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CAS No.: 199986-75-9

CVT-313 Catalog No. CSN16417

Synonyms: Cdk2 Inhibitor III;NG 26;Cyclin-dependent kinase 2 Inhibitor III

CVT-313 is a potent, selective, ATP-competitive and reversible inhibitor of CDK2 with IC50 of 0.5 μM for Cdk2/A and Cdk2/E; 4.2 μM for Cdk1/B; 215 μM for Cdk4/D1.

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400-920-2911

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技术信息

生物活性

描述Cell cycle progression in mammalian cells is regulated by a family of cyclin-dependent protein kinases (CDKs). CDK2 is a serine/threonine kinase whose activity is essential for the G₁ to S transition during cell division. CVT-313 is a potent, selective and ATP-competitive CDK2 inhibitor with an IC₅₀ of 0.5 μM and a K_i of 95 nM, and has no effect on other, nonrelated ATP-dependent serine/threonine kinases. The growth of mouse, rat, and human cells in culture was inhibited by CVT-313 with the IC₅₀ for growth arrest ranging from 1.25 to 20 μM. When nonsynchronized MRC-5 cells were treated with CVT-313 (6.25 μM) for 36 h, most of these cells had a 2 N DNA content, consistent with a G₁/S arrest. After removal of CVT313, cells reentered the cell cycle suggesting that the inhibition of cell proliferation was reversible. Moreover, if CVT-313 (6.25 mM) was added at 0, 4, or 8 h after serum stimulation, Rb hyperphosphorylation was inhibited. A brief intraluminal exposure of CVT-313 (1.25 mg/kg for 15 min) to a denuded rat carotid artery resulted in more than 80% inhibition of neointima formation^[3].
参考文献

[1] Graub R, Lancero H, et al. Cell cycle-dependent phosphorylation of human CDC5 regulates RNA processing. Cell Cycle. 2008 Jun 15;7(12):1795-803. Epub 2008 Jun 25.
[2] Brooks EE, Gray NS, et al. CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation. J Biol Chem. 1997 Nov 14;272(46):29207-11.
[3] Brooks EE, Gray NS, Joly A, Kerwar SS, et al. CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation. J Biol Chem. 1997 Nov 14;272(46):29207-11.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4970 mL
- 12.4852 mL
- 24.9704 mL
- 5 mM
- 0.4994 mL
- 2.4970 mL
- 4.9941 mL
- 10 mM
- 0.2497 mL
- 1.2485 mL
- 2.4970 mL

技术信息

CAS号

199986-75-9

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H28N6O3

运输

蓝冰

分子量

400.47

别名

Cdk2 Inhibitor III;NG 26;Cyclin-dependent kinase 2 Inhibitor III

溶解度

DMSO	240.0 mg/mL (599.3 mM)
Water	insoluble

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