Cat. No. | Product Name | Target | Signaling Pathways |
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T63360 | DNA topoisomerase II inhibitor 1 | ||
DNA topoisomerase II inhibitor 1 是 DNA 拓扑异构酶 II 的有效抑制剂,能够将细胞周期停滞在亚 G1 期,并诱导细胞凋亡 (apoptosis) ,具有抗增值作用。 | |||
T36968 |
ARN-21934
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Topoisomerase | DNA Damage/DNA Repair |
ARN-21934 是高选择性的人拓扑异构酶 II α 抑制剂,具有血脑屏障通透性。依托泊苷抑制 DNA 松弛的IC50为120 μM,ARN-21934 抑制 DNA 松弛的IC50为 2 μM。ARN-21934具有良好的体内药代动力学特性。 | |||
T61054 | Type II topoisomerase inhibitor 1 | ||
Type II topoisomerase inhibitor 1 可用于抗菌领域。Type II topoisomerase inhibitor 1 是大肠杆菌DNA 旋转酶的选择性抑制剂,IC50值为 1.7 nM,并能与 Asp73 残基形成氢键。Type II topoisomerase inhibitor 1 抑制拓扑异构酶 IV 的活性,IC50值为 0.98 μM。 | |||
T18317 |
MCC-Modified Daunorubicinol
|
Others | Others |
Daunorubicinol, a potent antitumor drug-linker conjugate for antibody-drug conjugate (ADC) applications, utilizes Aur0101 (DNA Topoisomerase II inhibitor) connected through the ADC linker[1]. | |||
T61283 |
Topoisomerase II inhibitor 3
|
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Topoisomerase II inhibitor 3 (Compound 6 h) is an acridone derivative that acts as a Type II DNA topoisomerase (topo II) inhibitor. It specifically inhibits the topo IIα/β subtypes, with an IC50 value of 0.17 μM for topo IIα and 0.23 μM for topo IIβ. This compound elicits significant DNA damage and induces apoptosis by triggering the loss of mitochondrial membrane potential [1]. | |||
T61017 | Topoisomerase II inhibitor 6 | ||
Topoisomerase II inhibitor 6 (Compound 5) 是色胺酮的衍生物。它是一种有效的拓扑异构酶的选择性抑制剂。Topoisomerase II inhibitor 6 在 G2 期阻断 CCRF-CEM 的细胞周期并诱导 DNA 双链断裂。Topoisomerase II inhibitor 6 对不同的肿瘤细胞系具有抗增殖活性,在癌症疾病研究中具有潜力。 | |||
T61351 |
Pixantrone hydrochloride
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Pixantrone (BBR 2778 (free base)) hydrochloride is a mitoxantrone analog compound that acts as a topoisomerase II inhibitor and DNA intercalator. It displays anti-tumor activity [1] [2]. | |||
T61045 | Topoisomerase I/II inhibitor 2 | ||
Topoisomerase I/II inhibitor 2 (compound 1a) 可显著抑制小鼠模型中的异种移植肿瘤的生长,可用于肝癌治疗。Topoisomerase I/II inhibitor 2 是一种DNA 拓扑异构酶 I/II 的双重抑制剂。Topoisomerase I/II inhibitor 2 是有效的拓扑异构酶抑制剂,对LM9 细胞和Huh7 细胞的 IC50值分别为 6.83 μM 和9.82 μM 。 | |||
T79539 |
Topoisomerase II inhibitor 16
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Topoisomerase | DNA Damage/DNA Repair |
TopoisomeraseII inhibitor 16(化合物CT3)是一个选择性的、口服活性的、能够穿透血脑屏障的,并对锥虫拓扑异构酶 II(trypanosomaltopoisomeraseII)产生不可逆抑制的化合物,能够稳定DNA双螺旋与酶之间的复合物。该抑制剂在恰加斯病的研究中显示出潜在应用价值。 | |||
T61431 | Topoisomerase IIα-IN-4 | ||
Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive inhibitor of human DNA topoisomerase II, specifically inhibiting TopoIIα with an IC50 value of 3.8 μM and TopoIIβ with an IC50 value of 10.1 μM. It demonstrates significant efficacy in inducing apoptosis and arresting the cell cycle in HepG2 cells. Moreover, Topoisomerase IIα-IN-4 exhibits robust antitumor effects against various human cancer cell lines, making it a valuable compound for cancer research [1]. | |||
T81745 |
MSN8C
|
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MSN8C为曼索酮E的类似物,作为一种新型人类DNA拓扑异构酶II催化抑制剂,能够诱导癌细胞凋亡,并在体外显著抑制肿瘤细胞增殖。 | |||
T61481 |
TP0480066
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TP0480066, a selective topoisomerase II inhibitor, demonstrates excellent inhibitory activity against DNA gyrase (IC50 = 1.10 nM) and topo IV (IC50 = 62.89 nM). This compound exhibits potent efficacy against multiple bacterial species, including drug-resistant strains. Moreover, TP0480066 displays significant inhibitory activity against N. gonorrhoeae, making it suitable for research on gonorrhea [1] [2]. | |||
T36695 |
TAS-103
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TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used for cancer research. TAS-103 is a dual inhibitor of DNA topoisomerase I/II. TAS-103 (0.1-10 μM) is active on CCRF-CEM cells, with an IC50 value of 5 nM. TAS-103 (0.1 μM) significantly increases levels of topo IIα FITC immunofluorescence in individual CCRF-CEM cells[1]. TAS-103 (0.01-1 μM) is highly cytotoxic to Lewis lung carcinoma (LLC) cells, and Liposomal TAS-103 is almost as active as free TAS-103[2]. TAS-103 inhibits the viability ... | |||
T73700 |
Daunorubicin citrate
|
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Daunorubicin citrate(Daunomycin citrate)作为一种拓扑异构酶 II(topoisomerase II)抑制剂,展现出有效的抗肿瘤活性,通过抑制 DNA 和 RNA 合成(DNA and RNA synthesis)发挥作用。作为一种细胞毒性药物,Daunorubicin citrate 能够抑制癌细胞活性,并诱导细胞凋亡(apoptosis)和坏死(necrosis),属于蒽环类抗生素范畴。该化合物广泛应用于包括白血病、非霍奇金淋巴瘤、尤文氏肉瘤、维尔姆斯氏瘤在内的多种癌症和感染研究领域。 | |||
T75303 |
Suramin
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Suramin为一种可逆的,竞争性PTPases抑制剂,有效抑制sirtuins:SirT1(IC50=297 nM),SirT2(IC50=1.15 μM),SirT5(IC50=22 μM)。同时,Suramin作为DNAtopoisomeraseII(IC50=5 μM)的竞争性逆转录酶抑制剂,以及SARS-CoV-2 RdRp有效抑制剂。此外,Suramin还能有效抑制IP5K,具有抗寄生虫、抗肿瘤及抗血管生成的作用。 | |||
T36199 |
AZD 1152 (hydrochloride)
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AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50= 0.36 nM).1AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis.2,3AZD 1152 inhibits tumor xenograft growthin vivo.4,5 1.Mortlock, A.A., Foote, K.M., Heron, N.M., et al.Discovery, synthesis, and in vivo activity of a new class of p... |