JAK Inhibitor I

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.

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

Packaged under inert gas

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

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

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

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

Toxicity: Irritant (B)