JAK3 Inhibitor VI

A cell-permeable 3′-pyridyl oxindole compound that acts as a potent and reversible inhibitor of JAK3 (IC₅₀ = 27 nM)and displays ~16-fold greater selectivity over JAK2. Binds to the enzyme active site and prevents IL-2-induced cellular phosphorylation of JAK3 and STAT5. Inhibits IL-2-induced cell proliferation (IC₅₀ = 760 and 250 nM for mouse CTLL and human T-cells, respectively) and alleviates oxazolone-induced ear odema in mouse with an efficacy comparable to that of Dexamethasone (Cat. No. 265005).

A cell-permeable, potent, and reversible inhibitor of Janus kinase 3 (JAK3) (IC₅₀ = 27 nM). Reported to bind to the enzyme active site and prevent IL-2-induced phosphorylation of JAK3 and STAT5. Also reported to inhibit IL-2-induced cell proliferation (IC₅₀ = 760 nM for murine CTLL cells and 250 nM for human T-cells). Shown to alleviate oxazolone-induced ear edema in mice with an efficacy comparable to Dexamethasone (Cat. No. 265005) and displays ~16-fold greater selectivity over JAK2.

Cell permeable: yes

Primary Target
JAK-3

Product does not compete with ATP.

Reversible: yes

Packaged under inert gas

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

Chen, J., et al. 2006. Bioorg. Med. Chem. Lett. In press.
Adams, C., et al. 2003. Bioorg. Med. Chem. Lett.13, 3105.

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

Toxicity: Carcinogenic / Teratogenic (D)