Selective, orally active, ATP-competitive
inhibitor of p38α
MAPK (IC50 values are 3.2, 122 and > 50000 nM for p38α, p38β and p38γ
respectively). Demonstrates no activity against a range of other kinases
including ERK2, JNK1 and MAPKAP2. Prevents development of diabetes and
alleviates mild and moderate hyperglycaemic states in NOD mice.
Myerset al
(2003) Inhibition of p38 MAP kinase activity enhances axonal regeneration.
Exp.Neurol. 184 606. Medicherlaet al (2006)
Preventive and therapeutic potential of p38α-selective mitogen-activated protein
kinase inhibitor in nonobese diabetic mice with type 1 diabetes.
J.Pharmacol.Exp.Ther. 318 99.