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GNF4877
Catalog No. T11447Cas No. 2041073-22-5
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.
GNF4877
Catalog No. T11447Cas No. 2041073-22-5
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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $127 | In Stock | |
| 5 mg | $312 | In Stock | |
| 10 mg | $543 | In Stock | |
| 25 mg | $987 | In Stock | |
| 50 mg | $1,370 | In Stock | |
| 100 mg | $1,850 | In Stock |
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Purity:99.40%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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. |
| 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 & Solubility Information
| 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. | |||||||||||||||
Solution Preparation Table | ||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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