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Chk2 Inhibitor (CAS 724708-21-8)




Product specification

Formula: C15H13N5O2
MW: 295.3
Purity: ≥95%
Appearance: Pale yellow solid
Solubility: DMSO
Storage: -20°C
CAS Number: 724708-21-8
Synonyms: (Z)-5-(2-amino-5-oxo-1H-imidazol-4(5H)-ylidene)-
2,3,4,5-tetrahydroazepino[3,4-b]indol-1(10H)-one
Cat.number: VD-CHR-0005

Product Description

Chk2 Inhibitor (CAS 724708-21-8) is a cell-permeable indoloazepine compound that displays anti-inflammatory and anti-proliferative properties. Acts as a potent inhibitor of Chk2 (IC50 = 8 nM) that targets the ATP binding pocket. Exhibits selectivity for Chk2 over MEK1, Chk1, CK1δ, PKCα, PKCβII and CK2 (IC50 = 89 nM, 237 nM, 1.352 µM, 2.539 µM, 3.381 µM, and > 10.0 µM, respectively). Blocks the production of IL-2 and TNF-α by preventing the transcriptional activation of NF-κB (IC50 = 3.55 µM for IL-2 production in PMA-stimulated Jurkat T cells; 8.16 µM for TNF-α production in LPS-stimulated THP-1 cells). Also reported to suppress the growth of leukemic T cells (GI50 = 1.73 µM).



Product References
1. Sharma, V., and Tepe, J.J. 2004. Bioorg. Med. Chem. Lett. 14, 4319.
2. Sharma, V., et al. 2004. J. Med. Chem. 47, 3700.