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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
S1208	Doxorubicin (Adriamycin) HCl	20 mg/mL	100 mg/mL	<1 mg/mL
S1225	Etoposide	<1 mg/mL	100 mg/mL	'''<1 mg/mL
S1288	Camptothecin	<1 mg/mL	3 mg/mL	''<1 mg/mL
S1231	Topotecan HCl	91 mg/mL	91 mg/mL	''<1 mg/mL
S1228	Idarubicin HCl	5 mg/mL	100 mg/mL	'<1 mg/mL
S2653	9-amino-CPT (9-Aminocamptothecin)	<1 mg/mL	25 mg/mL	'''<1 mg/mL
S0093	Genz-644282	<1 mg/mL	<1 mg/mL	'''<1 mg/mL
S2288	Rubitecan	<1 mg/mL	58 mg/mL	<1 mg/mL
S6747	SW-044248	<1 mg/mL	14 mg/mL	<1 mg/mL
S6631	Belotecan (CKD-602) hydrochloride	4 mg/mL	47 mg/mL	<1 mg/mL
S1223	Epirubicin HCl	100 mg/mL	100 mg/mL	''<1 mg/mL
S2485	Mitoxantrone 2HCl	89 mg/mL	89 mg/mL	''''<1 mg/mL
S3035	Daunorubicin HCl	100 mg/mL	100 mg/mL	''<1 mg/mL
S1465	Moxifloxacin HCl	60 mg/mL	87 mg/mL	<1 mg/mL
S2217	Irinotecan 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	<1 mg/mL	54 mg/mL	2 mg/mL
S1940	Levofloxacin	11 mg/mL	24 mg/mL	9 mg/mL
S1393	Pirarubicin	<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	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
S4119	Pefloxacin Mesylate Dihydrate	67 mg/mL	9 mg/mL	<1 mg/mL
S2064	Balofloxacin	<1 mg/mL	5 mg/mL	<1 mg/mL
S4591	Nitroxoline	<1 mg/mL	38 mg/mL	<1 mg/mL
S4604	Levofloxacin hydrate	5 mg/mL	74 mg/mL	10 mg/mL
S2423	(S)-10-Hydroxycamptothecin	<1 mg/mL	8 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
S3898	Hydroxy Camptothecine	-1 mg/mL	29 mg/mL	-1 mg/mL
S3181	Flumequine	<1 mg/mL	3 mg/mL	<1 mg/mL
S6790	Ellipticine hydrochloride	˂1 mg/mL	3 mg/mL	˂1 mg/mL

亜型選択性的な製品

Topoisomerase製品

All (47) Topoisomerase阻害剤(46)

