydrochloride salt form of amsacrine, which is an inhibitor of topoisomerase II with antineoplastic activity.
S5964	Gatifloxacin hydrochloride Gatifloxacin (AM-1155, CG5501, BMS-206584, PD135432) hydrochloride is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases with IC50 of 13.8 μg/ml and 0.109 μg/ml for S. aureus topoisomerase IV and E. coli DNA gyrase, respectively.
S2064	Balofloxacin Balofloxacin (Q-35) is a quinolone antibiotic, inhibiting the synthesis of bacterial DNA by interference with the enqyme DNA gyrase.
S5026	Irinotecan hydrochloride Irinotecan (CPT-11, (+)-Irinotecan) hydrochloride is an inhibitor of Topoisomerase I (Topo I) that exhibits cytotoxicity in LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.	Cancers (Basel), 2022, 14(5)1230 Biomedicines, 2022, 10(2)438 Biomaterials, 2021, 280:121276
S2271	Berberine chloride (NSC 646666) Berberine chloride (NSC 646666, Natural Yellow 18) is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	J Biomol Struct Dyn, 2022, 1-11 Front Pharmacol, 2021, 12:632201 Molecules, 2021, 26(5)1210
S4604	Levofloxacin hydrate Levofloxacin (Levaquin, Tavanic, Quixin, Iquix, Cravit) is a broad-spectrum, third-generation fluoroquinolone antibiotic and optically active L-isomer of ofloxacin with antibacterial activity. It acts by inhibiting DNA gyrase (bacterial topoisomerase II).	Adv Healthc Mater, 2022, e2102117 Exp Ther Med, 2021, 21(4):332 Front Microbiol, 2020, 10:2936
S0093	Genz-644282 Genz-644282 is a non-camptothecin topoisomerase I (Topo I) inhibitor that demonstrates potent cytotoxic activity with a median IC50 of 1.2 nM (range 0.2 nM-21.9 nM). Genz-644282 can be used in cancer research.
S2423	(S)-10-Hydroxycamptothecin (S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor with potent anti-tumor activity.	Nat Commun, 2022, 13(1):2861 ACS Appl Mater Interfaces, 2021, 13(47):56519-56529 Carcinogenesis, 2021, bgab002
S6790	Ellipticine hydrochloride Ellipticine Hydrochloride (NSC 71795, PZE) is a potent inhibitor of DNA topoisomerase II and forms covalent DNA adducts mediated by its oxidation with cytochromes P450 (CYP) and peroxidases. Ellipticine Hydrochloride is a natural product isolated from the Australian evergreen tree of the Apocynaceae family with antineoplastic activity.
S9321	Topotecan Topotecan is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.	Clin Transl Med, 2022, 12(5):e881 Int J Mol Sci, 2022, 23(10)5532 Nat Commun, 2021, 12(1):5404
S7518	Voreloxin (SNS-595) hydrochloride Voreloxin hydrochloride (SNS-595, Vosaroxin) is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2.	Adv Sci (Weinh), 2020, 7(21):2001018 Apoptosis, 2019, 24(11-12):849-861 Target Oncol, 2019, 14(3):351-364
S5059	Pixantrone Maleate Pixantrone (BBR-2778) is a novel aza-anthracenedione compound with antitumor activity. It is a weak topoisomerase II inhibitor and forms stable DNA adducts through alkylation with specificity for DNA hypermethylated sites.
S3603	Betulinic acid Betulinic acid (ALS-357, Lupatic acid, Betulic acid), a pentacyclic triterpenoid from Syzigium claviflorum, is a inhibitor of HIV-1 with EC50 of 1.4 μ M. Betulinic acid acts as a new activator of NF-kB. Phase 1/2.	Mol Ther Nucleic Acids, 2022, 28:435-449 Oxid Med Cell Longev, 2021, 2021:5519587 J Cardiovasc Pharmacol, 2021, 78(2):235-246
S5111	7-Ethylcamptothecin 7-Ethyl Camptothecin is an anti-cancer chemical that exhibits a strong activity against various murine tumors through Topo I (topoisomerase) inhibition.
