Topoisomerase
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| 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 |
| S5059 | Pixantrone Maleate | 100 mg/mL | 100 mg/mL | 1 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 |
| 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, ADR-529) | 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 |
| S7518 | Voreloxin (SNS-595) hydrochloride | 1 mg/mL | 1 mg/mL | <1 mg/mL |
| S3603 | Betulinic acid | <1 mg/mL | 20 mg/mL | 10 mg/mL |
| S3181 | Flumequine | <1 mg/mL | 3 mg/mL | <1 mg/mL |
- Topoisomerase抑制剂（39）
- 新Topoisomerase产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1208 |
Doxorubicin (Adriamycin) HClDoxorubicin (Adriamycin) HCl是一种抗生素类试剂，在肿瘤细胞中抑制DNA topoisomerase II，并诱导DNA损伤和凋亡。 |
Enhancement of apoptotic response by addition of targeted agents lapatinib and sunitinib to doxorubicin in the same device reservoir at 24 hours. P values were determined using Student’s t test for all graphs.
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| S1225 |
EtoposideEtoposide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。 |
ABT-199 synergizes strongly with lymphoma chemotherapy agents that affect MCL1 levels. Viability and CI vs Fa after 24-h exposure to etoposide alone or in combination with ABT-199 in Riva, U2932 and VavP-Bcl2/c-MYC murine tumor cells. Viability shown at 500 nM.
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| S1288 |
CamptothecinCamptothecin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。 |
CtIP and exonuclease 1 protect cells from chromosomal damage. (A) At 72 h after transfection with the indicated siRNA oligonucleotides, U2OS cells were treated with either DMSO or camptothecin (1 h, 1 μM; acute treatment) and survival was determined by colony formation. Data represent the mean±s.e.m. of five independent experiments. (B) Cell survival at low doses of camptothecin from the data shown in (A). Data represent the mean±s.e.m. of five independent experiments. (C) Cells transfected as in (A) were treated with either DMSO or camptothecin for 24 h (chronic treatment) and survival was determined by colony formation. Data represent the mean±s.e.m. of three independent experiments. (D) Metaphase spreads from cells transfected and treated as described in (A) were analysed for chromosomal aberrations. A total of 50 metaphase spreads was analysed for each sample. The percentages of metaphase spreads displaying the indicated numbers of radial chromosomes are shown. CNTL, control; DMSO, dimethyl sulphoxide; EXO1, exonuclease 1; siRNA, small interfering RNA. |
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| S1231 |
Topotecan HClTopotecan 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。 |
Cells were treated at the same concentrations as in Caspase3/7 assay for 16 hours and total cell lysates were prepared for Western blotting. GAPDH was used as a loading control.
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| S1228 |
Idarubicin HClIdarubicin 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。 |
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. |
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| S5059New |
Pixantrone MaleatePixantrone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。 |
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| S5111New |
7-Ethylcamptothecin7-Ethyl Camptothecin is an anti-cancer chemical that exhibits a strong activity against various murine tumors through Topo I (topoisomerase) inhibition. |
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| S3898New |
Hydroxy Camptothecine10-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. |
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| S1223 |
Epirubicin HClEpirubicin 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。 |
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. |
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| S2485 |
Mitoxantrone 2HClMitoxantrone 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)。 |
C18SH: C18NH2 mixed monolayer. Panel A: Cyclic voltammograms of MTX at various scan rates (1) 9 mV/s, (2) 36 mV/s, (3) 64 mV/s, (4) 100 mV/s. Panel B: Bode plots (circles) with fit (solid line) and corresponding electrical equivalent circuit (inset); 1×10-5 M MTX(Mitoxantrone) in aqueous 0.1 M LiClO4, pH = 5.6, E = 0.4 V.
