Topoisomerase

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研究领域

抑制剂选择性比较

特异性亚型抑制剂

Topoisomerase产品

所有产品 Topoisomerase抑制剂(44)

目录号	产品描述	文献引用	实验数据
S1208	Doxorubicin (Adriamycin) HCl Doxorubicin (Adriamycin) HCl是一种抗生素类试剂，可抑制DNA topoisomerase II，并在肿瘤细胞中诱导DNA损伤、线粒体自噬和凋亡。Doxorubicin 可降低 AMPK的基础磷酸化。Doxorubicin 可应用于HIV感染病人的联合治疗，但是在免疫治疗中有将HBV重活化的风险。	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是一种鬼臼毒素的半合成衍生物，通过抑制topoisomerase II 活性而抑制DNA合成。Etoposide可诱导自噬、线粒体自噬和细胞凋亡。	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是一种特异性的DNA拓扑异构酶I (Topo I)抑制剂，IC50为0.68 μM。Phase 2。	Cancer Cell, 2020, 37(3):371-386 Nat Chem Biol, 2020, 6 Nat Commun, 2020, 19;11(1):908	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是一种拓扑异构酶I抑制剂，作用于MCF-7 Luc细胞和DU-145 Luc细胞，无细胞试验中IC50分别为13 nM和2 nM。	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是蒽环类抗生素Idarubicin的盐酸盐形式，抑制MCF-7细胞中的DNA拓扑异构酶II (topo II)，无细胞试验中IC50为3.3 ng/mL。	Cancer Cell Int, 2020, 19;20:58 Cell Stem Cell, 2019, 25(2):258-272 Cancer Res, 2019, 79(10):2466-2479	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.
S2288^New	Rubitecan Rubitecan 是一种拓扑异构酶I topoisomerase I 的抑制剂，从中国喜树的树皮和叶子中提取。Rubitecan 也是一种具有抗肿瘤活性的口服喜树碱。
S6747^New	SW-044248 SW-044248是非经典的Topo1抑制剂，对非小细胞肺癌细胞具有选择性毒性作用。
S6631^New	Belotecan (CKD-602) hydrochloride Belotecan (CKD-602)是有效的DNA topoisomerase I抑制剂，可对多种类型的肿瘤发挥抗癌活性。
S1223	Epirubicin HCl Epirubicin HCl是阿霉素的半合成L-阿拉伯糖衍生物，通过抑制拓扑异构酶而具有抗肿瘤作用。	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是Mitoxantrone的盐酸盐形式，是一种合成的抗肿瘤蒽二酮(IC50为0.42 mM)。	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抑制DNA和RNA合成，无细胞试验中抑制DNA合成的K_i为0.02 μM。Daunorubicin 是 topoisomerase II 的抑制剂并可诱导凋亡。	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 HCl是一种第四代喹诺酮类抗菌剂。	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 HCl Trihydrate通过抑制Topoisomerase 1（拓扑异构酶1）而防止DNA解链。	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是CPT-11的一种活性代谢物，抑制DNA topoisomerase I，DNA合成，并造成频繁的DNA单链断裂。	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通过topoisomerase II（拓扑异构酶II）介导导致蛋白相关的DNA链断裂，但不会产生拓扑异构酶I介导的DNA裂解。Phase 3。	Nat Commun, 2019, 10(1):4217 Front Oncol, 2019, 9:1406 Theranostics, 2015, 5(5):477-88
S1787	Teniposide Teniposide 是一种化疗药物，主要用于治疗儿童急性淋巴细胞性白血病（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是第四代喹诺酮类抗生素。	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)是一种胞内铁螯合剂，能够减少氧自由基的生成，是心脏保护剂。也是topoisomerase II的抑制剂。	PLoS Genet, 2019, 15(2):e1007925 J Virol, 2019, 93(11) Oncotarget, 2016, 7(19):28286-300
