2. Academic Validation
  3. BMS309403 stimulates glucose uptake in myotubes through activation of AMP-activated protein kinase

BMS309403 stimulates glucose uptake in myotubes through activation of AMP-activated protein kinase

  • PLoS One. 2012;7(8):e44570. doi: 10.1371/journal.pone.0044570.
Wanhua Lin 1,  Xiaoli Huang,  Lina Zhang,  Dongmei Chen,  Dongye Wang,  Qilong Peng,  Lei Xu,  Jingya Li,  Xiujie Liu,  Kuai Li,  Ke Ding,  Shouguang Jin,  Jia Li,  Donghai Wu
Affiliations

Affiliation

  • 1 The Key Laboratory of Regenerative Biology, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou, China.
PMID: 22952994 DOI: 10.1371/journal.pone.0044570
Abstract

BMS309403 is a biphenyl azole inhibitor against fatty acid binding protein 4 (FABP4) and regarded as a lead compound for effective treatment of obesity related cardio-metabolic diseases. Here we discovered an off-target activity of BMS309403 in that it stimulates glucose uptake in C2C12 myotubes in a temporal and dose dependent manner via activation of AMP-activated protein kinase (AMPK) signaling pathway but independent of FABPs. Further analysis indicated that BMS309403 activates AMPK through increasing the ratio of intracellular AMP:ATP while decreasing mitochondrial membrane potential. These findings provide mechanistic insights on the action of BMS309403.

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