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Cat. No. | Product Name | Target | Signaling Pathways |
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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]. | |||
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。 | |||
T28017 |
Merbarone
RLBN-1001,NSC-336628,RLBN1001,NSC336628 |
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Merbarone is a Type II DNA topoisomerase inhibitor. Merbarone inhibits the catalytic activity of human topoisomerase IIalpha by blocking DNA cleavage. Merbarone induces activation of caspase-activated DNase and excision of chromosomal DNA loops from the n | |||
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 ... | |||
T68458 | Fostriecin (free base) | ||
Fostriecin (free base) is an inhibitor of the serine/threonine protein phosphatases 2A (PP2A) and 4 (PP4) (IC50s = 3.2 and 3 nM, respectively). It less effectively inhibits topoisomerase II and PP1 (IC50s = 40 and 131 μM, respectively) and does not inhibit PP2B. Through its effects on protein phosphatases, fostriecin increases the level of histone H3 phosphorylation and may alter epigenetic regulation of cell proliferation. On a related note, fostriecin was first identified as an antitumor antib... | |||
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... |
Cat. No. | Product Name | Target | Signaling Pathways |
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TN2915 |
3-Acetoxy-27-hydroxy-20(29)-lupen
3-Acetoxy-27-hydroxy-20(29)-lupen-28-oic acid methyl ester |
Others | Others |
3-Acetoxy-27-hydroxy-20(29)-lupen is an acetyl ester form of 3α, 27-Dihydroxylupen-20(29)-en-28-oic acid methyl ester, which is a topoisomerase II inhibitor. |