Tubulin inhibitor 23

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Tubulin inhibitor 23 

Tubulin inhibitor 23 是一种有效的 Tubulin 抑制剂，IC50 为 4.8 µM。Tubulin inhibitor 23 诱导细胞凋亡(apoptosis)。Tubulin inhibitor 23 以剂量依赖性方式显示抗血管生成活性。Tubulin inhibitor 23 具有研究白血病的潜力。

Tubulin inhibitor 23

Tubulin inhibitor 23 Chemical Structure

CAS No. : 170488-57-0

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生物活性

Tubulin inhibitor 23 is a potent Tubulin inhibitor with an IC50 of 4.8 µM. Tubulin inhibitor 23 induces cell apoptosis. Tubulin inhibitor 23 shows antiangiogenic activity in a dose-dependent manner. Tubulin inhibitor 23 has the potential for the research of leukaemia[1].

IC50 & Target

IC50: 4.8 µM (Tubulin)[1]
体外研究
(In Vitro)

Tubulin inhibitor 23 (compound 29e) (0-100 µM) inhibits tubulin polymerisation (IC50=4.8 µM) and anti-angiogenesis (IC50=3.4 µM) in Zebrafish[1].
Tubulin inhibitor 23 (0-200 nM; 48 h) induces cell apoptosis in a concentration-dependent manner[1].
Tubulin inhibitor 23 (0-20 µM; 0-29 min) binds to the colchicine site of tubulin and inhibit the microtubule polymerisation[1].
Tubulin inhibitor 23 (0.1, 1, 10 µM; 1 h) shows anti-angiogenesis activity with low toxicity (IC50=58.6 µM) in Human umbilical vein endothelial cells (HUVECs)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: MV4-11, HL60, K562, THP-1,CCRF-CEM, Jurkat, HuT 78 cells
Concentration:
Incubation Time: 72 h
Result: Showed potent growth inhibitory activity with IC50s of 0.25, 0.18, 0.09, 0.37, 0.84, 1.22, 0.26 µM for MV4-11, HL60, K562, THP-1,CCRF-CEM, Jurkat, HuT 78 cells, respectively.

Apoptosis Analysis[1]

Cell Line: K562 cells
Concentration: 0, 50, 100, 200 nM
Incubation Time: 48 h
Result: The percentage of apoptotic cell significantly increased from 5.95% to 45.81%.

Western Blot Analysis[1]

Cell Line: K562 cells
Concentration: 0, 50, 100, 200 nM
Incubation Time: 48 h
Result: Increased the expression of cleaved caspase-3 and PARP.

体内研究
(In Vivo)

Tubulin inhibitor 23 (2, 6 µM; add into embryo water) shows antiangiogenic activity in a dose-dependent manner[1].
Tubulin inhibitor 23 (2, 6 µM; add into embryo water) suppresses the proliferation and metastasis of K562 cells in zebrafish xenografts in a dose-dependent manner[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 3hpf zebrafish embryos[1]
Dosage: 2.0, 6.0 µM
Administration: Add into embryo water
Result: Decreased the number and length of ISVs (intersegmental vessels) in a dose-dependent inhibition pattern.
Animal Model: Transgenic zebrafish (fil1:EGFP) (K562 cell xenograft)[1]
Dosage: 2, 6 µM
Administration: Add into embryo water
Result: Reduced intensities and decreased tumour area.

分子量

477.53

Formula

C26H23NO6S
CAS 号

170488-57-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Yao Y,wt al. Angiogenesis and anti-leukaemia activity of novel indole derivatives as potent colchicine binding site inhibitors. J Enzyme Inhib Med Chem. 2022 Dec;37(1):652-665.

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