S2653	9-amino-CPT (9-Aminocamptothecin) 9-amino-CPT (9-Aminocamptothecin, 9-AC, Aminocamptothecin, 9-amino-20(S)-camptothecin) is a Topoisomerase I inhibitor with potent anticancer activities. 9-amino-CPT (9-Aminocamptothecin) is an active, water-insoluble derivative of camptothecin.
S3898	Hydroxy Camptothecine Hydroxy Camptothecine (10-Hydroxycamptothecin, Hydroxycamptothecine) is a cell-permeable powerful DNA topoisomerase I inhibitor. It has selective inhibitory effect on the phosphorylation of histone H1 and H3, but less effect on other histones.	Life Sci, 2020, 246:117428
S2288	Rubitecan Rubitecan (9-NC, 9-Nitro-camptothecin, Partaject Orathecin, Partaject rubitecan, RFS 2000) is a topoisomerase I inhibitor extracted from the bark and leaves of the Camptotheca acuminata tree, which is native to China. Rubitecan is an oral camptothecin with antitumour activity.
S6631	Belotecan (CKD-602) hydrochloride Belotecan (CKD-602) is a potent DNA topoisomerase I inhibitor that exerts a clinical anticancer effect on various types of tumor.
S3181	Flumequine Flumequine is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM.
S9634	Phenoxodiol (Haginin E) Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II.	Anticancer Res, 2018, 38(10):5709-5716

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
S1208	Doxorubicin (Adriamycin) HCl Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage, mitophagy and apoptosis in tumor cells. Doxorubicin reduces basal phosphorylation of AMPK. Doxorubicin is used in the concomitant treatment of HIV-infected patients but is found to be at high risk of HBV reactivation.	Adv Sci (Weinh), 2022, e2103332 Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 Bioact Mater, 2022, 18:459-470	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.
S1225	Etoposide (VP-16) Etoposide (VP-16, VP-16213) is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity. Etoposide induces autophagy, mitophagy and apoptosis.	Mol Cell, 2022, S1097-2765(22)00085-5 Nat Commun, 2022, 13(1):1714 Dev Cell, 2022, 57(5):638-653.e5	Cellular biomarker responses in HT29 cells exposed to various cytotoxic chemotherapeutic agents in combination with the Chk1 inhibitor V158411. HT29 cells were exposed to the combination GI80 of gemcitabine (0.2 uM), camptothecin (0.44 uM), cisplatin (68 uM), oxaliplatin (131 uM), doxorubicin (1.2 uM) or etoposide (59 uM) for 18 hours followed by DMSO (-) or 400 nM V158411 (+) for a further 24 hours. Protein expression was characterized by immunoblotting.
S1288	Camptothecin (NSC-100880) Camptothecin (NSC-100880, CPT, Campathecin, (S)-(+)-Camptothecin) is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM in a cell-free assay. Camptothecin induces apoptosis in cancer cells via microRNA-125b-mediated mitochondrial pathways. Phase 2.	Sci Adv, 2022, 8(3):eabj8357 Cell Rep, 2022, 38(12):110536 Elife, 2022, 11e70726	Growth suppression by UBE2M silencing is enhanced by DNA damaging agents. Growth sensitivity of HEY cells in the presence of Camptothecin(CPT) was monitored using clonogenic assay.
S1231	Topotecan (NSC609699) HCl Topotecan HCl (NSC609699, Nogitecan, SKFS 104864A) is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively. Topotecan HCl induces autophagy and apoptosis.	Clin Transl Med, 2022, 12(5):e881 Int J Mol Sci, 2022, 23(10)5532 Hum Cell, 2022, 10.1007/s13577-022-00671-y	Pax3:Foxo1a knockdown increases select chemotherapy sensitivities. MTS assay was performed for Pax3:Foxo1a knockdown mouse aRMS tumor cells treated with DNA damaging agents and microtubule inhibitors. Pax3:Foxo1a knockdown reduced the concentration at which viability was impaired by 50% (IC50) of topotecan by 4.8 fold, respectively, yet did not affect the IC50 of mafosfamide.
