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GNF4877

Catalog No. T11447 CAS 2041073-22-5

GNF4877 is a potent DYRK1A and GSK3β inhibitor (IC50s: 6 nM and 16 nM). It leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation cells.

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GNF4877, CAS 2041073-22-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 205.00
5 mg	In stock	$ 578.00
10 mg	In stock	$ 913.00
25 mg	In stock	$ 1,730.00
50 mg	In stock	$ 2,970.00

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Purity: 99.11%

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Description	GNF4877 is a potent DYRK1A and GSK3β inhibitor (IC50s: 6 nM and 16 nM). It leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation cells.
Targets&IC50	DYRK1A:6 nM, GSK-3β:16 nM
In vitro	Concentrations of GNF4877 (0.1 μM, 0.3 μM) well below the EC50 for β-cell proliferation are able to induce proliferation in the presence of high glucose or pharmacological activators of glucokinase. High glucose concentrations and glucokinase activators (GKAs) increase Ca2+ signaling in β-cells, and increase intracellular Ca2+ leads to activation of calcineurin and nuclear translocation of NFATc proteins. Finally, increasing intracellular Ca2+ with glibenclamide or Bay K8644 shows additive activity with GNF4877.
In vivo	In double transgenic RIP-DTA male mice, GNF4877 (50 mg/kg; oral gavage; twice a day; for 15 days) treatment induces β-cell proliferation, increases β-cell mass and insulin content, and improves glycaemic control.

Molecular Weight	494.52
Formula	C25H27FN6O4
CAS No.	2041073-22-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4.17 mg/mL (8.43 mM), Sonication and heating are recommended.

References and Literature

1. Shen W, et al. Inhibition of DYRK1A and GSK3β induces human β-cell proliferation. Nat Commun. 2015 Oct 26;6:8372.

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Inhibitor Library PI3K-AKT-mTOR Compound Library Oxidation-Reduction Compound Library Anti-Cancer Compound Library Kinase Inhibitor Library Wnt/Hedgehog/Notch Compound Library Anti-Obesity Compound Library Bioactive Compounds Library Max Metabolism Compound Library

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Keywords

GNF4877 2041073-22-5 Cell Cycle/Checkpoint PI3K/Akt/mTOR signaling Stem Cells Tyrosine Kinase/Adaptors DYRK GSK-3 inhibit Glycogen synthase kinase-3 Glycogen synthase kinase 3 GNF-4877 Inhibitor Dual specificity tyrosine regulated kinase GNF 4877 Dual specificity tyrosine phosphorylation regulated kinase inhibitor

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