General description

A cell-permeable benzothiazole compound that inhibits JNK kinase activity (IC₅₀ = 1.8 µM against ATF2 phosphorylation by JNK1) by competing with substrate binding (IC₅₀ = 0.16 µM against pepJIP1 binding to JNK2), while exhibiting much reduced activity toward two other kinases (IC₅₀ >100 µM against p38α and Akt) and two other proteases (IC₅₀ >50 and >100 µM, respectively, against furin and LF). Shown to effectively block cellular c-Jun phosphorylation upon TNF-α stimulation even in HeLa cultures with overexpressed c-Jun substrate (IC₅₀ = 15 µM) and display favorable stability in rat microsome (t_1/2 = 70 min) as well as plasma (80% remaining after 60 min) stability assays at 37°C.

Legal Information

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

Other Notes

De, S.K., et al. 2009. Bioorg. Med. Chem.17, 2712.

Packaging

Packaged under inert gas

Reconstitution

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

Warning

Toxicity: Harmful (C)