420097

JAK Inhibitor I

InSolution, ≥98%

• 別名: InSolution JAK Inhibitor I, 2-(1,1-Dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, P6, Pyridone 6, DBI, JAK1 Inhibitor I, JAK2 Inhibitor I, JAK3 Inhibitor X
• 実験式（ヒル表記法）: C₁₈H₁₆FN₃O
• CAS番号: 457081-03-7
• 分子量: 309.34
• MDL番号: MFCD17019334
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• フォーム: liquid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; desiccated (hygroscopic); protect from light
• 輸送温度: wet ice
• 保管温度: 2-8°C
• SMILES記法: Fc1cc2c(c3[nH]c(nc3c4c2c(ncc4)O)C(C)(C)C)cc1
• InChI: 1S/C18H16FN3O/c1-18(2,3)17-21-14-10-5-4-9(19)8-12(10)13-11(15(14)22-17)6-7-20-16(13)23/h4-8H,1-3H3,(H,20,23)(H,21,22)
• InChI Key: VNDWQCSOSCCWIP-UHFFFAOYSA-N

詳細

詳細

A potent inhibitor of Janus Protein tyrosine Kinases (JAKs). Displays potent inhibitory activity against JAK1 (IC₅₀ = 15 nM for murine JAK1), JAK2 IC₅₀ = 1 nM), JAK3 (K_i = 5 nM), and Tyk2 (IC₅₀ = 1 nM). It inhibits other kinases only at much higher concentrations. Also inhibits IL-2- and IL-4-dependent proliferation of CTLL cells and blocks the phosphorylation of STAT5.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
murine JAK1

Product competes with ATP.

Reversible: yes

Target IC₅₀: 15 nM, 1 nM against murine JAK1 and JAK2, respectively; 1 nM against Tyk2

Target K_i: 5 nM against JAK3

包装

Packaged under inert gas

警告

Toxicity: Irritant (B)

物理的形状

A 10 mM (500 µg/162 µl) solution of JAK Inhibitor I (Cat. No. 420099) in DMSO.

再構成

Following initial use, aliquot and refrigerate (4°C).

その他情報

Thompson, J.E., et al. 2002. Bioorg. Med. Chem. Lett.12, 1219.

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: 10 - Combustible liquids
• WGK: WGK 2
• 引火点(°F): 188.6 °F - closed cup - (Dimethylsulfoxide)
• 引火点(℃): 87 °C - closed cup - (Dimethylsulfoxide)