GNF7156, β Cell Proliferation Inducer

Overview
Catalog #	bs-60293c-2-mg-solid
Product Name	GNF7156, β Cell Proliferation Inducer
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 418.45 Formula: C22 H22 N6 O3 CAS Number: 2041071-54-7 InChi Key: HZCOFZVJMJRKIB-UHFFFAOYSA-N InChi: InChI=1S/C22H22N6O3/c23-20-19(26-16(13-25-20)14-4-2-1-3-5-14)21(29)27-17-12-24-9-6-18(17)28-10-7-15(8-11-28)22(30)31/h1-6,9,12-13,15H,7-8,10-11H2,(H2,23,25)(H,27,29)(H,30,31) Smiles: NC1=NC=C(N=C1C(=O)NC1C=NC=CC=1N1CCC(CC1)C(O)=O)C1C=CC=CC=1 Purity: 98.0 Solubility: DMSO up to 100 mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	GNF7156 is a highly potent and selective small molecule that promotes pancreatic β cell proliferation in rodent （EC50 ~2.2 µM）and human primary islets (EC50 ~0.76 µM). It acts most likely as a result of combined inhibition of DYRK1A and GSK3B. GNF7156-treated human islets retain functionality in vitro and after transplantation into diabetic mice. Oral dosing of GNF7156 in diabetic mice induces β-cell proliferation, increases β-cell mass and insulin content, and improves glycaemic control. Biochemical, genetic and cell biology data point to Dyrk1a as the key molecular target. GNF7156 is a good chemical tool to support the feasibility of treating diabetes with an oral therapy to restore β-cell mass, and highlights a tractable pathway for future drug discovery efforts.