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) 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.	Nat Commun, 2020, 24;11(1):1972 PLoS Biol, 2020, 23;18(3):e3000666 Cancer Res, 2020, 10.1158/0008-5472.CAN-19-2069	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 Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity. Etoposide induces autophagy, mitophagy and apoptosis.	Mol Cell, 2020, 22 pii: S1097-2765(20)30231-8 Nat Chem Biol, 2020, 6 Genes Dev, 2020, 1;34(9-10):637-649	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 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.	Cancer Cell, 2020, 37(3):371-386 Nat Chem Biol, 2020, 6 Nat Commun, 2020, 11(1):3018	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 HCl Topotecan HCl 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.	Nat Commun, 2020, 29;11(1):2086 Front Oncol, 2020, 12;10:700 Cancer Cell Int, 2020, 19;20:58	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.
S1228	Idarubicin HCl Idarubicin HCl 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.	Cancer Cell Int, 2020, 19;20:58 Toxicol In Vitro, 2020, 104928 Cell Stem Cell, 2019, 25(2):258-272	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.
S2653^新	9-amino-CPT (9-Aminocamptothecin) 9-amino-CPT (9-Aminocamptothecin) is a Topoisomerase I inhibitor with potent anticancer activities. 9-amino-CPT (9-Aminocamptothecin) is an active, water-insoluble derivative of camptothecin.
S0093^新	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.
S2288^新	Rubitecan Rubitecan 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.
S6747^新	SW-044248 SW-044248 is a non-canonical Top1 inhibitor with a pattern of selective toxicity for NSCLC cells.
S6631^新	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.
S1223	Epirubicin HCl Epirubicin HCl, a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase. Epirubicin induces apoptosis.	Cancer Cell Int, 2020, 19;20:58 Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193	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 2HCl Mitoxantrone 2HCl 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.	Cancer Cell Int, 2020, 19;20:58 J Lipid Res, 2019, 60(6):1078-1086 Front Oncol, 2019, 9:436	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 HCl Daunorubicin HCl 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.	Haematologica, 2020, 12;haematol.2019.233445 Cancer Cell Int, 2020, 19;20:58 Haematologica, 2019, 10.3324/haematol.2019.224956	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 HCl Moxifloxacin is a fourth-generation synthetic fluoroquinolone antibacterial agent.	Clin Transl Sci, 2019, 12(6):687-697 Front Microbiol, 2018, 6:336 Transl Vis Sci Technol, 2016, 5(6):3
S2217	Irinotecan HCl Trihydrate Irinotecan prevents DNA from unwinding by inhibition of topoisomerase 1.	Cancer Cell, 2020, 37(3):340-353 J Hematol Oncol, 2020, 1;13(1):40 J-Cancer, 2020, 6;11-14-:4047-4058	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 is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy.	Small, 2020, 10.1002/smll.201906360 J Pharm Biomed Anal, 2020, 20;181:113073 Pharmacol Res, 2019, 148:104368	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 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 is a chemotherapeutic medication mainly used in the treatment of childhood acute lymphocytic leukemia (ALL).	Cancer Cell Int, 2020, 19;20:58 Cell Syst, 2019, 8(2):97-108 Environ Mol Mutagen, 2019, 60(6):513-533
S1340	Gatifloxacin Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, and inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.	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) Oncotarget, 2016, 7(19):28286-300
S1342	Genistein Genistein, 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.	Cancer Cell Int, 2020, 19;20:58 Mol Cell, 2019, 75(6):1103-1116.e9 Cancer Manag Res, 2018, 10:6205-6216
S1940	Levofloxacin Levofloxacin is a broad-spectrum antibiotic topoisomerase II and topoisomerase IV inhibitor, used to treat respiratory, urinary tract, gastrointestinal, and abdominal infections.	Front Microbiol, 2020, 10:2936 ACS Infect Dis, 2019, 5(9):1559-1569 Nature, 2018, 560(7718):372-376
S1393	Pirarubicin Pirarubicin 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.	Cancer Cell, 2019, 36(2):179-193 Cell, 2019, 36(2):179-193 J Cell Mol Med, 2019, 23(5):3386-3401
S1464	Marbofloxacin Marbofloxacin is a potent antibiotic inhibiting bacterial DNA replication.
S2027	Ciprofloxacin Ciprofloxacin 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 Novobiocin Sodium is an aminocoumarin antibiotic that targets bacterial DNA gyrase (TopoIV), used to treat susceptible gram positive bacteria.	Mol Syst Biol, 2018, 14(3):e7858 Mol Cancer, 2014, 13(1):265	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 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 is a synthetic broad-spectrum antimicrobial agent.
S1509	Norfloxacin Norfloxacin is a broad-spectrum antibiotic.
S1327	Ellagic acid Ellagic acid has antiproliferative and antioxidant property.	Kaohsiung J Med Sci, 2020, 6 Nutr Cancer, 2017, 69(7):1088-1098 J Nutr Biochem, 2015, 26(11):1379-84
S2328	Nalidixic acid Nalidixic acid 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.	Int J Mol Sci, 2018, 19(6)
S7261	Beta-Lapachone Beta-Lapachone is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2.	Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0220-1 Environ Mol Mutagen, 2019, 60(6):513-533 Anticancer Res, 2019, 39(7):3677-3686
S4006	Clinafloxacin Clinafloxacin is a fluoroquinolone that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumoniae.
S4119	Pefloxacin Mesylate Dihydrate Pefloxacin Mesylate Dihydrate is the third generation of fluoroquinolone class of antibacterials, which inhibits Topoisomerase II activity and DNA replication.
S5627	Amsacrine hydrochloride Amsacrine hydrochloride is the hydrochloride salt form of amsacrine, which is an inhibitor of topoisomerase II with antineoplastic activity.
S2064	Balofloxacin Balofloxacin is a quinolone antibiotic, inhibiting the synthesis of bacterial DNA by interference with the enqyme DNA gyrase.
S4591	Nitroxoline Nitroxoline is a urinary antibacterial agent active against susceptible gram-positive and gram-negative organisms commonly found in urinary tract infections. It is a fluorquinolone that is active against bacterial gyrases.	mBio, 2018, 9(5)
S4604	Levofloxacin hydrate Levofloxacin 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).	Front Microbiol, 2020, 10:2936
S2423	(S)-10-Hydroxycamptothecin 10-Hydroxycamptothecin is a DNA topoisomerase I inhibitor with potent anti-tumor activity.	J Cell Physiol, 2019, 10.1002/jcp.29307 J Pharmacol Exp Ther, 2014, 348(3):432-41
S9321	Topotecan Topotecan is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.	Front Oncol, 2020, 12;10:700 Genome Res, 2019, 29(10):1659-1672 Front Oncol, 2019, 9:1202
S7518	Voreloxin (SNS-595) hydrochloride Voreloxin is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2.	Apoptosis, 2019, 24(11-12):849-861 Target Oncol, 2019, 14(3):351-364 PLoS One, 2018, 13(5):e0196805
S5059	Pixantrone Maleate Pixantrone 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, 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.	Eur J Pharmacol, 2020, 873:172981 Acta Biochim Biophys Sin (Shanghai), 2020, 10.1093/abbs/gmz148
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.
S3898	Hydroxy Camptothecine 10-Hydroxycamptothecin 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
S3181	Flumequine Flumequine is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM.
S6790^新	Ellipticine hydrochloride Ellipticine Hydrochloride 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.

