Checkpoint kinase 1 (Chk1) regulates S and G2-M phase cell cycle checkpoints in response to DNA damage. CHIR124 is a cell-permeable, quinolone-based inhibitor of Chk1 (IC50 = 0.3 nM in vitro).{27078} It demonstrates high selectivity for Chk1 by displaying inhibitory values 2,000-fold higher against Chk2 (IC50 = 0.7 µM).{27078} In synergy with topoisomerase I poisons or ionizing radiation, CHIR124 can inhibit the growth of p53-mutant solid tumor cells both in vitro and in a xenograft model, potentiating tumor apoptosis.{27078,27079}
产品描述
A selective, cell-permeable, quinolone-based inhibitor of Chk1 (IC50 = 0.3 nM versus 0.7 µM for Chk1 and Chk2, respectively); inhibits p53-mutant solid tumor cell growth in synergy with topoisomerase I poisons or ionizing radiation, potentiating tumor apoptosis