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| S3035 |
Daunorubicin HClDaunorubicin HCl抑制DNA和RNA合成，无细胞试验中抑制DNA合成的Ki为0.02 μM。 |
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). |
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| S1465 |
Moxifloxacin HClMoxifloxacin HCl是一种第四代喹诺酮类抗菌剂。 |
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| S2217 |
Irinotecan HCl TrihydrateIrinotecan HCl Trihydrate通过抑制Topoisomerase 1（拓扑异构酶1）而防止DNA解链。 |
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. |
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| S4908 |
SN-38SN-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。 |
(B) HCT116 cells were treated with increasing doses of SN-38 and treated with 4 nM SN-38 for different time. Cell extracts were prepared and analyzed by Western blotting with indicated antibody. These experiments were repeated thrice. (C) HCT116 cells were transfected with 2 μg of EGFP-LC3 construct. At 8 h post-transfection, cells were treated with 4 nM of SN-38 for 48 h. And then cells were examined by confocal microscopy (magnification × 400). The percentage of cells showing accumulation of EGFP-LC3 in puncta (EGFP-LC3vac) was quantified. (D) LOVO and HCT116 cells were treated with 2 nM and 4 nM of SN-38 combined with 10 mM of 3-Methyladenine (3-MA) for 48 h respectively. Cell extracts were prepared and analyzed by Western blotting with indicated antibody. These experiments were repeated thrice. (E) Cells were treated with indicated concentrations of 3-MA and SN-38 for 48 h. Cell apoptosis was assessed by Annexin V-FITC/PI staining assay by flow cytometry. Columns, means of three determinations; bars, SD. (F) and (G) LOVO and HCT116 cells were transfected with 50 nM of NC siRNA, ATG5 siRNA respectively, and then were treated with increasing doses of SN-38 for 48 h, the knockdown effects on ATG5 were confirmed by Western blot analysis (upper panel). Cell viability was measured using CCK8 assay. Columns, means of three determinations; bars, SD.
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| S1367 |
AmonafideAmonafide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。 |
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| S1787 |
TeniposideTeniposide 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）。 |
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| S1340 |
GatifloxacinGatifloxacin是第四代喹诺酮类抗生素。 |
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%. |
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| S1222 |
Dexrazoxane HCl (ICRF-187, ADR-529)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。 |
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| S1342 |
GenisteinGenistein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。 |
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| S1940 |
LevofloxacinLevofloxacin 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。 |
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| S1393 |
PirarubicinPirarubicin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。 |
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| S1464 |
MarbofloxacinMarbofloxacin是有效的抗生素，抑制细菌DNA复制。 |
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| S2027 |
CiprofloxacinCiprofloxacin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。 |
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). |
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| S2492 |
Novobiocin SodiumNovobiocin 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，Ki分别为14.87±0.40μM, 4.77±1.12μM 和 90.50±7.50μM。 |
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). |
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| S1756 |
EnoxacinEnoxacin 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。 |
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| S1463 |
OfloxacinOfloxacin是一种合成的广谱抗菌剂。 |
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| S1509 |
NorfloxacinNorfloxacin是一种广谱抗生素。 |
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| S1327 |
Ellagic acidEllagic acid具有抗增殖和抗氧化性能。 |
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| S2328 |
Nalidixic acidNalidixic 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。 |
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| S7261 |
Beta-LapachoneBeta-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。 |
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| S4006 |
ClinafloxacinClinafloxacin 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。 |
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| S4119 |
Pefloxacin Mesylate DihydratePefloxacin 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。 |
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| S2064 |
BalofloxacinBalofloxacin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。 |
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| S4591 |
NitroxolineNitroxoline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。 |
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| S4604 |
Levofloxacin hydrateLevofloxacin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。 |
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| 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。 |
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| S7518 |
Voreloxin (SNS-595) hydrochlorideVoreloxin 是强效的广谱抗肿瘤活性的Topoisomerase II抑制剂。Phase 2。 |
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| S3603 |
Betulinic acidBetulinic 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。Phase 1/2 |
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| S3181 |
FlumequineFlumequine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。 |
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