GNF4877 --- beta Cell Proliferation Inducer

Bioss Antibodies

GNF4877 --- beta Cell Proliferation Inducer [2041073-22-5]

16

Research Use Only

GNF4877 is a highly potent and selective small molecule that promotes pancreatic beta cell proliferation in rodent (EC50 ~0.66 microM) and human primary islets (EC50 ~0.54 microM), better than its analog GNF7156. It acts most likely as a result of combined inhibition of DYRK1A and GSK3B. GNF4877-treated human islets retain functionality in vitro and after transplantation into diabetic mice. Oral dosing of GNF4877 in diabetic mice induces beta-cell proliferation, increases beta-cell mass and insulin content, and improves glycaemic control. Biochemical, genetic and cell biology data point to Dyrk1a as the key molecular target. GNF4877 and its analog GNF7156 are the good chemical tools to support the feasibility of treating diabetes with an oral therapy to restore beta-cell mass, and highlights a tractable pathway for future drug discovery efforts.

-20°C

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