• Catalog Number:

  E1KS2683

• Amount:

  2mg1​ PHYSICAL AND CHEMICAL PROPERTIES

2​ Biological Activity CHIR-124 is a novel and potent chk1 inhibitor with an IC50 of 0.3 nM. Chk1 kinase is a critical regulator of both the S and G2/M phase cell cycle checkpoints in response to DNA damage. It has been shown that inhibitors of chk1 can selectively sensitize tumor cells with mutant p53 to genotoxic agents. CHIR-124 is a quinolone-based small molecule that is structurally unrelated to other known inhibitors of chk1. CHIR-124 interacts synergistically with camptothecin in causing growth inhibition in MDA-MB-435 cells as determined by isobologram analysis. In HCT116 human colon carcinoma cells, CHIR-124 increased the effect of SN-38, an active metabolite of irinotecan, in a sequence-dependent manner, with the highest induction of mitotic catastrophe and apoptosis seen when CHIR-124 was given sequentially after SN-38 pretreatment. More importantly, the enhancement of cell death by CHIR-124 was markedly increased in isogenic p53-null and p21-null HCT116 cells. [1][2] 3​ References: Radiosensitization by Chir-124, a selective CHK1 inhibitor: effects of p53 and cell cycle checkpoints. Tao Y et al. Cell Cycle. 2009 Apr 15;8(8):1196-205. CHIR 124, a novel and potent inhibitor of chk1, potentiates the anti-tumor activity of topoisomerase I poisons in vitro and in vivo. Tse AN et al. Clin Cancer Res. 2007 Jan 15;13(2 Pt 1):591-602. The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.