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.

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

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