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Merck
CN

420148

JAK3/GSK-3β/PKCα Inhibitor

The JAK3/GSK-3β/PKCα Inhibitor, also referenced under CAS 1260181-14-3, controls the biological activity of JAK3/GSK-3β/PKCα. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

别名:

JAK3/GSK-3β/PKCα Inhibitor, 3-(5-(4-(2-Hydroxy-2-methyl-propionyl)-piperazin-1-yl)-2-trifluoromethyl-phenyl)-4-(1H-indol-3-yl)-pyrrole-2,5-dione, JAK3 Inhibitor XII, NIBR3049, JAK3 Inhibitor XII, NIBR3049, 3-(5-(4-(2-Hydroxy-2-methyl-propionyl)-piperazin-1-yl)-2-trifluoromethyl-phenyl)-4-(1H-indol-3-yl)-pyrrole-2,5-dione

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关于此项目

经验公式（希尔记法）:
C27H25F3N4O4
化学文摘社编号:
1260181-14-3
分子量:
526.51
MDL编号:
MFCD19380092
UNSPSC代码:
12352200
NACRES:
NA.77

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质量水平

100

方案

≥95% (HPLC)

表单

solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

yellow

溶解性

DMSO: soluble

运输

ambient

储存温度

2-8°C

SMILES字符串

O=C1NC(C(C2=CNC3=C2C=CC=C3)=C1C4=CC(N5CCN(C(C(C)(C)O)=O)CC5)=CC=C4C(F)(F)F)=O

InChI

1S/C27H25F3N4O4/c1-26(2,38)25(37)34-11-9-33(10-12-34)15-7-8-19(27(28,29)30)17(13-15)21-22(24(36)32-23(21)35)18-14-31-20-6-4-3-5-16(18)20/h3-8,13-14,31,38H,9-12H2,1-2H3,(H,32,35,36)

InChI key

CLGRAWDGLMENOD-UHFFFAOYSA-N

相关类别

一般描述

A cell-permeable phenyl-indolyl maleimide compound that acts as a potent, ATP-binding site targeting and reversible inhibitor of GSK-3β, JAK3, PKCα and PKCθ (IC50 = 3, 8, 13 and 68 nM, respectively) with excellent selectivity over 40-kinases, including JAK1, JAK2 and Tyk2 (IC50 = 1.017, 2.55 and 8.055 µM, respectively). Shown to efficiently block interleukin stimulated STAT5 phosphorylation and T cell costimulation (IC50 = 0.525, 1.294 and 0.689 µM in IL15-MO7, IL2-CTLL and TCR/CD28-Jurkat cells, respectively).

包装

Packaged under inert gas

其他说明

Haan, C., et al. 2011. Chem. Biol.18, 314.
Thoma, G., et al. 2011. J. Med. Chem.54, 284.

法律信息

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

免责声明

Toxicity: Standard Handling (A)

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

分析证书(COA)

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Gebhard Thoma et al.
Journal of medicinal chemistry, 54(1), 284-288 (2010-12-16)
We describe a synthetic approach toward the rapid modification of phenyl-indolyl maleimides and the discovery of potent Jak3 inhibitor 1 with high selectivity within the Jak kinase family. We provide a rationale for this unprecedented selectivity based on the X-ray
Claude Haan et al.
Chemistry & biology, 18(3), 314-323 (2011-03-29)
Genetic deficiency of Jak3 leads to abrogation of signal transduction through the common gamma chain (γc) and thus to immunodeficiency suggesting that specific inhibition of Jak3 kinase may result in immunosuppression. Jak1 cooperates with Jak3 in signaling through γc-containing receptors.

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