Research Area
Product Type
United States ( Change Country )
CHIR-124 Chemical Structure
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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]
References on CHIR-124
- [1] Cell Cycle. 2009 Apr 15;8(8):1196-205.
- [2] Clin Cancer Res. 2007 Jan 15;13(2 Pt 1):591-602.
Chemical Information
| Molecular Weight (WM): | 419.91 |
|---|---|
| Formula: | C23H22ClN5O |
| CAS No.: | 405168-58-3 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
Research Area
Notes:
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