CHM-1(Synonyms: NSC656158)

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。

CHM-1 (Synonyms: NSC656158)

CHM-1 是一种微管失稳剂,可抑制微管蛋白聚合。CHM-1 是一种有效且选择性的抗人肝癌有丝分裂的抗肿瘤活性。CHM-1 通过激活 Cdc2 激酶活性诱导人肝癌细胞 G2-M 期阻滞,从而诱导细胞生长抑制和凋亡。

CHM-1(Synonyms: NSC656158)

CHM-1 Chemical Structure

CAS No. : 154554-41-3

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生物活性

CHM-1, a microtubule-destabilizing agent, inhibits tubulin polymerization. CHM-1 is a potent and selective antimitotic antitumor activity against human hepatocellular carcinoma. CHM-1 induces growth inhibition and apoptosis via G2-M phase arrest in human hepatocellular carcinoma cells by activation of Cdc2 kinase activity[1][2][3].

IC50 & Target

IC50: 0.75 μM (HA22T)[1]

体外研究
(In Vitro)

CHM-1 (0-100μM; 24 hours) induces significant concentration-dependent growth inhibition in HA22T, Hep3B, and HepG2 cells, with the most potent effects observed in HA22T cells (IC50 = 0.75 μM)[1].
CHM-1 (0-10 μM; 24 hours) significantly increases the binding of cyclin B1 to Cdc2 in HA22T cells[1].

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

Cell Viability Assay[1]

Cell Line: HA22T, Hep3B, and HepG2 cells
Concentration: 0-100 μM
Incubation Time: 24 hours
Result: Induced G2-M arrest of the cell cycle followed by apoptosis.

Western Blot Analysis[1]

Cell Line: HA22T cells
Concentration: 0-10 μM
Incubation Time: 24 hours
Result: Induced change in expressed and phosphorylated status of G2-M regulators in human hepatocellular carcinoma cells.

体内研究
(In Vivo)

CHM-1 (10 mg/kg; I.p.) induces a dose-dependent inhibition of HA22T tumor growth[1].

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

Animal Model: Male severe combined immunodeficient mice (HA22T)[1]
Dosage: 10 mg/kg
Administration: I.p.
Result: Induced a dose-dependent inhibition of HA22T tumor growth.

分子量

283.25

Formula

C16H10FNO3

CAS 号

154554-41-3

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]. Wang SW, et al. CHM-1, a novel synthetic quinolone with potent and selective antimitotic antitumor activity against human hepatocellular carcinoma in vitro and in vivo. Mol Cancer Ther. 2008 Feb;7(2):350-60.

    [2]. Liu CW, et al. CHM-1, a novel microtubule-destabilizing agent exhibits antitumor activity via inducing the expression of SIRT2 in human breast cancer cells. Chem Biol Interact. 2018 Jun 1;289:98-108.

    [3]. Tsai AC, et al. CHM-1, a new vascular targeting agent, induces apoptosis of human umbilical vein endothelial cells via p53-mediated death receptor 5 up-regulation. J Biol Chem. 2010 Feb 19;285(8):5497-506.

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