GNF2133 HCl
| CAS号 | 2561414-57-9 | 货号 | BCP45493 |
| 中文名 | GNF2133 HCl | ||
| 英文名 | GNF2133 HCl | ||
| 中文别名 | |||
| 英文别名 | GNF2133 hydrochloride; GNF-2133 HCl; GNF 2133 HCl; | ||
| 分子式 | C24H31ClN6O2 | 分子量 | 471.0 |
| 生物活性 | GNF2133 hydrochloride is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 hydrochloride shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 hydrochloride significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 hydrochloride has the potential for the research of type 1 diabetes.GNF2133 is a potent and selective DYRK1A inhibitor (IC50 = 6 nM). In vitro, GNF2133 is able to proliferate both rodent and human β-cells. In vivo, GNF2133 demonstrated significant dose-dependent glucose disposal capacity and insulin secretion in response to glucose-potentiated arginine-induced insulin secretion (GPAIS) challenge in rat insulin promoter and diphtheria toxin A (RIP-DTA) mice. | ||
| 信号通路 | Angiogenesis/Protein Tyrosine Kinase | ||
| 靶 点 | DYRK | ||
结构式
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