PV1019 (NSC744039) is a potent, ATP-competitive and highly selective Chk2 inhibitor with IC50 of 138 nM.
PV1019 displays much reduced or no activity against a panel of 52 other cellular kinases, including Chk1.
PV1019 inhibits Chk2-mediated phosphorylation of Cdc25C (IC50=260 nM), and nd HDMX degradation in response to DNA damage.
PV1019 protects normal mouse thymocytes against ionizing radiation-induced apoptosis.
