VX-745

VX-745 is a potent inhibitor of p38alpha MAPK (IC50=10nM) with 20-fold selectivity over p38beta and 1000-fold selectivity over closely related kinases, ERK1, MK2 and JNK1-3. p38alpha is a member of the mitogen-activated protein kinase (MAPK) family of serine/threonine protein kinases and is widely expressed in endothelial, immune or inflammatory cells and plays a central role in the regulation of proinflammatory cytokine production including TNF-alpha, IL-1beta and IL-6. VX-745 is an anti-inflammatory agent that blocks IL-1beta and TNF-alpha release in whole blood in vitro with IC50 values of 150 and 180nM, respectively. VX-745 showed anti-inflammatory efficacy in an animal model of rheumatoid arthritis and recently anti-neuroinflammatory potential in prevention of early-stage Alzheimers diseases (AD). Appearance: Off-white to yellowish solid. Solubility: Soluble in DMSO (25mg/ml) or DMF (30mg/ml). Insoluble in water. InChi Key: VEPKQEUBKLEPRA-UHFFFAOYSA-N Smiles: FC1=CC(F)=C(SC2=NN(C=N3)C(C=C2)=C(C4=C(Cl)C=CC=C4Cl)C3=O)C=C1