The JNK Inhibitor XI, BI-87G3, also referenced under CAS 2207-44-5, controls the biological activity of JNK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
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 (t1/2 = 70 min) as well as plasma (80% remaining after 60 min) stability assays at 37°C.
Packaging
Packaged under inert gas
Warning
Toxicity: Harmful (C)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
De, S.K., et al. 2009. Bioorg. Med. Chem.17, 2712.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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