A cell-permeable naphthyridine compound that acts as a potent, reversible, and ATP-competitive inhibitor of Tpl2 kinase (IC₅₀ = 50 nM). Displays significant selectivity over other related kinases (IC₅₀ = 5, >40, 110, 180, >400 and >400 µM for EGFR, MEK, MK2, p38, Src, and PKC, respectively). Shown to inhibit LPS-induced TNF-α production both from primary human monocytes and in whole blood (IC₅₀ = 700 nM and 8.5 µM, respectively).

Cell permeable: yes

Primary Target
Tpl2 Kinase

Product competes with ATP.

Reversible: yes

Target IC₅₀: 50 nM against Tpl2 kinase

Packaged under inert gas

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

Gavrin, L.K., et al. 2005. Bioorg. Med. Chem. Lett.15, 5288.

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

Toxicity: Irritant (B)