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CHIR124
- CHIR-124
- Optical Purity: >98% e.e.
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C23H22ClN5O
- MW: 419.91
Description
CHIR124 is a potent, cell-permeable and selective Chk1 inhibitor with reported IC50 values of 0.32 nM for Chk1 and 697 nM for Chk2.
Chk1 controls replication stress responses and DNA damage checkpoints that allow cell-cycle arrest and repair. CHIR124 is useful for studying checkpoint abrogation, replication stress and sensitization of tumor cells to DNA-damaging agents.
Key Features
- Potent and selective Chk1 inhibitor
- Reported IC50: 0.32 nM for Chk1 versus 697 nM for Chk2
- Cell-permeable checkpoint kinase inhibitor
- Useful for DNA damage sensitization studies
Applications
- Chk1 kinase assays
- DNA damage checkpoint research
- Replication stress model studies
- Chemotherapy combination and sensitization assays
More Information
| Parent CAS No. | 405168-58-3 |
|---|---|
| Chemical Name | (S)-3-(1H-benzo[d]imidazol-2-yl)-6-chloro-4-(quinuclidin-3-ylamino)quinolin-2(1H)-one |
| SMILES | N([C@@H]1CN2CCC1CC2)C1C2=CC(Cl)=CC=C2NC(=O)C=1C1=NC2=CC=CC=C2N1 |&1:1,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C23H22ClN5O/c24-14-5-6-16-15(11-14)21(25-19-12-29-9-7-13(19)8-10-29)20(23(30)28-16)22-26-17-3-1-2-4-18(17)27-22/h1-6,11,13,19H,7-10,12H2,(H,26,27)(H2,25,28,30)/t19-/m1/s1 |
| InChiKey | MOVBBVMDHIRCTG-LJQANCHMSA-N |
| CID | 135399748 |
| Short Description | CHK1 inhibitor |
References
- ZJ Ni et al. 4-(Aminoalkylamino)-3-benzimidazolequinolinones as potent CHK-1 inhibitors. Bioorg. Med. Chem. Lett. 2006, 16(12), 3121-3124.
- AN Tse et al. CHIR-124, a Novel Potent Inhibitor of Chk1, Potentiates the Cytotoxicity of Topoisomerase I Poisons In vitro and In vivo. Clin. Cancer Res. 2007, 13, 591-602.
- Y Tao et al. Radiosensitization by Chir-124, a selective CHK1 inhibitor: effects of p53 and cell cycle checkpoints. Cell Cycle. 2009, 8(8), 1196-205.
- JL Smith. Role of checkpoint kinase 1 in malignant melanoma. PhD thesis 2013, University of Glasgow, UK.
- List of publications using CHIR124 (Axon 1636) purchased from Axon Medchem
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