MG JAK Inhibitor I

Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Target K_i: 5 nM against JAK3

Primary Targetmurine JAK1

Cell permeable: yes

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

General description

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).

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.

Legal Information

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

Other Notes

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.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

500 µg in Plastic ampoule

Reconstitution

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

Warning

Toxicity: Standard Handling (A)