CVT-313 is a cell-permeable purine analog that acts as a potent, selective, reversible, and ATP-competitive inhibitor of Cdk2 (IC50 = 0.5 µM for Cdk2/A and Cdk2/E; 4.2 µM for Cdk1/B; 215 µM for Cdk4/D1). It inhibits other kinases only at much higher concentrations.
1. CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation: E.E. Brooks, et al.; J. Biol. Chem. 272, 29207 (1997) 2. Histone H1 phosphorylation by Cdk2 selectively modulates mouse mammary tumor virus transcription through chromatin remodeling: R.N. Bhattacharjee, et al.; Mol. Cell. Biol. 21, 5417 (2001)
See how others have used CVT-313. Click on the entry to view the PubMed entry .
PMID: # 27109354
Chen, X. et al. 2016. Nuclear phosphoproteomics analysis reveals that CDK1/2 are involved in EGF-regulated constitutive pre-mRNA splicing in MDA-MB-468 cells. Journal of proteomics.
PMID: # 25149358
Zalzali, H. et al. 2015. CDK2 transcriptional repression is an essential effector in p53-dependent cellular senescence-implications for therapeutic intervention. Molecular cancer research : MCR. 13: 29-40.
PMID: # 26606677
Paiva, C. et al. 2015. Cyclin-Dependent Kinase Inhibitor P1446A Induces Apoptosis in a JNK/p38 MAPK-Dependent Manner in Chronic Lymphocytic Leukemia B-Cells. PloS one. 10: e0143685.
PMID: # 22548705
Zalzali, H. et al. 2012. Temporally distinct roles for tumor suppressor pathways in cell cycle arrest and cellular senescence in Cyclin D1-driven tumor. Molecular cancer. 11: 28.
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