Inhibitor of checkpoint kinase 1 (Chk1) that displays selectivity over other protein kinases (IC50
values are 15, 250 and 1000 nM for Chk1, cdc2 and PKC respectively). Abrogates G2
cell cycle arrest caused by γ
-irradiation and topoisomerase I inhibition. Potentiates cytotoxicity of DNA-damaging drugs, enhancing the efficacy of some chemotherapeutics.
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An indolocarbazole inhibitor of human checkpoint kinase (Chk1) abrogates cell cycle arrest caused by DNA damage.
Jackson et al.
Cancer Res., 2000;60:566
G2 checkpoint abrogators as anticancer drugs.
Mol.Cancer Ther., 2004;3:513
Checkpoint kinase 1-mediated phosphorylation of cdc25C and bad proteins are involved in antitumor effects of loratadine-induced G2/M phase cell-cycle arrest and apoptosis.
Chen et al.
The citations listed below are publications that use Tocris products. Selected citations for SB 218078 include:
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