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GNF2133

Chemical Structure : GNF2133

CAS No.: 2561414-56-8

GNF2133 (GNF-2133)

Catalog No.: PC-72351Not For Human Use, Lab Use Only.

GNF2133 (GNF-2133) is a potent and selective DYRK1A inhibitor with IC50 of 6 nM, without inhibitory effect on GSK3β.

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Biological Activity

GNF2133 (GNF-2133) is a potent and selective DYRK1A inhibitor with IC50 of 6 nM, without inhibitory effect on GSK3β.
In vitro, GNF2133 is able to proliferate both rodent and human β-cells.
In vivo, GNF2133 demonstrated significant dose-dependent glucose disposal capacity and insulin secretion in response to glucose-potentiated arginine-induced insulin secretion (GPAIS) challenge in rat insulin promoter and diphtheria toxin A (RIP-DTA) mice.

Physicochemical Properties

M.Wt 434.544
Formula C24H30N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-Piperazinecarboxamide, 4-ethyl-N-[4-[1-(tetrahydro-2H-pyran-4-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-2-pyridinyl]-

References

1. Yahu A Liu, et al. J Med Chem. 2020 Mar 26;63(6):2958-2973.

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