S1342	Genistein Genistein是一种来源于大豆的植物雌激素，是一种高特异性的蛋白酪氨酸激酶(PTK) 的抑制剂，在NIH-3T3细胞中通过EGF或者胰岛素介导而抑制有丝分裂，IC50分别为12μM和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 是一种宽谱的的抗生素类 topoisomerase II和topoisomerase IV抑制剂，用于治疗呼吸道，尿道及消化道感染。	Front Microbiol, 2020, 10:2936 ACS Infect Dis, 2019, 5(9):1559-1569 Nature, 2018, 560(7718):372-376
S1393	Pirarubicin Pirarubicin是一种蒽环类抗生素，同时也是一种DNA/RNA合成抑制剂，掺入DNA并与topoisomerase II相互作用，是一种抗肿瘤药物。	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是有效的抗生素，抑制细菌DNA复制。
S2027	Ciprofloxacin Ciprofloxacin是一种喹诺酮类抗生素, 具有广谱有效的抗菌活性，MIC90为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 是一种非常有效的细菌DNA旋转酶和人体有机阴离子转运体，作用于hOAT1，hOAT3和hOAT4，K_i分别为14.87±0.40μM, 4.77±1.12μM 和 90.50±7.50μM。	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 是一种口服的广谱喹诺酮类抗菌剂，用于治疗尿路感染和淋病。常见的副作用有失眠。	J Virol, 2020, 17;94(3) pii: e01233-19
S1463	Ofloxacin Ofloxacin是一种合成的广谱抗菌剂。
S1509	Norfloxacin Norfloxacin是一种广谱抗生素。
S1327	Ellagic acid Ellagic acid具有抗增殖和抗氧化性能。	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 是一种合成的1,8-二氮杂萘类抗菌剂，具有有限的抗菌谱，抑制细菌DNA促旋酶的A亚基。	Int J Mol Sci, 2018, 19(6)
S7261	Beta-Lapachone Beta-Lapachone是一种选择性的DNA topoisomerase I（DNA拓扑异构酶I）抑制剂，对DNA拓扑异构酶II或连接酶无抑制作用。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 是一种氟喹诺酮类药物，可以抑制肺炎双球菌中 DNA旋转酶和拓扑异构酶IV。
S4119	Pefloxacin Mesylate Dihydrate Pefloxacin Mesylate Dihydrate是第三代氟喹诺酮类抗菌药，可以抑制拓扑异构酶II的活性和DNA复制。
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是一种喹诺酮类抗生素，通过干扰DNA促旋酶，而抑制细菌DNA合成。
S4591	Nitroxoline Nitroxoline是一种尿液抗菌剂。它是一种氟喹诺酮，具有抗细菌促旋酶活性。	mBio, 2018, 9(5)
S4604	Levofloxacin hydrate Levofloxacin是一种广谱的第三代氟喹诺酮抗生素，是氧氟沙星具有光学活性的L型异构体，具有抗菌活性。它通过抑制DNA gyrase（细菌topoisomerase II）发挥作用。	Front Microbiol, 2020, 10:2936
S2423	(S)-10-Hydroxycamptothecin (S)-10-Hydroxycamptothecin是DNA拓扑异构酶I抑制剂，具有有效的抗肿瘤活性。	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 是强效的广谱抗肿瘤活性的Topoisomerase II抑制剂。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是一种新型的aza-anthracenedione化合物，具有抗肿瘤活性。它对topoisomerase II具有弱抑制活性，通过对DNA超甲基化位点烷基化，形成DNA加合物。
S3603	Betulinic acid Betulinic acid是一种天然的五环三萜类化合物，具有抗病毒，抗疟药，抗发炎和抗肿瘤的特性。Betulinic acid也是 NF-kB 的活化剂。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是一种人工合成的化疗用抗生素，抑制拓扑异构酶II， IC50为15 μM。
S6790^New	Ellipticine hydrochloride Ellipticine Hydrochloride 是一种有效的 DNA topoisomerase II 的抑制剂，并通过其与 cytochromes P450 (CYP) 和 peroxidases 的氧化作用介导形成共价DNA加合物。Ellipticine Hydrochloride 是从澳大利亚的夹竹桃科常绿乔木中分离出来的具有抗肿瘤活性的天然产物。

