GNF4877

CAS NO.：2041073-22-5
Empirical Formula: C25H27FN6O4
Molecular Weight: 494.52
MDL number: MFCD32263043
Update Date: 2026-04-17 17:02:34

What is GNF4877?

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.

Properties of GNF4877

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

Safety information for GNF4877

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07
GHS Hazard Statements	H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes	P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P280:Wear protective gloves/protective clothing/eye protection/face protection. P301+P312:IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for GNF4877

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