CVT-313

"目录号: HY-15339

Cell Cycle/DNA Damage-

CVT-313 是一种有效的ATP-竞争性的选择性CDK2抑制剂，IC50为 0.5 μM。

CDK

相关产品

LY2835219-Palbociclib-THZ1-Dinaciclib-LEE011-Roscovitine-Ro-3306-Flavopiridol-THZ2-1-NM-PP1-BIO-AZD-5438-BS-181-SNS-032-LY2857785-

生物活性

Description

CVT-313 is a potent, selective, reversible, and ATP-competitive inhibitor ofCDK2wirhIC50of 0.5 μM.

IC50& Target

IC50: 0.5 μM (CDK2), 4.2 μM (CDK1), 215 μM (CDK4)[1]

In Vitro

CVT-313 has been shown to inhibit other kinases, but at much higher IC50values, i.e., CDK1 (IC50=4.2 μM), CDK4 D1 (IC50=215 μM), and MAPK/PKA/PKC (IC50>1.25 mM), compared to CDK2 (IC50=0.5 μM). CVT-313 has been shown to have profound effects on cell proliferation at concentrations of 5-20 μM[1]. CVT-313 is a potent CDK2 inhibitor, which is identified from a purine analog library with an IC50of 0.5 μM in vitro. Inhibition is competitive with respect to ATP (Ki=95 nM), and selective CVT-313 has no effect on other, nonrelated ATP-dependent serine/threonine kinases. When added to CDK1 or CDK4, a 8.5- and 430-fold higher concentration of CVT-313 is required for half-maximal inhibition of the enzyme activity. Using normal and tumor human/murine cell lines, the effects of CVT-313 on cell proliferation is measured. The IC50for growth inhibition ranged from 1.25 to 20 μM[2].

References

[1].Graub R, et al. Cell cycle-dependent phosphorylation of human CDC5 regulates RNA processing. Cell Cycle. 2008 Jun 15;7(12):1795-803.

[2].Brooks EE, 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.