CARTProduct Variations
| Product # | Price | Quantity | |
|---|---|---|---|
| VD-CHR-0005-0001-1mg | $100 | ||
| VD-CHR-0005-0010-10mg | $900 |
Chk2 Inhibitor (CAS 724708-21-8)
$100.00 – $900.00
Product Specification
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Appearance:
Pale yellow solid
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CAS Number:
724708-21-8
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Cat.number:
VD-CHR-0005
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Formula:
C15H13N5O2
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MW:
295.3
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Purity:
≥95%
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Solubility:
DMSO
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Storage:
-20°C
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Synonyms:
(Z)-5-(2-amino-5-oxo-1H-imidazol-4(5H)-ylidene)- 2,3,4,5-tetrahydroazepino[3,4-b]indol-1(10H)-one
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Size:
10mg, 1mg
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).
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.
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