NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2), exhibiting an IC50 of 200 nM in a cell-free assay. This compound selectively inhibits Chk2 while displaying lesser activity against Brk, c-Met, IGFR, and LCK at higher concentrations. NSC 109555 disrupts Chk2 autophosphorylation and histone H1 phosphorylation with an IC50 of 240 nM. Its biological activity includes inducing autophagy and inhibiting growth in L1210 leukemia cells, as well as enhancing gemcitabine-induced cytotoxicity and increasing reactive oxygen species levels in various pancreatic cancer cell lines.
NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2), exhibiting an IC50 of 200 nM in a cell-free assay. This compound selectively inhibits Chk2 while displaying lesser activity against Brk, c-Met, IGFR, and LCK at higher concentrations. NSC 109555 disrupts Chk2 autophosphorylation and histone H1 phosphorylation with an IC50 of 240 nM. Its biological activity includes inducing autophagy and inhibiting growth in L1210 leukemia cells, as well as enhancing gemcitabine-induced cytotoxicity and increasing reactive oxygen species levels in various pancreatic cancer cell lines.
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