| 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 | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 4.17 mg/mL (8.43 mM), Sonication and heating are recommended.
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| Keywords | GSK-3 | inhibit | Glycogen synthase kinase-3 | Glycogen synthase kinase 3 | GNF4877 | GNF-4877 | Inhibitor | Dual specificity tyrosine regulated kinase | GNF 4877 | Dual specificity tyrosine phosphorylation regulated kinase | DYRK |
| Inhibitors Related | Harmine | PHA-767491 | Cromolyn sodium | GSK 3 Inhibitor IX | CHIR-99021 | AT7519 | 5-Bromoindole | 4-Chloro-2'-bromoacetophenone | SNS-032 | GSK-3 Inhibitor 5 | MeBIO | 1-Azakenpaullone |
| Related Compound Libraries | PI3K-AKT-mTOR Compound Library | Bioactive Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Anti-Obesity Compound Library | Inhibitor Library | Neuroprotective Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
United States
