MT47-100 is a novel potent, allosteric, simultaneously direct activator and inhibitor of AMPK complexes containing the β1 or β2 isoform, respectively.
MT47-100 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.
MT47-100 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.
MT47-100 augmentes glucose-stimulated insulin secretion from isolated mouse pancreatic islets via a β2-dependent mechanism.
