Biochem/physiol Actions

Cell permeable: no

Reversible: no

Product competes with ATP.

pIC50 = 7.1 against JAK3

Primary TargetJAK-3

General description

A potent, selective, and ATP-competitive inhibitor of Janus tyrosine kinase-3 (JAK3) (pIC₅₀ = 7.1). Weakly inhibits JAK1 (pIC₅₀ = 4.4) and EGF-R (pIC₅₀ = 5.6). Undergoes a retro-Michael breakdown to another active analog, 2-naphthylvinyl ketone (JAK3 Inhibitor V, Cat. No. 420122) (t_½ = 36 min. at 25°C, pH 7.43).

A (β-aminoethyl)ketone that acts as a potent and selective ATP-competitive inhibitor of Janus tyrosine kinase-3 (JAK3; pIC₅₀ = 7.1). A weak inhibitor of other tyrosine kinases (pIC₅₀ = 5.6 for EGF-R; 4.4 for JAK1). It undergoes a retro-Michael breakdown (t_1/2 = 36 min at 25°C, pH 7.43) to another active 2-naphthylvinyl ketone analog (JAK Inhibitor V; Cat. No. 420122) [pIC₅₀ = 6.8 for JAK3; 5.0 for EGF-R; 4.7 for JAK1].

Legal Information

Sold under license of PCT Application W098/22,103.

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

Other Notes

Brown, G.R., et al. 2000. Bioorg. Med. Chem. Lett.10, 575.

Packaging

Packaged under inert gas

10 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Warning

Toxicity: Standard Handling (A)