InSolution JAK Inhibitor I

Not available outside of the UK & Ireland.

Biochem/physiol Actions

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

Reversible: yes

Product competes with ATP.

Target K_i: 5 nM against JAK3

Primary Targetmurine JAK1

Cell permeable: yes

General description

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.

Legal Information

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

Other Notes

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

Packaging

Packaged under inert gas

500 µg in Plastic ampoule

Physical form

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

Reconstitution

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

Warning

Toxicity: Irritant (B)