S1198	Irinotecan (CPT-11) Irinotecan (CPT-11, (+)-Irinotecan) is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.	Cancers (Basel), 2022, 14(5)1230 Cancer Cell, 2021, 39(4):566-579.e7 J Cachexia Sarcopenia Muscle, 2021, 10.1002/jcsm.12703	In vitro cell uptake data showing the HA coating on HAC-PFP-DC nanoparticles significantly improves drug delivery into prostasphere and mammosphere cells enriched with CSCs. Fluorescence micrographs of mammosphere cells after incubated with the simple mixture of free DOX&CPT, PFP-DC nanoparticles, and HAC-PFPDC nanoparticles for 3 h at 37℃.
E2516^新	Doxorubicin Adriamycin (Doxorubicin, Hydroxydaunorubicin), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent, inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication, and induces apoptosis, also inhibits human DNA topoisomerase I with an IC50 of 0.8 μM.
S8942^新	Suramin sodium salt Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatase (PTPases) inhibitor, also is the potent inhibitor of sirtuins, purified topoisomerase II and SARS-CoV-2 RNA-dependent RNA polymerase (RdRp).
E0459^新	Robinetin Robinetin inhibits HIV integrase cleavage and integration in a dose-dependent manne, inhibits the DNA synthesis in Proteus vulgaris, and the RNA synthesis in S. aureus, also inhibits egg yolk phosphatidylcholine (EYPC) membrane lipid peroxidation and hemoglobin A (HbA) glycosylation with high efficiency.
S8999^新	Exatecan Mesylate Exatecan Mesylate (DX-8951f) is a water-soluble and non-pro-drug analog of camptothecin and shows significant topoisomerase I inhibition with IC50 of 0.975 μg/ml.
S1228	Idarubicin HCl Idarubicin HCl (4-demethoxydaunorubicin, NSC256439, 4-DMDR) is a hydrochloride salt form of Idarubicin which is an anthracycline antibiotic and a DNA topoisomerase II (topo II) inhibitor for MCF-7 cells with IC50 of 3.3 ng/mL in a cell-free assay. Idarubicin induces mTOR-dependent cytotoxic autophagy.	Hum Cell, 2022, 10.1007/s13577-022-00671-y Cancers (Basel), 2021, 13(14)3586 Biomolecules, 2021, 11(8)1128	Sensitivity of AML cells to conventional induction treatment and small-molecule p53 activators. Cell viability in OCI-AML3 cells treated for 24 hours with cytarabin/idarubicin (CI) and Nultin-3A (Nut; A), CI and Leptomycin-B (LMB; B), or Nut and LMB (D), respectively. CI was tested at 0, 100, 200, and 300 nmol/L CI; Nutlin-3A at 0, 2.5, 5, 7.5; and LMB at 0, 2, 8, 32 ng/mL in dosages 0, 1, 2, and 3, respectively. Cell viability in normal and AML bone marrow cells.
S1223	Epirubicin (IMI 28) HCl Epirubicin HCl (IMI 28, NSC 256942, 4'-epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase. Epirubicin induces apoptosis.	Mol Med, 2022, 28(1):49 Bioengineered, 2022, 13(5):12888-12898 Hum Cell, 2022, 10.1007/s13577-022-00671-y	Growth inhibitory effects of Epirubicin human pancreatic cancer cells. MiaPaCa-2 cells were plated in triplicates into 48-well plates at a density of 10,000 cells/ml. After 24 hours, complete culture medium was changed into fresh low-serum-containing medium (0.5% FBS) containing DMSO (control) or indicated doses of Epirubicin (Selleckchem). Cell viability 48 hours after treatment was determined by AlamarBlue assay (Invitrogen) according to manufacturer's instructions. Results are expressed as percentages of control, which was arbitrarily assigned 100% viability, and represented as the mean ± standard deviation (SD) of the tripicate wells.
