Purvalanol a

Description

Purvalanol A (212844-53-6) is a cyclin-dependent kinase inhibitor. IC50s= 4, 70, 35, 75 and 850 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk5/p35 and cdk4/cyclin D1 and respectively.1?Reversibly arrests synchronized cells in G1 and G2 phase.2?Induces ER stress-mediated apoptosis and autophagy in colon cancer cells.3?Suppresses Src-mediated transformation by inhibiting both CDKs and c-Src.4?In cells transformed with MYC, purvalanol A rapidly down-regulates survivin expression and induces MYC-dependent apoptosis.5?Cell permeable.

The Uses of Purvalanol a

Purvalanol A acts as a potent, cell-permeable CDK inhibitor used in the treatment of cell proliferative disorders. Anti-cancer.

What are the applications of Application

Purvalanol A is a selective inhibitor of cyclin-dependent kinases

Definition

ChEBI: Purvalanol A is a purvalanol.

Biological Activity

Cyclin-dependent kinase inhibitor. IC 50 values are 4, 70, 35, 850 and 75 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively. Reversibly arrests synchronised cells in G1 and G2, and inhibits cell proliferation and cell death.

Storage

Store at +4°C

References

1) Gray?et al.?(1998),?Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors; Science,?281?533 2) Villerbu?et al.?(2002),?Cellular effects of purvalanol A: a specific inhibitor of cyclin-dependent kinase activities; Int. J. Cancer,?97?761 3) Coker-Gurkan?et al.?(2015),?Purvalanol induces endoplasmic reticulum stress-mediated apoptosis and autophagy in a time dependent manner in HCT116 colon cancer cells; Oncol. Rep.,?33?2761 4) Hikita?et al.?(2010),?Purvalanol A, a CDK inhibitor, effectively suppresses Src-mediated transformation by inhibiting both CDKs and c-Src; Genes Cells,?15?1051 5) Goga?et al.?(2007),?Inhibition of CDK1 as a potential therapy for tumors over-expressing MYC; Nat. Med.,?13?820