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) 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.	Nat Commun, 2020, 24;11(1):1972 PLoS Biol, 2020, 23;18(3):e3000666 Cancer Res, 2020, 10.1158/0008-5472.CAN-19-2069	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 Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity. Etoposide induces autophagy, mitophagy and apoptosis.	Mol Cell, 2020, 22 pii: S1097-2765(20)30231-8 Nat Chem Biol, 2020, 6 Genes Dev, 2020, 1;34(9-10):637-649	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 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.	Cancer Cell, 2020, 37(3):371-386 Nat Chem Biol, 2020, 6 Nat Commun, 2020, 11(1):3018	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 HCl Topotecan HCl 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.	Nat Commun, 2020, 29;11(1):2086 Front Oncol, 2020, 12;10:700 Cancer Cell Int, 2020, 19;20:58	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.
S1228	Idarubicin HCl Idarubicin HCl 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.	Cancer Cell Int, 2020, 19;20:58 Toxicol In Vitro, 2020, 104928 Cell Stem Cell, 2019, 25(2):258-272	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.
S2653^新	9-amino-CPT (9-Aminocamptothecin) 9-amino-CPT (9-Aminocamptothecin) is a Topoisomerase I inhibitor with potent anticancer activities. 9-amino-CPT (9-Aminocamptothecin) is an active, water-insoluble derivative of camptothecin.
S0093^新	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.
S2288^新	Rubitecan Rubitecan 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.
S6747^新	SW-044248 SW-044248 is a non-canonical Top1 inhibitor with a pattern of selective toxicity for NSCLC cells.
S6631^新	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.
S1223	Epirubicin HCl Epirubicin HCl, a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase. Epirubicin induces apoptosis.	Cancer Cell Int, 2020, 19;20:58 Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193	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 2HCl Mitoxantrone 2HCl 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.	Cancer Cell Int, 2020, 19;20:58 J Lipid Res, 2019, 60(6):1078-1086 Front Oncol, 2019, 9:436	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 HCl Daunorubicin HCl 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.	Haematologica, 2020, 12;haematol.2019.233445 Cancer Cell Int, 2020, 19;20:58 Haematologica, 2019, 10.3324/haematol.2019.224956	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 HCl Moxifloxacin is a fourth-generation synthetic fluoroquinolone antibacterial agent.	Clin Transl Sci, 2019, 12(6):687-697 Front Microbiol, 2018, 6:336 Transl Vis Sci Technol, 2016, 5(6):3
S2217	Irinotecan HCl Trihydrate Irinotecan prevents DNA from unwinding by inhibition of topoisomerase 1.	Cancer Cell, 2020, 37(3):340-353 J Hematol Oncol, 2020, 1;13(1):40 J-Cancer, 2020, 6;11-14-:4047-4058	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 is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy.	Small, 2020, 10.1002/smll.201906360 J Pharm Biomed Anal, 2020, 20;181:113073 Pharmacol Res, 2019, 148:104368	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 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 is a chemotherapeutic medication mainly used in the treatment of childhood acute lymphocytic leukemia (ALL).	Cancer Cell Int, 2020, 19;20:58 Cell Syst, 2019, 8(2):97-108 Environ Mol Mutagen, 2019, 60(6):513-533
S1340	Gatifloxacin Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, and inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.	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) Oncotarget, 2016, 7(19):28286-300
S1342	Genistein Genistein, 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.	Cancer Cell Int, 2020, 19;20:58 Mol Cell, 2019, 75(6):1103-1116.e9 Cancer Manag Res, 2018, 10:6205-6216
