GNF2133 是一种有效的、选择性的、具有口服活性的 DYRK1A 抑制剂，对 DYRK1A 和 GSK3β 的 IC50 分别为 0.0062、>50 uM。GNF2133 对大鼠和人原代 β 细胞具有良好的增殖能力和功效。GNF2133 显著提高葡萄糖处理能力并增加胰岛素分泌。GNF2133 具有研究1型糖尿病的潜力。
货号:ajcx38174
CAS:2561414-56-8
分子式:C24H30N6O2
分子量：434.53
溶解度:DMSO : 5 mg/mL (11.51 mM; ultrasonic and warming and heat to 60°C)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

GNF2133 is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 &#181M for DYRK1A and GSK3β, respectively. GNF2133 shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 has the potential for the research of type 1 diabetes[1].

In Vivo：

参考文献：

[1]. Liu YA, et al. Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133. J Med Chem. 2020 Mar 26;63(6):2958-2973.