JNK Inhibitor X, BI-78D3

Toxicity: Standard Handling (A)

A cell-permeable benzodioxin-triazole compound that competes with JNK-interacting protein-1 (IC₅₀ = 500 nM in competitive binding to JNK1 with pepJIP1) and D-domain-containing substrates binding (K_i = 200 nM in competitive binding to JNK1 with ATF2) by targeting JNK JIP1-interacting site (K_d = 8.1 µM). BI-78D3 inhibits the phosphorylation of ATF2, but not that of a D-domain-less peptide substrate, by JNK1 in kinase assays, while showing 100-fold less potency against p38α and no effect against mTOR or PI3-Kα. Shown to inhibit the TNF-α-stimulated GFP-cJun phosphorylation in transfected HeLa cultures in vitro (IC₅₀ = 12.4 µM) and effectively reduce ConA-induced murine liver failure (10 mg/kg, i.p.) as well as restore insulin sensitivity in a murine type 2 diabetes model (25 mg/kg, i.p.) in vivo.

Stebbins, J.L., et al. 2008. Proc. Natl. Acad. Sci. USA105, 16809.

Packaged under inert gas

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

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