PV-1019 (NSC 744039) is a potent, selective Chk2 inhibitor with an IC50 value of 24 nM. PV-1019 inhibits the Topotecan -induced Chk2 autophosphorylation. PV-1019 inhibits IR-induced apoptosis.
PV-1019 (NSC 744039; 0.1-100 μM; 48 h) has antiproliferative effect in human tumor cells[1].PV-1019 inhibits Chk2 autophosphorylation and histone H1 phosphorylation with an IC50 value of 138 nM[1].PV-1019 (1-50 μM; 1 h; OVCAR-5 cells) inhibits the Topotecan-induced Chk2 autophosphorylation with an IC50 value of 2.8 μM[1].PV-1019 (1 μM; 16 h) abrogates IR-induced apoptosis in mouse tmocytes[1].
References:
[1]. Jobson AG, et, al. Cellular inhibition of checkpoint kinase 2 (Chk2) and potentiation of camptothecins and radiation by the novel Chk2 inhibitor PV1019 [7-nitro-1H-indole-2-carboxylic acid {4-[1-(guanidinodrazone)-etl]-phenyl}-amide]. J Pharmacol Exp Ther. 2009 Dec;331(3):816-26.