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EX229

CAS No. : 1219739-36-2

MCE 站：EX229

产品活性：EX229 是一个苯并咪唑的衍生物，是 AMP 活化蛋白激酶 (AMPK) 的有效变构激动剂，其对 α1β1γ1、α2β1γ1 和 α1β2γ1 的 K_d 值分别为 0.06 μM、0.06 μM 和 0.51 μM。

研究领域：Epigenetics  |  PI3K/Akt/mTOR

作用靶点：AMPK

In Vitro: EX229 is a potent and allosteric activator of AMP-activated protein kinase (AMPK), with K_ds of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1 and α1β2γ1, respectively.. Treatment of hepatocytes with EX229 (991) alone results in a slight increase in the phosphorylation of AMPK and RAPTOR only at 0.3 μM, whereas a robust increase in ACC phosphorylation is readily observed and saturated at a concentration of 0.03 μM EX229. AICAR or C13 alone robustly increases T172 phosphorylation of AMPKα, and when 991 is coincubated, there is a modest additional dose-dependent increase in AMPKα phosphorylation. RAPTOR phosphorylation is modestly increased by AICAR or C13 alone, and it is dose dependently increased when coincubations are carried out with EX229. EX229 also dose dependently (0.01 and 0.1 μM) inhibits lipogenesis (34% and 63%, respectively), which is further reduced when it is coincubated with a low dose of AICAR (0.03 mM) or C13 (1 μM). Treatment with EX229 promotes dose-dependent increases in ACC and RAPTOR phosphorylation. Similar to the observations in hepatocytes.

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