Chk2 Inhibitor, PV1019

A cell-permeable nitroindolo-guanidinohydrazone compound that acts as a potent, ATP-competitive, and highly selective Chk2 inhibitor (IC₅₀ = 138 and 570 nM against the phosphorylation of histone H1 by Chk2 in the presence of 10 µM and 1 mM of ATP, respectively), while exhibiting much reduced or no activity against a panel of 52 other cellular kinases, including Chk1 (IC₅₀ = 15.73 and 55 µM against substrate phosphorylation and Chk1 autophosphorylation with 10 µM ATP). Shown to effectively suppress radiation-induced phosphorylation of Chk2 (on Ser⁵¹⁶) and its downstream substrate Cdc25c (on Ser²¹⁶) in MCF7 cultures (IC₅₀<10 µM) and reduce the sensitivity of wild-type murine thymocytes to radiation-induced apoptosis to the level seen in Chk2^-/- cultures.

Packaged under inert gas

Following reconstitution, aliqout and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Jobson, A.G., et al. 2009. J. Pharmacol. Exp. Ther.331, 816.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)