S1940	Levofloxacin Levofloxacin is a broad-spectrum antibiotic topoisomerase II and topoisomerase IV inhibitor, used to treat respiratory, urinary tract, gastrointestinal, and abdominal infections.	Front Microbiol, 2020, 10:2936 ACS Infect Dis, 2019, 5(9):1559-1569 Nature, 2018, 560(7718):372-376
S1393	Pirarubicin Pirarubicin 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.	Cancer Cell, 2019, 36(2):179-193 Cell, 2019, 36(2):179-193 J Cell Mol Med, 2019, 23(5):3386-3401
S1464	Marbofloxacin Marbofloxacin is a potent antibiotic inhibiting bacterial DNA replication.
S2027	Ciprofloxacin Ciprofloxacin 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 Novobiocin Sodium is an aminocoumarin antibiotic that targets bacterial DNA gyrase (TopoIV), used to treat susceptible gram positive bacteria.	Mol Syst Biol, 2018, 14(3):e7858 Mol Cancer, 2014, 13(1):265	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 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 is a synthetic broad-spectrum antimicrobial agent.
S1509	Norfloxacin Norfloxacin is a broad-spectrum antibiotic.
S1327	Ellagic acid Ellagic acid has antiproliferative and antioxidant property.	Kaohsiung J Med Sci, 2020, 6 Nutr Cancer, 2017, 69(7):1088-1098 J Nutr Biochem, 2015, 26(11):1379-84
S2328	Nalidixic acid Nalidixic acid 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.	Int J Mol Sci, 2018, 19(6)
S7261	Beta-Lapachone Beta-Lapachone is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2.	Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0220-1 Environ Mol Mutagen, 2019, 60(6):513-533 Anticancer Res, 2019, 39(7):3677-3686
S4006	Clinafloxacin Clinafloxacin is a fluoroquinolone that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumoniae.
S4119	Pefloxacin Mesylate Dihydrate Pefloxacin Mesylate Dihydrate is the third generation of fluoroquinolone class of antibacterials, which inhibits Topoisomerase II activity and DNA replication.
S5627	Amsacrine hydrochloride Amsacrine hydrochloride is the hydrochloride salt form of amsacrine, which is an inhibitor of topoisomerase II with antineoplastic activity.
S2064	Balofloxacin Balofloxacin is a quinolone antibiotic, inhibiting the synthesis of bacterial DNA by interference with the enqyme DNA gyrase.
S4591	Nitroxoline Nitroxoline is a urinary antibacterial agent active against susceptible gram-positive and gram-negative organisms commonly found in urinary tract infections. It is a fluorquinolone that is active against bacterial gyrases.	mBio, 2018, 9(5)
S4604	Levofloxacin hydrate Levofloxacin 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).	Front Microbiol, 2020, 10:2936
S2423	(S)-10-Hydroxycamptothecin 10-Hydroxycamptothecin is a DNA topoisomerase I inhibitor with potent anti-tumor activity.	J Cell Physiol, 2019, 10.1002/jcp.29307 J Pharmacol Exp Ther, 2014, 348(3):432-41
S9321	Topotecan Topotecan is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.	Front Oncol, 2020, 12;10:700 Genome Res, 2019, 29(10):1659-1672 Front Oncol, 2019, 9:1202
S7518	Voreloxin (SNS-595) hydrochloride Voreloxin is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2.	Apoptosis, 2019, 24(11-12):849-861 Target Oncol, 2019, 14(3):351-364 PLoS One, 2018, 13(5):e0196805
S5059	Pixantrone Maleate Pixantrone 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, 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.	Eur J Pharmacol, 2020, 873:172981 Acta Biochim Biophys Sin (Shanghai), 2020, 10.1093/abbs/gmz148
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.
S3898	Hydroxy Camptothecine 10-Hydroxycamptothecin 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
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
S6790^新	Ellipticine hydrochloride Ellipticine Hydrochloride 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.

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

S6790^新

Ellipticine hydrochloride

Ellipticine Hydrochloride 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.