GNF4877 is a potentDYRK1AandGSK3βinhibitor withIC₅₀s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC₅₀of 0.66 μM for mouse β (R7T1) cells)^[1].

High glucose concentrations and glucokinase activators (GKAs) increase Ca²⁺signalling in β-cells, and increase intracellular Ca²⁺leads to activation of calcineurin and nuclear translocation of NFATc proteins. Indeed, concentrations of GNF4877 ((0.1 μM, 0.3 μM) well below theEC₅₀for β-cell proliferation are able to induce proliferation in the presence of high glucose or pharmacological activators of glucokinase. Finally, increasing intracellular Ca²⁺with glibenclamide (a sulfonylurea receptor 1 inhibitor) or Bay K8644 (an L-type Ca²⁺channel activator) show additive activity with GNF4877^[1].

GNF4877 (50 mg/kg; oral gavage; twice a day; for 15 days; double transgenic RIP-DTA male mice) treatment induces β-cell proliferation, increases β-cell mass and insulin content, and improves glycaemic control^[1].

494.52

Solid

C₂₅H₂₇FN₆O₄

2041073-22-5

Room temperature in continental US; may vary elsewhere.

DMSO : 4.17 mg/mL(8.43 mM;Need ultrasonic and warming)

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