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SB218078 C화학적 특성, 용도, 생산
개요
SB 218078 is an inhibitor of checkpoint kinase 1 (Chk1) that blocks phosphorylation of cdc25 with an IC50 value of 15 nM. It less potently inhibits cdc2 and PKC (IC50s = 250 and 1,000 nM, respectively) and causes 85% inhibition of PKD1 at 1 μM. SB 218078 releases G2 cell cycle arrest induced by γ-irradiation or the topoisomerase I inhibitor topotecan . In this way, SB 218078 enhances the cytotoxicity of DNA-damaging compounds.
용도
SB 218078 is a selective inhibitor of Chk1.
생물학적 활성
Inhibitor of checkpoint kinase 1 (Chk1) that displays selectivity over other protein kinases (IC 50 values are 15, 250 and 1000 nM for Chk1, cdc2 and PKC respectively). Abrogates G 2 cell cycle arrest caused by γ -irradiation and topoisomerase I inhibition. Potentiates cytotoxicity of DNA-damaging drugs, enhancing the efficacy of some chemotherapeutics.