Tubulin inhibitor 23

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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].

上海金畔生物科技有限公司 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].

上海金畔生物科技有限公司 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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