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.

• 別名: 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
• 実験式（ヒル表記法）: C₁₅H₁₃N₅O₂
• CAS番号: 724708-21-8
• 分子量: 295.30
• MDL番号: MFCD22380609
• UNSPSCコード: 12352202

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; desiccated (hygroscopic); protect from light
• 色: pale yellow
• 溶解性: DMSO: 100 mg/mL
• 保管温度: −20°C
• SMILES記法: Cl.N1C(=N\C(=C2\CCNC(=O)c3[nH]c4c(c3\2)cccc4)\C1=O)N

詳細

詳細

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).

生物化学的／生理学的作用

Primary Target
Chk2

Target IC₅₀: 8 nM against Chk2

警告

Toxicity: Carcinogenic / Teratogenic (D)

再構成

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

その他情報

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

法的情報

Sold under license from Michigan State University.

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 1
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable