GNF2133 是一种有效的特异性 DYRK1A 抑制剂，IC50 为 6.2 nM。 GNF2133 可用于关于 1 型糖尿病的研究。

GNF2133 is an effective and selective inhibitor of DYRK1A with IC50s of 6.2 nM. GNF2133 can be used in studies about type 1 diabetes.

GNF2133 has an IC50 of >50 μM for GSK3β. GNF2133 significantly improves glucose disposal capacity and increases insulin secretion[1].

In Diphtheria toxin A (RIP-DTA) mice, GNF2133 (3, 10, 30 mg/kg) significantly improves glucose disposal capacity and increased insulin secretion. In CD-1 mice, GNF2133 (30 mg/kg; p.o.) shows moderate plasma exposure and good oral absorption with oral bioavailability of 22.3%[1]. In Wistar Han rat, GNF2133 (30 mg/kg; p.o.) increases in cell proliferation marker Ki67 and insulin and reduces cyclin D1 levels and overall cell density[1].

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C24H30N6O2

434.53

DMSO:4.5 mg/mL (10.36 mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years