MT47-100

A novel potent, allosteric, simultaneously direct activator and inhibitor of AMPK complexes containing the β1 or β2 isoform, respectively; maximally activates α1β1γ1 approximately 2.5-fold with half-maximal activation Ka of 3.7 uM and activates all AMPKβ1 complexes regardless α or γ isoforms; directly inhibits AMPKβ2 complexes independently of α or γ isoforms with Ki of 24.8 uM, this inhibition is dependent on the β2 carbohydrate-binding module (CBM) and independent of β2-Ser108 phosphorylation; augmentes glucose-stimulated insulin secretion from isolated mouse pancreatic islets via a β2-dependent mechanism.

References 1. Scott JW, et al. Chem Biol. 2015 Jun 18;22(6):705-11. View Related Products by Target AMPK