AMPK activator

AMPK activator is an indirect activator of AMP-activated protein kinase, AMPK (EC₅₀ = 11.7 μM).¹ It is thought to activate AMPK by inhibiting mitochondrial complex I, producing an increase in AMP levels.¹ AMPK activator stimulates glucose uptake in L6 myocytes and promotes phosphorylation of acetyl-CoA carboxylase, a known target of AMPK.¹ AMPK activator also decreases blood glucose concentrations in female Zucker diabetic rats, demonstrating its utility in whole animals.¹ At 50 μM, it inhibits the growth of multiple myeloma cells.² AMPK activator induces phosphorylation of raptor in PC3 prostate cancer cells, down-regulating mTORC1 signaling and reducing survivin expression.³

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1. Kosaka, T., Okuyama, R., Sun, W., et al. Identification of molecular target of AMP-activated protein kinase activator by affinity purification and mass spectrometry. Anal. Chem. 77(7), 2050-2055 (2005).

2. Baumann, P., Mandl-Weber, S., Emmerich, B., et al. Activation of adenosine monophosphate activated protein kinase inhibits growth of multiple myeloma cells. Exp. Cell Res. 313(16), 3592-3603 (2007).

3. Roca, H., Varsos, Z.S., and Pienta, K.J. CCL2 is a negative regulator of AMP-activated protein kinase to sustain mTOR complex-1 activation, survivin expression, and cell survival in human prostate cancer PC3 cells. Neoplasia 11(12), 1309-1317 (2009).