MLR-1023 is an allosteric activator of Lyn kinase (EC₅₀ = 63 nM). It reduces blood glucose levels without increasing insulin secretion in vivo. MLR-1023 does not activate peroxisome proliferator-activated α, d, and g receptors or glucagon-like peptide-1 receptors or inhibit dipeptidyl peptidase-4 (DPP-4) or -glucosidase enzyme activity.