| 产品介绍 |
Harmine is a potent, selective and orally bioavailable DYRK1A inhibitor with IC50 of 80 nM. It inhibits phosphorylation of tau directly by DYRK1A (IC50 ~700 nM). It has >10-fold selectivity over DYRK3 and DYRK2 (IC50 ~800 nM and 900 nM respectively. Harmine is also a unique regulator of PPARγ expression that acts by inhibiting the Wnt signalling pathway in a cell-specific manner. It attenuates inflammatory gene expression (TNFα, IL-1β, iNOS) and macrophage accumulation in adipose tissue. Administration of harmine (30 mg/kg) to obese db/db mice resulted in reduced blood glucose, free fatty acids, and triglyceride levels, delayed hyperglycemia, and improved insulin sensitivity. Being function as a new class of human beta cell mitogenic compound, by using three different mouse and human islet in vivo-based models, harmine is able to induce beta cell proliferation, increase islet mass and improve glycemic control. The nuclear factors of activated T cells (NFAT) family of transcription factors are defined as likely mediators of human beta cell proliferation and differentiation.
|
