M77976 是一种特异性的，ATP 竞争性的丙酮酸脱氢酶激酶 PDK4 抑制剂，其作用的 IC50 值为 648 μM。M77976 有用于肥胖症和糖尿病研究的潜力。
货号:ajcx29476
CAS:394237-61-7
分子式:C17H16N2O3
分子量：296.32
溶解度:DMSO: 250 mg/mL (843.68 mM)
纯度：98%
存储：Store at -20°C
库存： 现货

Background:

M77976 is a specific ATP-competitive inhibitor of PDK4 (pyruvate dehydrogenase kinase isoforms 4), with an IC50 of 648 μM. M77976 is potential for the research of obesity and diabetes[1].

M77976 binds to the ATP-binding pocket of PDK4 and causes local conformational changes with complete disordering of the ATP lid[1].M77976 makes hydrophobic interactions with the side chains of Asn258, Ala262, Val298, Leu306 and Thr358 of PDK4[1].

[1]. Kukimoto-Niino M, et al. Inhibitor-bound structures of human pyruvate dehydrogenase kinase 4. Acta Crystallogr D Biol Crystallogr. 2011 Sep;67(Pt 9):763-73.