GNF4877
- Product Name
- GNF4877
- CAS No.
- 2041073-22-5
- Chemical Name
- GNF4877
- Synonyms
- GNF4877;CID 139600315;GNF-4877 GNF4877;CID 139600315(GNF-4877);3-Piperidinecarboxylic acid, 1-[3-[[[3-amino-6-[2-fluoro-5-(1-methylethoxy)phenyl]-2-pyrazinyl]carbonyl]amino]-4-pyridinyl]-, (3R)-;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
- CBNumber
- CB55540441
- Molecular Formula
- C25H27FN6O4
- Formula Weight
- 494.52
- MOL File
- 2041073-22-5.mol
GNF4877 Property
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- SML2664
- Product name
- GNF-4877
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $107
- Updated
- 2025/07/31
- Product number
- SML2664
- Product name
- GNF-4877
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $346
- Updated
- 2025/07/31
- Product number
- CS-0105879
- Product name
- GNF4877
- Purity
- 98.85%
- Packaging
- 5mg
- Price
- $700
- Updated
- 2021/12/16
- Product number
- CS-0105879
- Product name
- GNF4877
- Purity
- 98.85%
- Packaging
- 10mg
- Price
- $1100
- Updated
- 2021/12/16
- Product number
- CS-0105879
- Product name
- GNF4877
- Purity
- 98.85%
- Packaging
- 25mg
- Price
- $2100
- Updated
- 2021/12/16
GNF4877 Chemical Properties,Usage,Production
Uses
GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6?nM and 16?nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66?μM 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
Raw materials
Preparation Products
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