PF-06260933是一种高度选择性的MAP4K4小分子抑制剂，在激酶实验和细胞实验中的IC50值分别为3.7和160nM。
CAS：1811510-56-1
分子式：C16H13ClN4
分子量：296.75
纯度：98%
存储：Store at -20°C

Background:

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.