pf06260933 dihydrochloride

PF-06260933 Dihydrochloride is a MAP4K4 (HGK) inhibitor (IC50 = 140 nM). It can improve the fasting hyperglycemia in mice. In addition, it inhibited Mink and Tnik (IC50 values of 8 and 13 nM, respectively).

MAP4K4 (HGK) inhibitor (IC50 = 140 nM). Also inhibits MINK and TNIK (IC50 values are 8 and 13 nM, respectively). Improves fasting hyperglycemia in mice. Orally active. Ammirati et al (2015) Discovery of an in vivo tool to establish proof-of-concept for MAP4K4-based antidiabetic treatment. ACS Med.Chem.Lett. 6 1128 PMID:26617966

PF-06260933 是一种具有高度选择性及口服有活性的MAP4K4小分子抑制剂，在激酶实验中IC50为 3.7 nM，在细胞实验中IC50为 160 nM。

PF-3758309 dihydrochloride 是一种有效的、可逆的、口服具有活力的、 ATP 竞争性的 PAK4 抑制剂，其 Kd 值为 2.7 nM，Ki 值为 18.7 nM。PF-3758309 dihydrochloride 显示出 PAK4 抑制剂的预期细胞功能，能够抑制锚定独立生长、诱导凋亡、细胞骨架重塑和抑制增殖。