| Name | GNF4877 |
| Description | GNF4877 is a potent inhibitor of DYRK1A and GSK3β (IC50s: 6 nM and 16 nM, respectively), resulting in the blockade of nuclear export of nuclear factor of activated T-cells (NFATc) and increased β-cell proliferation. |
| 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 10 mg/mL (20.22 mM), Sonication is recommended.
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| Keywords | Inhibitor | inhibit | GSK-3β | GSK3β | GSK-3 | GSK3 | GNF-4877 | GNF4877 | GNF 4877 | Glycogen synthase kinase-3 | Glycogen synthase kinase 3 | DYRK1A | DYRK | Dual specificity tyrosine regulated kinase | Dual specificity tyrosine phosphorylation regulated kinase |
| Inhibitors Related | Cromolyn sodium | 4-Methyl-6-Methoxycoumarin | Indazole | GSK 3 Inhibitor IX | AT7519 | 5-Bromoindole | 4-Chloro-2'-bromoacetophenone | Ethyl linoleate | Ginsenoside Rg2 | GSK-3 Inhibitor 5 | (E/Z)-10-Hydroxy-2-decenoic acid | ROCK-IN-5 |
| Related Compound Libraries | Anti-Colorectal Cancer Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Neuroprotective Compound Library | Inhibitor Library | NO PAINS Compound Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Fluorochemical Library |
United States
