PF-06260933 (Synonyms: PF-06260933) |
| Catalog No.GC31675 |
PF-06260933 est un inhibiteur oralement actif et hautement sélectif de MAP4K4 avec des IC50 de 3,7 et 160 nM pour la kinase et la cellule, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1811510-56-1
Sample solution is provided at 25 µL, 10mM.
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PF-06260933 is a highly selective small-molecule inhibitor of MAP4K4 with IC50s of 3.7 and 160 nM for kinase and cell, respectively.
PF-06260933 treatment of human aortic endothelial cell (EC) robustly prevents TNF-α-mediated endothelial permeability in vitro, similar to MAP4K4 knockdown[2].
In the mice model, PF-06260933 treatment does not alter plasma lipid content, although reductions in glucose levels are observed, which is consistent with whole-body-inducible Map4k4 knockout animals. PF-06260933 administration ameliorates further plaque development and/or promotes plaque regression in this animal model (46.0% versus 25.5%), and a reduction in plasma glucose as well as lipid content is also observed[2].
[1]. Ammirati M, et al. Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment. ACS Med Chem Lett. 2015 Oct 6;6(11):1128-33. [2]. Roth Flach RJ, et al. Endothelial protein kinase MAP4K4 promotes vascular inflammation and atherosclerosis. Nat Commun. 2015 Dec 21;6:8995.
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