目录号	产品描述	文献引用	实验数据
S1208	Doxorubicin (Adriamycin) HCl Doxorubicin (Adriamycin) HCl是一种抗生素类试剂，可抑制DNA topoisomerase II，并在肿瘤细胞中诱导DNA损伤、线粒体自噬和凋亡。Doxorubicin 可降低 AMPK的基础磷酸化。Doxorubicin 可应用于HIV感染病人的联合治疗，但是在免疫治疗中有将HBV重活化的风险。	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是一种鬼臼毒素的半合成衍生物，通过抑制topoisomerase II 活性而抑制DNA合成。Etoposide可诱导自噬、线粒体自噬和细胞凋亡。	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是一种特异性的DNA拓扑异构酶I (Topo I)抑制剂，IC50为0.68 μM。Phase 2。	Cancer Cell,2020, 37(3):371-386 Nat Chem Biol,2020, 6 Nat Commun,2020, 19;11(1):908	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是一种拓扑异构酶I抑制剂，作用于MCF-7 Luc细胞和DU-145 Luc细胞，无细胞试验中IC50分别为13 nM和2 nM。	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是蒽环类抗生素Idarubicin的盐酸盐形式，抑制MCF-7细胞中的DNA拓扑异构酶II (topo II)，无细胞试验中IC50为3.3 ng/mL。	Cancer Cell Int,2020, 19;20:58 Cell Stem Cell,2019, 25(2):258-272 Cancer Res,2019, 79(10):2466-2479	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.
S2288^New	Rubitecan Rubitecan 是一种拓扑异构酶I topoisomerase I 的抑制剂，从中国喜树的树皮和叶子中提取。Rubitecan 也是一种具有抗肿瘤活性的口服喜树碱。
S6747^New	SW-044248 SW-044248是非经典的Topo1抑制剂，对非小细胞肺癌细胞具有选择性毒性作用。
S6631^New	Belotecan (CKD-602) hydrochloride Belotecan (CKD-602)是有效的DNA topoisomerase I抑制剂，可对多种类型的肿瘤发挥抗癌活性。
S1223	Epirubicin HCl Epirubicin HCl是阿霉素的半合成L-阿拉伯糖衍生物，通过抑制拓扑异构酶而具有抗肿瘤作用。	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是Mitoxantrone的盐酸盐形式，是一种合成的抗肿瘤蒽二酮(IC50为0.42 mM)。	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抑制DNA和RNA合成，无细胞试验中抑制DNA合成的K_i为0.02 μM。Daunorubicin 是 topoisomerase II 的抑制剂并可诱导凋亡。	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 HCl是一种第四代喹诺酮类抗菌剂。	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 HCl Trihydrate通过抑制Topoisomerase 1（拓扑异构酶1）而防止DNA解链。	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是CPT-11的一种活性代谢物，抑制DNA topoisomerase I，DNA合成，并造成频繁的DNA单链断裂。	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通过topoisomerase II（拓扑异构酶II）介导导致蛋白相关的DNA链断裂，但不会产生拓扑异构酶I介导的DNA裂解。Phase 3。	Nat Commun,2019, 10(1):4217 Front Oncol,2019, 9:1406 Theranostics,2015, 5(5):477-88
S1787	Teniposide Teniposide 是一种化疗药物，主要用于治疗儿童急性淋巴细胞性白血病（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是第四代喹诺酮类抗生素。	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)是一种胞内铁螯合剂，能够减少氧自由基的生成，是心脏保护剂。也是topoisomerase II的抑制剂。	PLoS Genet,2019, 15(2):e1007925 J Virol,2019, 93(11) Oncotarget,2016, 7(19):28286-300
S1342	Genistein Genistein是一种来源于大豆的植物雌激素，是一种高特异性的蛋白酪氨酸激酶(PTK) 的抑制剂，在NIH-3T3细胞中通过EGF或者胰岛素介导而抑制有丝分裂，IC50分别为12μM和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 是一种宽谱的的抗生素类 topoisomerase II和topoisomerase IV抑制剂，用于治疗呼吸道，尿道及消化道感染。	Front Microbiol,2020, 10:2936 ACS Infect Dis,2019, 5(9):1559-1569 Nature,2018, 560(7718):372-376
