GNF4877 manufacturers
- GNF4877
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- $56.00
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2026-08-30
- CAS:2041073-22-5
- Purity: 99.51%
- Supply Ability: 10g
- GNF4877
-
- $56.00
-
2026-07-27
- CAS:2041073-22-5
- Purity: 99.51%
- Supply Ability: 10g
- GNF4877
-
-
2026-07-17
- CAS:2041073-22-5
- Min. Order: 1KG
- Purity: 98%
- Supply Ability: 1000kg
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| | GNF4877 Basic information |
| Product Name: | GNF4877 | | Synonyms: | GNF4877;CID 139600315;3-Piperidinecarboxylic acid, 1-[3-[[[3-amino-6-[2-fluoro-5-(1-methylethoxy)phenyl]-2-pyrazinyl]carbonyl]amino]-4-pyridinyl]-, (3R)-;CID 139600315(GNF-4877);GNF 4877,GSK-3,inhibit,Glycogen synthase kinase-3,Glycogen synthase kinase 3,GNF-4877,GNF4877,Inhibitor,Dual specificity tyrosine regulated kinase,Dual specificity tyrosine phosphorylation regulated kinase,DYRK;GNF-4877 GNF4877 | | CAS: | 2041073-22-5 | | MF: | C25H27FN6O4 | | MW: | 494.52 | | EINECS: | | | Product Categories: | | | Mol File: | 2041073-22-5.mol |  |
| | GNF4877 Chemical Properties |
| Boiling point | 669.7±55.0 °C(Predicted) | | density | 1.367±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO: 4.17 mg/mL (8.43 mM and warming) | | pka | 2.82±0.70(Predicted) | | form | Solid | | color | Light yellow to yellow | | InChIKey | UZIATSFXNVOVFE-OAHLLOKOSA-N | | SMILES | N1(C2C=CN=CC=2NC(C2=NC(C3=CC(OC(C)C)=CC=C3F)=CN=C2N)=O)CCC[C@@H](C(O)=O)C1 |
| | GNF4877 Usage And Synthesis |
| Uses | GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6nM and 16nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66μM for mouse β (R7T1) cells)[1]. | | Biological Activity | GNF4877 is a potent inhibitor of DYRK1A and GSK3β with IC50 values of 6 nM and 16 nM, respectively, resulting in blocked NFATc nuclear export and increased β-cell proliferation (EC50 for mouse β (R7T1) cells 0.66 μM). | | in vitro | High glucose concentrations and glucokinase activators (GKAs) increase Ca 2+ signalling in β-cells, and increase intracellular Ca 2+ leads to activation of calcineurin and nuclear translocation of NFATc proteins. Indeed, concentrations of GNF4877 ((0.1 μM, 0.3 μM) well below the EC 50 for β-cell proliferation are able to induce proliferation in the presence of high glucose or pharmacological activators of glucokinase. Finally, increasing intracellular Ca 2+ with glibenclamide (a sulfonylurea receptor 1 inhibitor) or Bay K8644 (an L-type Ca 2+ sup> 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. | Animal Model: | Double transgenic RIP-DTA male mice (Tg (Ins 2-rtTA) 2 Efr Tg (teto -DTA) 1 Gfi/J) with Doxycycline (28.8±2.4 g; 82±2 days) | | Dosage: | 50 mg/kg | | Administration: | Oral gavage; twice a day; for 15 days | | Result: | Induced β-cell proliferation, increased β-cell mass and insulin content, and improved glycaemic control. | | | target | | GSK3β 16 nM (IC 50 ) | DYRK1A 6 nM (IC 50 ) | | | IC 50 | GSK3β: 16 nM (IC50); DYRK1A: 6 nM (IC50) | | References | [1] Shen W, et al. Inhibition of DYRK1A and GSK3β induces human β-cell proliferation. Nat Commun. 2015 Oct 26;6:8372. DOI:10.1038/ncomms9372 |
| | GNF4877 Preparation Products And Raw materials |
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