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Search Results for " topoisomerase iiα "

23

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T36968	ARN-21934	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。
T67899	Topoisomerase II inhibitor 13	Topoisomerase	DNA Damage/DNA Repair
	Topoisomerase II inhibitor 13抑制拓扑异构酶II (Topo II)，对HL-60衍生的HL-60/MX2癌细胞具有较强的抗Topo II 毒性的抗增殖活性。
T62224	Topoisomerase IIα-IN-2
	Topoisomerase IIα-IN-2 (compound 5) 是一种 DNA 结合配体 (DNA-binding ligands)，也是一种拓扑异构酶 TopoIIα的有效抑制剂。Topoisomerase IIα-IN-2 对人癌症细胞株表现出较高的抗增殖活作用。Topoisomerase IIα-IN-2 能够将癌细胞的细胞周期停滞在 G2/M 期，明显诱导 DNA 损伤。
T62223	Topoisomerase IIα-IN-1
	Topoisomerase IIα-IN-1 (compound 2) 是一种 DNA 结合配体 (DNA-binding ligands)，也是一种拓扑异构酶TopoIIα的有效抑制剂。Topoisomerase IIα-IN-1 对人类癌症细胞株表现出较好的抗增殖作用。
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].
T63594	Topoisomerase IIα-IN-3
	Topoisomerase IIα-IN-3 是 DNA 插入型 topoisomerase-Iiα 抑制剂，能够将细胞周期阻滞在 G0/G1 期，并诱导细胞凋亡 (apoptosis)。
T60781	Topoisomerase II inhibitor 8
	Topoisomerase II inhibitor 8 (化合物 22) 显示出良好的抗增殖活性，并将细胞周期阻滞在 G2/M 期。Topoisomerase II inhibitor 8是拓扑异构酶 II 的有效抑制剂 (IC 50 = 0.52 μM)。
T63304	Topoisomerase II inhibitor 9
	Topoisomerase II inhibitor 9 是 Topo II 抑制剂 (IC50: 0.97 μM)，也是 DNA 嵌入剂 (IC50: 43.51 μM)，能够在 G2/M 期阻滞 Hep G‐2 细胞周期，诱导细胞凋亡 (apoptosis)。
T79506	Topoisomerase II inhibitor 15	Topoisomerase	DNA Damage/DNA Repair
	TopoisomeraseII inhibitor 15 (compound 2g) 为 TopoisomeraseII 的一种抑制剂，能有效诱导细胞凋亡 (apoptotic) 并对头颈部肿瘤展示出较高选择性。
T64164	Topoisomerase II inhibitor 11
	Topoisomerase II inhibitor 11 (compound 3d) 是一种拓扑异构酶 II (Topoisomerase II) 的有效抑制剂 (IC50: 2.89 μM)。Topoisomerase II inhibitor 11 对肾癌 A498 细胞有 92.46% 的抑制效果 (IC50: 3.5 μM)。Topoisomerase II inhibitor 11 能够将细胞周期阻滞在 G2/M 期，抑制细胞增殖并具有凋亡活性。
T72157	Topoisomerase II inhibitor 7
	TopoisomeraseII inhibitor 7 (化合物 3a) 作为一种高效的拓扑异构酶IIα亚型抑制剂，展现出3.19 μM的IC50值。其能够诱导细胞周期阻滞与凋亡。
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。
T64047	Topoisomerase II inhibitor 10
	Topoisomerase II inhibitor 10 是拓扑异构酶II (topoisomerase II) 的有效抑制剂 (IC50: 7.45 μM)。Topoisomerase II inhibitor 10 对 HepG-2、MCF-7 和 HCT-116 细胞表现出良好的抗增殖作用。Topoisomerase II inhibitor 10 能够将 HepG-2 细胞的细胞周期阻滞在 G2-M 期，并诱导其凋亡 (apoptosis)。
T61283	Topoisomerase II inhibitor 3
	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].
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。
T63068	Topoisomerase II inhibitor 5
	Topoisomerase II inhibitor 5 (Compound E24) 是一种 DNAtopoisomerase II 抑制剂，具有抗癌作用。
T79539	Topoisomerase II inhibitor 16	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。
T62887	Topoisomerase II inhibitor 4
	Topoisomerase II inhibitor 4 (compound E17) 是一种拓扑异构酶 II (Topoisomerase II) 的有效抑制剂。Topoisomerase II inhibitor 4 具有抗肿瘤效果，能够将阻滞细胞周期于 G2/M 期，抑制癌细胞增殖并表现出细胞毒性。
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 。
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。
T63526	Topoisomerase I/II inhibitor 4
	Topoisomerase I/II inhibitor 4 是有效的拓扑异构酶 I(Topo I) 和 II(Topo II) 双重抑制剂，对细胞增殖、侵袭和迁移，诱导细胞凋亡 (apoptosis) 具有抑制作用，能够用于研究肝癌。
T61990	Topoisomerase I/II inhibitor 3
	Topoisomerase I/II inhibitor 3 (化合物7) 是拓扑异构酶 I (Topo I)和 II (Topo II)的有效双抑制剂。通过抑制 PI3K/Akt/mTOR 信号通路，Topoisomerase I/II inhibitor 3抑制细胞增殖、侵袭和迁移，诱导细胞凋亡(apoptosis)。Topoisomerase I/II inhibitor 3 在肝癌中具有研究价值。
T36695	TAS-103
	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 ...

