219511

Cdc2-Like Kinase Inhibitor IV, KH-CB19

The Cdc2-Like Kinase Inhibitor IV, KH-CB19 controls the biological activity of Cdc2-Like KInase. This small molecule/inhibitor is primarily used for Cell Structure applications.

• 別名: Cdc2-Like Kinase Inhibitor IV, KH-CB19, ( E)-Ethyl-3-(2-amino-1-cyanovinyl)-6,7-dichloro-1-methyl-1H-indole-2-carboxylate, Clk Inhibitor IV, (E)-Ethyl-3-(2-amino-1-cyanovinyl)-6,7-dichloro-1-methyl-1H-indole-2-carboxylate, Clk Inhibitor IV
• 実験式（ヒル表記法）: C₁₅H₁₃Cl₂N₃O₂
• 分子量: 338.19
• MDL番号: MFCD20926346
• UNSPSCコード: 12352200

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; protect from light
• 色: white
• 溶解性: DMSO: 50 mg/mL
• 輸送温度: ambient
• 保管温度: −20°C
• SMILES記法: ClC1=C(Cl)C(N(C)C(C(OCC)=O)=C2/C(C#N)=C\N)=C2C=C1

詳細

詳細

A cell-permeable N-methylindolyl-enaminonitrile that acts as a more potent inhibitor than TG003 (Cat. No. 219479) against CLK1 activity (IC₅₀ = 19.7 and 48.6 nM, respectively) by targeting the kinase ATP binding site in a non-ATP mimetic fashion. KH-CB19 is also reported to exhibit higher potency than TG003 against DYRK1A (IC₅₀ = 55.2 vs. 156.1 nM, respectively) and CLK3 (IC₅₀ = 0.53 vs. >4 µM, respectively), while exhibiting no activity against a panel of 71 other protein kinases. Thermostability shift assay reveals stronger interaction of KH-CB19 toward CLK4 than CLK1, predicting better or at least comparable potency against CLK4. KH-CB19 is shown to be more effective than TG003 in suppressing both basal and TNF-α-stimulated phosphorylation of serine/arginine rich proteins SRp55 (77.5% vs. 45% inhibition by 5 µM respective inhibitor against stimulated level) and SRp75 (80% vs. 27.5% inhibition by 5 µM respective inhibitor against stimulated level), as well as human tissue factor spliced variants, flTF and asHTF, mRNA levels in human microvascular endothelial cells HMEC-1.

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 3 months at -20°C.

その他情報

Fedorov, O., et al. 2011. Chem. Biol.18, 67.

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 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable