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.
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
1 mg | 在庫あり | ¥ 47,000 |
5 mg | 在庫あり | ¥ 133,000 |
10 mg | 在庫あり | ¥ 209,500 |
25 mg | 在庫あり | ¥ 397,000 |
50 mg | 在庫あり | ¥ 682,000 |
説明 | 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. |
ターゲット&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. |
分子量 | 494.52 |
分子式 | 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), Sonification and heating are recommended.
You can also refer to dose conversion for different animals. 詳細
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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