gk-gkrp

AMG-1694, a potent disruptor of the glucokinase–glucokinase regulatory protein (GK-GKRP) complex, operates by promoting the dissociation of this complex, thereby indirectly enhancing GK enzymatic activity with an IC50 of 7 nM. It effectively normalizes blood glucose levels in various rodent diabetes models [1] and lowers blood glucose specifically in diabetic animals without affecting normoglycemic ones. Additionally, AMG-1694 reverses the GKRP-induced inhibition of GK activity and facilitates GK translocation.

(1S,2R)-Globalagliatin is a highly potent glucokinase (GK) activator for the study of type 2 diabetes.

RO-28-1675 is a direct and selective glucokinase activator that indirectly affects the activity of the GK GKRP (glucokinase regulatory protein) complex, with efficacy decreasing with increasing glucose concentration, and can be used in studies related to insulin secretion and type 2 diabetes.

AMG-3969 is an effective glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor (IC50: 4 nM).

AMG-7549 is a disrupter of Glucokinase−Glucokinase Regulatory Protein (GK−GKRP) binding.