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.

• Sinônimo(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
• Fórmula empírica (Notação de Hill): C₁₅H₁₃N₅O₂
• Número CAS: 724708-21-8
• Peso molecular: 295.30
• Número MDL: MFCD22380609
• Código UNSPSC: 12352202

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥95% (HPLC)
• Formulário: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; desiccated (hygroscopic); protect from light
• cor: pale yellow
• solubilidade: DMSO: 100 mg/mL
• temperatura de armazenamento: −20°C
• cadeia de caracteres SMILES: Cl.N1C(=N\C(=C2\CCNC(=O)c3[nH]c4c(c3\2)cccc4)\C1=O)N
• chave InChI: FRROPNANZGODOW-MKFZHGHUSA-N

Descrição

Descrição geral

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).

Ações bioquímicas/fisiológicas

Primary Target
Chk2

Target IC₅₀: 8 nM against Chk2

Advertência

Toxicity: Carcinogenic / Teratogenic (D)

Reconstituição

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

Outras notas

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

Informações legais

Sold under license from Michigan State University.

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 1
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable