1. Protein Tyrosine Kinase/RTK
    Stem Cell/Wnt
    PI3K/Akt/mTOR
  2. DYRK
    GSK-3
  3. GNF4877

GNF4877 

Cat. No.: HY-129492
Handling Instructions

GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s 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 (EC50 of 0.66 μM for mouse β (R7T1) cells).

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GNF4877 Chemical Structure

GNF4877 Chemical Structure

CAS No. : 2041073-22-5

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Description

GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s 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 (EC50 of 0.66 μM for mouse β (R7T1) cells)[1].

IC50 & Target[1]

GSK3β

16 nM (IC50)

DYRK1A

6 nM (IC50)

In Vitro

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 the EC50 for 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].

In Vivo

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].

Animal Model: Double transgenic RIP-DTA male mice (Tg (Ins 2-rtTA) 2 Efr Tg (teto-DTA) 1 Gfi/J) with Doxycycline (28.8±2.4 g; 82±2 days)[1]
Dosage: 50 mg/kg
Administration: Oral gavage; twice a day; for 15 days
Result: Induced β-cell proliferation, increased β-cell mass and insulin content, and improved glycaemic control.
Molecular Weight

494.52

Formula

C₂₅H₂₇FN₆O₄

CAS No.

2041073-22-5

SMILES

O=C([[email protected]]1CN(C2=C(NC(C3=NC(C4=CC(OC(C)C)=CC=C4F)=CN=C3N)=O)C=NC=C2)CCC1)O

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

GNF4877GNF 4877GNF-4877DYRKGSK-3Dual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseGlycogen synthase kinase-3Glycogen synthase kinase 3Inhibitorinhibitorinhibit

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GNF4877
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