S1393	Pirarubicin Pirarubicin是一种蒽环类抗生素，同时也是一种DNA/RNA合成抑制剂，掺入DNA并与topoisomerase II相互作用，是一种抗肿瘤药物。	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是有效的抗生素，抑制细菌DNA复制。
S2027	Ciprofloxacin Ciprofloxacin是一种喹诺酮类抗生素, 具有广谱有效的抗菌活性，MIC90为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 是一种非常有效的细菌DNA旋转酶和人体有机阴离子转运体，作用于hOAT1，hOAT3和hOAT4，K_i分别为14.87±0.40μM, 4.77±1.12μM 和 90.50±7.50μM。	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 是一种口服的广谱喹诺酮类抗菌剂，用于治疗尿路感染和淋病。常见的副作用有失眠。	J Virol,2020, 17;94(3) pii: e01233-19
S1463	Ofloxacin Ofloxacin是一种合成的广谱抗菌剂。
S1509	Norfloxacin Norfloxacin是一种广谱抗生素。
S1327	Ellagic acid Ellagic acid具有抗增殖和抗氧化性能。	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 是一种合成的1,8-二氮杂萘类抗菌剂，具有有限的抗菌谱，抑制细菌DNA促旋酶的A亚基。	Int J Mol Sci,2018, 19(6)
S7261	Beta-Lapachone Beta-Lapachone是一种选择性的DNA topoisomerase I（DNA拓扑异构酶I）抑制剂，对DNA拓扑异构酶II或连接酶无抑制作用。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 是一种氟喹诺酮类药物，可以抑制肺炎双球菌中 DNA旋转酶和拓扑异构酶IV。
S4119	Pefloxacin Mesylate Dihydrate Pefloxacin Mesylate Dihydrate是第三代氟喹诺酮类抗菌药，可以抑制拓扑异构酶II的活性和DNA复制。
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是一种喹诺酮类抗生素，通过干扰DNA促旋酶，而抑制细菌DNA合成。
S4591	Nitroxoline Nitroxoline是一种尿液抗菌剂。它是一种氟喹诺酮，具有抗细菌促旋酶活性。	mBio,2018, 9(5)
S4604	Levofloxacin hydrate Levofloxacin是一种广谱的第三代氟喹诺酮抗生素，是氧氟沙星具有光学活性的L型异构体，具有抗菌活性。它通过抑制DNA gyrase（细菌topoisomerase II）发挥作用。	Front Microbiol,2020, 10:2936
S2423	(S)-10-Hydroxycamptothecin (S)-10-Hydroxycamptothecin是DNA拓扑异构酶I抑制剂，具有有效的抗肿瘤活性。	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 是强效的广谱抗肿瘤活性的Topoisomerase II抑制剂。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是一种新型的aza-anthracenedione化合物，具有抗肿瘤活性。它对topoisomerase II具有弱抑制活性，通过对DNA超甲基化位点烷基化，形成DNA加合物。
S3603	Betulinic acid Betulinic acid是一种天然的五环三萜类化合物，具有抗病毒，抗疟药，抗发炎和抗肿瘤的特性。Betulinic acid也是 NF-kB 的活化剂。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是一种人工合成的化疗用抗生素，抑制拓扑异构酶II， IC50为15 μM。

目录号	产品描述	文献引用	实验数据
S6790^New	Ellipticine hydrochloride Ellipticine Hydrochloride 是一种有效的 DNA topoisomerase II 的抑制剂，并通过其与 cytochromes P450 (CYP) 和 peroxidases 的氧化作用介导形成共价DNA加合物。Ellipticine Hydrochloride 是从澳大利亚的夹竹桃科常绿乔木中分离出来的具有抗肿瘤活性的天然产物。

目录号

产品描述

文献引用

实验数据

S6790^New

Ellipticine hydrochloride

Ellipticine Hydrochloride 是一种有效的 DNA topoisomerase II 的抑制剂，并通过其与 cytochromes P450 (CYP) 和 peroxidases 的氧化作用介导形成共价DNA加合物。Ellipticine Hydrochloride 是从澳大利亚的夹竹桃科常绿乔木中分离出来的具有抗肿瘤活性的天然产物。

研究领域

产品类型

Topoisomerase

信号通路图

研究领域

抑制剂选择性比较

特异性亚型抑制剂

Topoisomerase产品