Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 4.17 mg/mL (8.43 mM), Sonication and heating are recommended.
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
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