A769662, 10 mg

A cell-permeable, direct activator of AMP-activated protein kinase (AMPK) supplied by STEMCELL Technologies. It activates AMPK with an EC₅₀ of 116 nM and produces a 4.1-fold stimulation via an allosteric mechanism, which potentially inhibits dephosphorylation on Thr172. The compound specifically activates β1 subunit–containing AMPK heterotrimers, and its effects are independent of kinases upstream of AMPK. Activation of AMPK by this agent can inhibit the mTORC1 signaling pathway. A769662 is also an inhibitor of Na(+)-K(+)-ATPase.

The chemical name is 6,7-dihydro-4-hydroxy-3-(2'-hydroxy[1,1'-biphenyl]-4-yl)-6-oxo-thieno[2,3-b]pyridine-5-carbonitrile (CAS 844499-71-4), with molecular formula C₂₀H₁₂N₂O₃S and a molecular weight of 360.4 g/mol. The product is supplied as a crystalline solid with a reported purity of ≥98%. Reported solubility values are ~0.5 mg/mL in a 1:1 solution of DMSO:PBS (pH 7.2), ~20 mg/mL in DMSO, and ~0.5 mg/mL in EtOH and DMF. Stock solutions may be prepared in DMSO at concentrations up to 55 mM or in absolute ethanol up to 1 mM. The product is stable at -20 °C as supplied, should be protected from prolonged exposure to light, and is stable for 12 months from the date of receipt.

Published research applications include inhibiting proliferation of mesenchymal stem cells, inhibiting reprogramming of mouse fibroblasts to induced pluripotent stem cells, delaying tumor onset in PTEN-deficient mice, inhibiting fatty acid synthesis in primary rat hepatocytes, and lowering blood glucose in Sprague Dawley rats.