VX-745 is highly potent and selective p38α inhibitor (IC50 = 10 nM). VX-745 also blocks TNFα production in LPS-stimulated HWB in vitro (IC50 = 177 nM). VX-745 displays 1000-fold selectivity over closely related kinases, including ERK1, MK2 and
Storage Temp
Protected from light,Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
MAP kinase p38 alpha inhibitor
Note
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2.Karaman MW, Herrgard S, Treiber DK, Gallant P, Atteridge CE, Campbell BT, Chan KW, Ciceri P, Davis MI, Edeen PT et al.. (2008) A quantitative analysis of kinase inhibitor selectivity.. Nat Biotechnol, 26 (1):(127-32). [PMID:18183025]
3.Munoz L, Ralay Ranaivo H, Roy SM, Hu W, Craft JM, McNamara LK, Chico LW, Van Eldik LJ, Watterson DM. (2007) A novel p38 alpha MAPK inhibitor suppresses brain proinflammatory cytokine up-regulation and attenuates synaptic dysfunction and behavioral deficits in an Alzheimer's disease mouse model.. J Neuroinflammation, 4 (3):(21). [PMID:17784957]
4.Duffy JP, Harrington EM, Salituro FG, Cochran JE, Green J, Gao H, Bemis GW, Evindar G, Galullo VP, Ford PJ et al.. (2011) The Discovery of VX-745: A Novel and Selective p38α Kinase Inhibitor.. ACS Med Chem Lett, 2 (10):(758-63). [PMID:24900264]
5.Alam JJ. (2015) Selective Brain-Targeted Antagonism of p38 MAPKα Reduces Hippocampal IL-1β Levels and Improves Morris Water Maze Performance in Aged Rats.. J Alzheimers Dis, 48 (1):(219-27). [PMID:26401942]
6.Alam J, Blackburn K, Patrick D. (2017) Neflamapimod: Clinical Phase 2b-Ready Oral Small Molecule Inhibitor of p38α to Reverse Synaptic Dysfunction in Early Alzheimer's Disease.. J Prev Alzheimers Dis, 4 (4):(273-278). [PMID:29181493]
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