化合物

Cat.No: T36968

Target: Topoisomerase

Topoisomerase II inhibitor 13

Cat.No: T67899

Target: Topoisomerase

Topoisomerase IIα-IN-2

Cat.No: T62224

Topoisomerase IIα-IN-1

Cat.No: T62223

Topoisomerase IIα-IN-4

Cat.No: T61431

Topoisomerase IIα-IN-3

Cat.No: T63594

Topoisomerase II inhibitor 8

Cat.No: T60781

Topoisomerase II inhibitor 9

Cat.No: T63304

Topoisomerase II inhibitor 15

Cat.No: T79506

Target: Topoisomerase

Topoisomerase II inhibitor 11

Cat.No: T64164

Topoisomerase II inhibitor 7

Cat.No: T72157

Topoisomerase II inhibitor 6

Cat.No: T61017

Topoisomerase II inhibitor 10

Cat.No: T64047

Topoisomerase II inhibitor 3

Cat.No: T61283

Type II topoisomerase inhibitor 1

Cat.No: T61054

Topoisomerase II inhibitor 5

Cat.No: T63068

Topoisomerase II inhibitor 16

Cat.No: T79539

Target: Topoisomerase

Topoisomerase II inhibitor 4

Cat.No: T62887

Topoisomerase I/II inhibitor 2

Cat.No: T61045

DNA topoisomerase II inhibitor 1

Cat.No: T63360

Topoisomerase I/II inhibitor 4

Cat.No: T63526

Topoisomerase I/II inhibitor 3

Cat.No: T61990

Cat.No: T36695

Cat. No.	Product Name	Target	Signaling Pathways
TN5133	3',5,5',7-Tetrahydroxy-4',6-dimethoxyflavone	HIV Protease; Topoisomerase	DNA Damage/DNA Repair; Microbiology/Virology; Proteases/Proteasome
	5,7,3',5'-tetrahydroxy-6,4'-dimethoxyflavone exhibits anti-HIV-1 activity in the anti-syncytium assay using (∆Tat/rev)MC99 virus and 1A2 cell line system, it shows considerably activity against HIV-1 reverse transcriptase. It exhibits cytotoxic activity against P-388 cell lines, it can inhibit DNA topoisomerase IIα activity, which may be responsible for the observed cytotoxicity.
T79978	6,6′-Dihydroxythiobinupharidine
	6,6′-Dihydroxythiobinupharidine 作为一种抑制剂，主要针对半胱氨酸蛋白酶(cysteine proteases)。研究表明，该化合物能显著促进人拓扑异构酶IIα(topoisomeraseIIα)和IIβ(topoisomeraseIIβ)介导的DNA裂解，分别提高了8倍和3倍的效率。

天然产物

3',5,5',7-Tetrahydroxy-4',6-dimethoxyflavone

Cat.No: TN5133

Target: HIV Protease, Topoisomerase

6,6′-Dihydroxythiobinupharidine

Cat.No: T79978

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