219491

Cdk/Crk Inhibitor

The Cdk/Crk Inhibitor, also referenced under CAS 784211-09-2, controls the biological activity of Cdk/Crk. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• 別名: Cdk/Crk Inhibitor, 1-(2,6-Dichlorophenyl)-1,5-dihydro-6-((4-(2-hydroxyethoxy)phenyl)methyl)-3-(1-methylethyl)-4H-pyrazolo[3,4-d]pyrimidin-4-one, RGB-286147, Cdk7 Inhibitor IV
• 実験式（ヒル表記法）: C₂₃H₂₂Cl₂N₄O₃
• CAS番号: 784211-09-2
• 分子量: 473.35
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: white
• 溶解性: DMSO: 5 mg/mL
• 輸送温度: ambient
• 保管温度: −20°C

詳細

詳細

A cell-permeable pyrazolo-pyrimidinone compound that acts as a potent, selective, and ATP-competitive inhibitor of Cdks (IC₅₀ = 48 nM, 15 nM, 9 nM, 10 nM, 71 nM, and 9 nM for Cdk1/B, Cdk2/E, Cdk3/E, Cdk5/p35, Cdk7/H/MAT1, and Cdk9, respectively). It inhibits Cdk4/D1, Cdk6/D3, and GSK-3β only at much higher concentrations (IC₅₀ = 839 nM, 282 nM, and 754 nM, respectively) and exhibits little activity towards a panel of 60 other kinases. A broad-spectrum growth inhibitor toward tumor cells, but not non-transformed quiescent fibroblasts.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
Cdk1/B, Cdk2/E, Cdk3/E, Cdk5/p35, Cdk7/H/MAT1, and Cdk9

Product competes with ATP.

Reversible: no

Target IC₅₀: 48 nM, 15 nM, 9 nM, 10 nM, 71 nM, and 9 nM for Cdk1/B, Cdk2/E, Cdk3/E, Cdk5/p35, Cdk7/H/MAT1, and Cdk9, respectively

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

その他情報

Caligiuri, M., et al. 2005. Chem. Biol.12, 1103.

法的情報

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