S2485	Mitoxantrone (NSC-301739) 2HCl Mitoxantrone 2HCl (NSC-301739) is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis.	J Cell Biochem, 2022, 10.1002/jcb.30213 Hum Cell, 2022, 10.1007/s13577-022-00671-y Cancers (Basel), 2021, 13(8)1954	Immunohistochemistry and quantification of cleaved caspase 3 expression in DU145-DR tumor xenografts from (D). Scale bar, 100 mm. Data represent the mean ± SD. *p < 0.05.
S3035	Daunorubicin (RP 13057) HCl Daunorubicin HCl (Daunomycin, RP 13057, Rubidomycin) 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.	Nat Cell Biol, 2022, 10.1038/s41556-021-00814-7 Cell Rep, 2022, 39(1):110643 J Cell Biochem, 2022, 10.1002/jcb.30213	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).
S1465	Moxifloxacin (BAY12-8039) HCl Moxifloxacin (BAY12-8039) is a fourth-generation synthetic fluoroquinolone antibacterial agent.	Clin Transl Sci, 2019, 12(6):687-697 Front Microbiol, 2018, 6:336 J Pharmacol Toxicol Methods, 2017, 90:39-47
S2217	Irinotecan (CPT-11) HCl Trihydrate Irinotecan (CPT-11) prevents DNA from unwinding by inhibition of topoisomerase 1.	Stem Cell Res Ther, 2022, 13(1):219 Cancers (Basel), 2022, 14(8)1968 Cancers (Basel), 2022, 14(5)1230	Growth inhibitory effects of Irinotecan in human pancreatic cancer cells. Panc1 cells were plated in triplicates into 48-well plates at a density of 10,000 cells/ml. After 24 hours, complete culture medium was changed into fresh low-serum-containing medium (1% FBS) containing DMSO (control) or indicated doses of Irinotecan (Selleckchem). Cell viability 72 hours after treatment was determined by AlamarBlue assay (Invitrogen) according to manufacturer's instructions. Results are expressed as percentages of control, which was arbitrarily assigned 100% viability, and represented as the mean ± standard deviation (SD) of the tripicate wells.
S4908	SN-38 SN-38 (NK012) is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy.	Adv Healthc Mater, 2022, e2102816 Clin Transl Med, 2022, 12(5):e881 Biomedicines, 2022, 10(3)638	HCT116 cells were pretreated with tested compounds for 1 hour and then cotreated with 1 μM SN-38 for 2 hours. Cell lysates were then subjected to Western blot analysis. Data shown are representative of three independent experiments. Con, concentration.
S1367	Amonafide Amonafide (NSC308847, AS1413) produces protein-associated DNA-strand breaks through a topoisomerase II-mediated reaction, but does not produce topoisomerase I-mediated DNA cleavage. Phase 3.	Nat Commun, 2019, 10(1):4217 Front Oncol, 2019, 9:1406 Theranostics, 2015, 5(5):477-88
S1787	Teniposide Teniposide (NSC 122819, VM-26) is a chemotherapeutic medication mainly used in the treatment of childhood acute lymphocytic leukemia (ALL).	Hum Cell, 2022, 10.1007/s13577-022-00671-y Cancer Cell, 2021, S1535-6108(21)00659-0 Nat Commun, 2021, 12(1):6813
S1340	Gatifloxacin Gatifloxacin (AM-1155, CG5501, BMS-206584) is an antibiotic of the fourth-generation fluoroquinolone family, and inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.	Cancer Discov, 2020, CD-20-0160 Biochem Pharmacol, 2015, 95(4):227-37	Cleavable complex formation with nuclear DNA in P. falciparum treated with topoisomerase poisons. Parasites were metabolically labeled with [3H]hypoxanthine, treated with etoposide (■), gatifloxacin (●), levofloxacin(▲), ciprofloxacin (□), fleroxacin (○), or nalidixic acid (△) at the indicated concentrations for 18-22 h, lysed with SDS and digested with RNases. SDS and protein-bound DNA were precipitated with potassium. The fold increase in nuclear DNA capture as compared to solvent controls (mean of triplicate determinations) was plotted against concentration. Coefficient of variation for each data point was 19%.
S1222	Dexrazoxane HCl (ICRF-187) Dexrazoxane HCl (ICRF-187, ADR-529) is an intracellular iron chelator, which decreases the formation of superoxide radicals, used as a cardioprotective agent; also an inhibitor of topoisomerase II	PLoS Genet, 2019, 15(2):e1007925 J Virol, 2019, 93(11) EMBO Rep, 2017, 18(8):1412-1428
S1342	Genistein (NPI 031L) Genistein (NPI 031L), a phytoestrogen found in soy products, is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM or by insulin with IC50 of 19 μM.	ACS Appl Mater Interfaces, 2022, 14(21):24144-24159 Hum Cell, 2022, 10.1007/s13577-022-00671-y Adv Sci (Weinh), 2021, e2103360
S1940	Levofloxacin Levofloxacin (Fluoroquinolone) is a broad-spectrum antibiotic topoisomerase II and topoisomerase IV inhibitor, used to treat respiratory, urinary tract, gastrointestinal, and abdominal infections.	Adv Healthc Mater, 2022, e2102117 Exp Ther Med, 2021, 21(4):332 Mol Cell, 2020, 80(6):1104-1122.e9
S1393	Pirarubicin (NSC-333054) Pirarubicin (NSC-333054) is an anthracycline antibiotic, and also a DNA/RNA synthesis inhibitor by intercalating into DNA and interacts with topoisomerase II, used as an antineoplastic agent.	Cell Death Dis, 2022, 13(5):492 Int J Nanomedicine, 2021, 16:951-976 Pharmaceuticals (Basel), 2020, 14(1)E22
S1464	Marbofloxacin Marbofloxacin is a potent antibiotic inhibiting bacterial DNA replication.
S2027	Ciprofloxacin Ciprofloxacin (Bay o 9867) is a fluoroquinolone antibiotic, shows broad and potent antibacterial activity, with MIC90 of 0.024-6 μM.	Environ Mol Mutagen, 2019, 60(6):513-533	Ciprofoxacin (Cipro) reduces cancer cell survival in combination with chemotherapy. A and B, colony formation was conducted with A549 and SW48 cells treated with the clinically relevant chemotherapeutics cisplatin or 5-FU in the presence or absence of 2 μmol/L cipro ﬂoxacin. C, cipro ﬂ oxacin at 2 μmol/L decreased proliferation of KG-1 cells and slightly enhanced the effect of etoposide (Etop). , P < 0.05; *, P < 0.01 ( t tests).
S2492	Novobiocin Sodium (NSC 2382) Novobiocin Sodium (NSC 2382, Albamycin, Cathomycin) is an aminocoumarin antibiotic that targets bacterial DNA gyrase (TopoIV), used to treat susceptible gram positive bacteria.	Mol Cancer Ther, 2021, 10.1158/1535-7163.MCT-21-0215 Nat Cancer, 2021, 2(6):598-610 Mol Syst Biol, 2018, 14(3):e7858	Cell viability and caspase 3/7 activity in MDA-MB-231 cells co-treated with carbenoxolone, novobiocin, ibrutinib and bisphosphonates. Cell viability (A) and caspase 3/7 activity (B) was determined after treatment with ZA (zoledronic acid), RIS (risedronate), IBN (ibandronate), ALN (alendronate) in combination with carbenoxolone, novobiocin and ibrutinib. All data are expressed as means of three different measure points of three independent experiments ± SEM and were normalized to BP treatment alone. Significances were calculated with the Mann Whitney U test (p < 0.05; *p < 0.005).
S1756	Enoxacin Enoxacin (AT-2266, CI919, Pd107779, NSC 629661) is an oral broad-spectrum fluoroquinolone antibacterial agent by inhibiting bacterial DNA gyrase and topoisomerase IV, used to treat a wide variety of infections.	J Virol, 2020, 17;94(3) pii: e01233-19
S1463	Ofloxacin Ofloxacin (DL8280) is a synthetic broad-spectrum antimicrobial agent.
S1509	Norfloxacin Norfloxacin (MK-0366) is a broad-spectrum antibiotic. Norfloxacin (MK-0366) targets bacterial gyrase and topoisomerase IV enzymes.
S1327	Ellagic acid Ellagic acid (Elagostasine, Gallogen) has antiproliferative and antioxidant property.	Mol Cell, 2020, 80(6):1104-1122.e9 Kaohsiung J Med Sci, 2020, 6 Nutr Cancer, 2017, 69(7):1088-1098
S2328	Nalidixic acid Nalidixic acid (NSC-82174) is a synthetic 1,8-naphthyridine antimicrobial agent with a limited bacteriocidal spectrum. It is an inhibitor of the A subunit of bacterial DNA gyrase.	Hum Mol Genet, 2020, ddaa244 Int J Mol Sci, 2018, 19(6)
S7261	Beta-Lapachone Beta-Lapachone (β-Lapachone, ARQ-501) is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2.	Comput Struct Biotechnol J, 2022, 20:2442-2454 Free Radic Biol Med, 2021, 173:64-69 Front Pharmacol, 2021, 12:766909
S4006	Clinafloxacin Clinafloxacin (CI-960, PD127391, AM-1091) is a fluoroquinolone that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumoniae.
S6747	SW-044248 SW-044248 is a non-canonical Top1 inhibitor with a pattern of selective toxicity for NSCLC cells.
S5008	Ciprofloxacin hydrochloride Ciprofloxacin (CPX, Cetraxal, Ciloxan, Cipro, Bay-09867) hydrochloride, a fluorinated quinolone, is a β-diketone antibiotic with a broad spectrum antibacterial activity. Ciprofloxacin is an inhibitor of bacterial DNA gyrase (a subclass of Type II topoisomerases).
S4119	Pefloxacin Mesylate Dihydrate Pefloxacin Mesylate Dihydrate (1589 RB) is the third generation of fluoroquinolone class of antibacterials, which inhibits Topoisomerase II activity and DNA replication.
S5627	Amsacrine hydrochloride Amsacrine hydrochloride (m-AMSA, acridinyl anisidide) is the hydrochloride salt form of amsacrine, which is an inhibitor of topoisomerase II with antineoplastic activity.
S5964	Gatifloxacin hydrochloride Gatifloxacin (AM-1155, CG5501, BMS-206584, PD135432) hydrochloride is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases with IC50 of 13.8 μg/ml and 0.109 μg/ml for S. aureus topoisomerase IV and E. coli DNA gyrase, respectively.
S2064	Balofloxacin Balofloxacin (Q-35) is a quinolone antibiotic, inhibiting the synthesis of bacterial DNA by interference with the enqyme DNA gyrase.
S5026	Irinotecan hydrochloride Irinotecan (CPT-11, (+)-Irinotecan) hydrochloride is an inhibitor of Topoisomerase I (Topo I) that exhibits cytotoxicity in LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.	Cancers (Basel), 2022, 14(5)1230 Biomedicines, 2022, 10(2)438 Biomaterials, 2021, 280:121276
S2271	Berberine chloride (NSC 646666) Berberine chloride (NSC 646666, Natural Yellow 18) is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	J Biomol Struct Dyn, 2022, 1-11 Front Pharmacol, 2021, 12:632201 Molecules, 2021, 26(5)1210
S4604	Levofloxacin hydrate Levofloxacin (Levaquin, Tavanic, Quixin, Iquix, Cravit) is a broad-spectrum, third-generation fluoroquinolone antibiotic and optically active L-isomer of ofloxacin with antibacterial activity. It acts by inhibiting DNA gyrase (bacterial topoisomerase II).	Adv Healthc Mater, 2022, e2102117 Exp Ther Med, 2021, 21(4):332 Front Microbiol, 2020, 10:2936
S0093	Genz-644282 Genz-644282 is a non-camptothecin topoisomerase I (Topo I) inhibitor that demonstrates potent cytotoxic activity with a median IC50 of 1.2 nM (range 0.2 nM-21.9 nM). Genz-644282 can be used in cancer research.
S2423	(S)-10-Hydroxycamptothecin (S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor with potent anti-tumor activity.	Nat Commun, 2022, 13(1):2861 ACS Appl Mater Interfaces, 2021, 13(47):56519-56529 Carcinogenesis, 2021, bgab002
S6790	Ellipticine hydrochloride Ellipticine Hydrochloride (NSC 71795, PZE) is a potent inhibitor of DNA topoisomerase II and forms covalent DNA adducts mediated by its oxidation with cytochromes P450 (CYP) and peroxidases. Ellipticine Hydrochloride is a natural product isolated from the Australian evergreen tree of the Apocynaceae family with antineoplastic activity.
S9321	Topotecan Topotecan is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.	Clin Transl Med, 2022, 12(5):e881 Int J Mol Sci, 2022, 23(10)5532 Nat Commun, 2021, 12(1):5404
S7518	Voreloxin (SNS-595) hydrochloride Voreloxin hydrochloride (SNS-595, Vosaroxin) is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2.	Adv Sci (Weinh), 2020, 7(21):2001018 Apoptosis, 2019, 24(11-12):849-861 Target Oncol, 2019, 14(3):351-364
S5059	Pixantrone Maleate Pixantrone (BBR-2778) is a novel aza-anthracenedione compound with antitumor activity. It is a weak topoisomerase II inhibitor and forms stable DNA adducts through alkylation with specificity for DNA hypermethylated sites.
S3603	Betulinic acid Betulinic acid (ALS-357, Lupatic acid, Betulic acid), a pentacyclic triterpenoid from Syzigium claviflorum, is a inhibitor of HIV-1 with EC50 of 1.4 μ M. Betulinic acid acts as a new activator of NF-kB. Phase 1/2.	Mol Ther Nucleic Acids, 2022, 28:435-449 Oxid Med Cell Longev, 2021, 2021:5519587 J Cardiovasc Pharmacol, 2021, 78(2):235-246
S5111	7-Ethylcamptothecin 7-Ethyl Camptothecin is an anti-cancer chemical that exhibits a strong activity against various murine tumors through Topo I (topoisomerase) inhibition.
S2653	9-amino-CPT (9-Aminocamptothecin) 9-amino-CPT (9-Aminocamptothecin, 9-AC, Aminocamptothecin, 9-amino-20(S)-camptothecin) is a Topoisomerase I inhibitor with potent anticancer activities. 9-amino-CPT (9-Aminocamptothecin) is an active, water-insoluble derivative of camptothecin.
S3898	Hydroxy Camptothecine Hydroxy Camptothecine (10-Hydroxycamptothecin, Hydroxycamptothecine) is a cell-permeable powerful DNA topoisomerase I inhibitor. It has selective inhibitory effect on the phosphorylation of histone H1 and H3, but less effect on other histones.	Life Sci, 2020, 246:117428
S2288	Rubitecan Rubitecan (9-NC, 9-Nitro-camptothecin, Partaject Orathecin, Partaject rubitecan, RFS 2000) is a topoisomerase I inhibitor extracted from the bark and leaves of the Camptotheca acuminata tree, which is native to China. Rubitecan is an oral camptothecin with antitumour activity.
S6631	Belotecan (CKD-602) hydrochloride Belotecan (CKD-602) is a potent DNA topoisomerase I inhibitor that exerts a clinical anticancer effect on various types of tumor.
S3181	Flumequine Flumequine is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM.

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
S9634	Phenoxodiol (Haginin E) Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II.	Anticancer Res, 2018, 38(10):5709-5716

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

S9634

Phenoxodiol (Haginin E)

Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II.

Anticancer Res, 2018, 38(10):5709-5716