JNK Inhibitor XIV, SR-3306

A cell-permeable, blood-brain-barrier-permeant, and orally available anilinopyrimidine compound that acts as a highly selective, potent, reversible, and ATP-competitive JNK inhibitor (IC₅₀ = 67, 283, and 159 nM against JNK1, JNK2, and JNK3, respectively), exhibiting little or no activity toward a panel of more than 300 kinases, including p38 (IC₅₀ >20 µM). Shown to inhibit c-jun phosphorylation both in STZ- (Streptozotocin, Cat. No. 572201 ) stimulated INS-1 β-pancreatic cells in vitro (IC₅₀ = 216 nM) and in SNpc (substantia nigra pars compacta) TH- (tyrosine hydroxylase) positive neurons (by 75%; single p.o. dose of 30 mg/kg) from MPTP- (N-methyl-4-phenyl-1,2,3,6-tetrahydropyridine) treated mice in vivo. Effectively protects against SNpc TH-positive dopaminergic neuron loss in mice (46% vs. 27% loss with vehicle or 30 mg/kg SR-3306; p.o. b.i.d.) and rats (6-fold increase of vehicle control cell count; 10 mg/kg/day; s.c.) due to MPTP and 6-OHDA- (6-hydroxydopamine) intoxication, respectively, in vivo.

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Chambers, J.W., et al. 2011. ACS Chem Neurosci.2, 198.
Crocker, C.E., et al. 2011. ACS Chem. Neurosci.2, 207.

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

Toxicity: Standard Handling (A)