JAK Inhibitor I-CAS 457081-03-7-Calbiochem

产品说明

一般描述

A potent, reversible, cell-permeable, and ATP-competitive 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). Inhibits other kinases at much higher concentrations. Shown to inhibit IL2- and IL4-dependent proliferation of CTLL cells and block the phosphorylation of STAT5; and further induce growth inhibition of multiple myeloma cells expressing activated JAKs and STAT3, unlike AG 490 (Cat. No. 658401). A 10 mM (500 µg/162 µl) solution of JAK Inhibitor I (Cat. No. 420097) in DMSO is also available.
A potent, cell-permeable, reversible, and ATP-competitive 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). Inhibits other kinases at much higher concentrations. Shown to inhibit IL2- and IL4-dependent proliferation of CTLL cells and block the phosphorylation of STAT5, and further induce growth inhibition of multiple myeloma cells expressing activated JAKs and STAT3, unlike AG 490 (Cat. No. 658401).

包装

500 μg in Plastic ampoule
1 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Target K_i: 5 nM against JAK3
Target IC₅₀: 15 nM against murine JAK1; 1 nM against JAK2; 1 nM against Tyk2
Reversible: yes
Cell permeable: yes
Primary Target
murine JAK1
Product competes with ATP.

警告

Toxicity: Standard Handling (A)

重悬

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

其他说明

Pedranzini, L., et al. 2006. Cancer Res.66, 9714.
Lucet, I.S., et al. 2005. Blood107, 176.
Thompson, J.E., et al. 2002. Bioorg. Med. Chem. Lett.12, 1219.

法律信息

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

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