GNF4877 free base · Synonyms: GNF-4877 · GNF 4877
GNF4877 is a potent DYRK1A and GSK3β inhibitor.
For research use only. Not for human or veterinary use.
GNF4877 structure
CAS No.: 2041073-22-5
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 100 mg | USD 350.00 | BP-02145-100mg | In stock | Get quote |
| 250 mg | USD 560.00 | BP-02145-250mg | In stock | Get quote |
| 500 mg | USD 910.00 | BP-02145-500mg | In stock | Get quote |
| 1 g | USD 1,460.00 | BP-02145-1g | In stock | Get quote |
| 2 g | USD 2,250.00 | BP-02145-2g | In stock | Get quote |
| 3 g | USD 3,400.00 | BP-02145-3g | In stock | Get quote |
Need another size or custom synthesis? Request a quote.
Description
GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively.
Biological activity
In Vitro High glucose concentrations and glucokinase activators (GKAs) increase Ca2+ signalling in β-cells, and increase intracellular Ca2+ leads to activation of calcineurin and nuclear translocation of NFATc proteins. Indeed, 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. Finally, increasing intracellular Ca2+ with glibenclamide (a sulfonylurea receptor 1 inhibitor) or Bay K8644 (an L-type Ca2+ channel activator) show additive activity with GNF4877. In Vivo GNF4877 (50 mg/kg; oral gavage; twice a day; for 15 days; double transgenic RIP-DTA male mice) treatment induces β-cell proliferation, increases β-cell mass and insulin content, and improves glycaemic control.
Identifiers
- SMILES
-
O=C([C@H]1CN(C2=C(NC(C3=NC(C4=CC(OC(C)C)=CC=C4F)=CN=C3N)=O)C=NC=C2)CCC1)O - InChIKey
-
UZIATSFXNVOVFE-OAHLLOKOSA-N
Specifications
- MW (average)
- 494.5181
- Formula
- C25H27FN6O4
- CAS No.
- 2041073-22-5
- Physical state
- Solid
- Color
- Light yellow to yellow
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20℃ 2 years; In solvent -20℃ 1 month;
Solubility
Soluble in DMSO