A selective

CHIR124 – 10 mg

Brand:
Cayman
CAS:
405168-58-3
Storage:
-20
UN-No:
Non-Hazardous - /

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}  

 

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Description

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

Formal name: 4-[(3S)-1-azabicyclo[2.2.2]oct-3-ylamino]-3-(1H-benzimidazol-2-yl)-6-chloro-2(1H)-quinolinone

Synonyms: 

Molecular weight: 419.9

CAS: 405168-58-3

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Checkpoint Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling

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