220485-M

Chk2 Inhibitor

The Chk2 Inhibitor, also referenced under CAS 724708-21-8, controls the biological activity of Chk2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): Chk2 Inhibitor, 5-(2-Amino-5-oxo-1,5-dihydroimidazol-4-ylidine)-3,4,5,10-2H-azepino[3,4-b]indol-1-one, Chk1 Inhibitor II, Chk2 Inhibitor I
• Empirical Formula (Hill Notation): C₁₅H₁₃N₅O₂
• CAS Number: 724708-21-8
• Molecular Weight: 295.30
• UNSPSC Code: 12352202

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: pale yellow
• solubility: DMSO: 100 mg/mL
• storage temp.: −20°C

Description

General description

A cell-permeable, ATP competitive, and reversible indoloazepine compound that displays anti-proliferative and anti-inflammatory 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).

Biochem/physiol Actions

Primary Target
Chk2

Target IC₅₀: 8 nM against Chk2

Warning

Toxicity: Carcinogenic / Teratogenic (D)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

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

Legal Information

Sold under license from Michigan State University.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable