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Kenpaullone
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Kenpaullone图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议

产品介绍
Kenpaullon 是一种有效的 CDK1/cyclin B 和 GSK-3β 抑制剂,IC50 为 0.4 μM 和 23 nM,还抑制 CDK2/cyclin A、CDK2/cyclin E 和 CDK5/p25,IC50 分别为 0.68 μM、7.5 μM、分别为 0.85 μM。 Kenpaullon 是一种 KLF4 的小分子抑制剂,可在体外减少乳腺癌干细胞的自我更新和细胞运动。

Kinase experiment:

The kinase assay is run for 10 min at 30℃ with 1 mg/mL histone H1, in the presence of 15 μM [g-32P]ATP (3000 Ci/μmol; 1 mCi/mL) in a final volume of 30 ml. Purification and assays or inhibition of other kinases are performed. In kinetic experiments, the histone H1 concentration is lowered to 3.5 mg/mL; the ATP concentration ranged from 50 to 400 μM, and the kenpaullone concentration ranges from 1 to 4 μM.

产品描述

Kenpaullone is a potent inhibitor of CDK1/cyclin B and GSK-3β, with IC50s of 0.4 μM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC50s of 0.68 μM, 7.5 μM, 0.85 μM, respectively.

Kenpaullone shows much less effect on c-src (IC50, 15 μM), casein kinase 2 (IC50, 20 μM), erk 1 (IC50, 20 μM), and erk 2 (IC50, 9 μM). Kenpaullone acts by competitive inhibition of ATP binding, and the apparent Ki is 2.5 μM. Kenpaullone can inhibit the growth of tumor cells in culture (mean GI50, 43 μM) and causes altered cell cycle progression most clearly revealed under conditions of recovery from serum starvation[1]. Kenpaullone demonstrates a wide range of biological utility, extending from maintenance of pancreatic β cell survival and proliferation to the induction of apoptosis in cancer cells[2].

References:
[1]. Zaharevitz DW, et al. Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases. Cancer Res. 1999 Jun 1;59(11):2566-9.
[2]. Lyssiotis CA, et al. Reprogramming of murine fibroblasts to induced pluripotent stem cells with chemical complementation of Klf4. Proc Natl Acad Sci U S A. 2009 Jun 2;106(22):8912-7.