Molecular structure of CHIR-124, CAS Number: 405168-58-3
CHIR-124 (CAS 405168-58-3)
See product citations (2)
Alternate Names:
(S)-3-(1H-benzo[d]imidazol-2-yl)-6-chloro-4-(quinuclidin-3-ylamino)quinolin-2(1H)-one
Application:
CHIR-124 is a potent inhibitor of Chk1
CAS Number:
405168-58-3
Molecular Weight:
419.91
Molecular Formula:
C23H22ClN5O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
CHIR-124 is a potent inhibitor of checkpoint kinase 1 (Chk1) with an IC50 value of 0.3 nM. Chk1 is an ATP-dependent serine-threonine kinase that is very important to the checkpoint monitoring system of DNA replication. CHIR-124 promotes growth inhibition in many cancer cell lines by interacting with topoisomerase poisons.
CHIR-124 (CAS 405168-58-3) References
- CHIR-124, a novel potent inhibitor of Chk1, potentiates the cytotoxicity of topoisomerase I poisons in vitro and in vivo. | Tse, AN., et al. 2007. Clin Cancer Res. 13: 591-602. PMID: 17255282
- The intra-S-phase checkpoint affects both DNA replication initiation and elongation: single-cell and -DNA fiber analyses. | Seiler, JA., et al. 2007. Mol Cell Biol. 27: 5806-18. PMID: 17515603
- Radiosensitization by Chir-124, a selective CHK1 inhibitor: effects of p53 and cell cycle checkpoints. | Tao, Y., et al. 2009. Cell Cycle. 8: 1196-205. PMID: 19305158
- Role of checkpoint kinase 1 (Chk1) in the mechanisms of resistance to histone deacetylase inhibitors. | Lee, JH., et al. 2011. Proc Natl Acad Sci U S A. 108: 19629-34. PMID: 22106282
- Multicellular tumor spheroid model to evaluate spatio-temporal dynamics effect of chemotherapeutics: application to the gemcitabine/CHK1 inhibitor combination in pancreatic cancer. | Dufau, I., et al. 2012. BMC Cancer. 12: 15. PMID: 22244109
- Small-molecule inhibitors of Ataxia Telangiectasia and Rad3 related kinase (ATR) sensitize lymphoma cells to UVA radiation. | Biskup, E., et al. 2016. J Dermatol Sci. 84: 239-247. PMID: 27743911
- Coordinately Targeting Cell-Cycle Checkpoint Functions in Integrated Models of Pancreatic Cancer. | Chung, S., et al. 2019. Clin Cancer Res. 25: 2290-2304. PMID: 30538111
- A cell-based high-throughput screen identifies inhibitors that overcome P-glycoprotein (Pgp)-mediated multidrug resistance. | Zahra, R., et al. 2020. PLoS One. 15: e0233993. PMID: 32484843
- Synergistic targeting of CHK1 and mTOR in MYC-driven tumors. | Song, X., et al. 2021. Carcinogenesis. 42: 448-460. PMID: 33206174
- Efficient Hit-to-Lead Searching of Kinase Inhibitor Chemical Space via Computational Fragment Merging. | Andrianov, GV., et al. 2021. J Chem Inf Model. 61: 5967-5987. PMID: 34762402
- Syntaxin 18 regulates the DNA damage response and epithelial-to-mesenchymal transition to promote radiation resistance of lung cancer. | Thumser-Henner, C., et al. 2022. Cell Death Dis. 13: 529. PMID: 35668077
- ATR inhibition overcomes platinum tolerance associated with ERCC1- and p53-deficiency by inducing replication catastrophe. | Heyza, JR., et al. 2023. NAR Cancer. 5: zcac045. PMID: 36644397
- FBXW7 loss of function promotes esophageal squamous cell carcinoma progression via elevating MAP4 and ERK phosphorylation. | Pan, Y., et al. 2023. J Exp Clin Cancer Res. 42: 75. PMID: 36991467
- The MRN complex maintains the biliary-derived hepatocytes in liver regeneration through ATR-Chk1 pathway. | Song, J., et al. 2023. NPJ Regen Med. 8: 20. PMID: 37024481
Inhibitor of:
Chk1.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
CHIR-124, 2 mg | sc-364463 | 2 mg | $97.00 |