| 货号 | 5075/50 |
| 别名 | 7-Methoxy-1-methyl-9H-pyrido[3,4-b] |
| 供应商 | Tocris |
| 生物活性 | Potent and selective inhibitor of DYRK1A (IC50 values are 80, 800 and 900 nM for DYRK1A, DYRK3 and DYRK2 respectively). Inhibits DYRK1A-mediated tau phosphorylation and regulates PPARγ expression. Also induces pancreatic beta cell proliferation. Exhibits antidiabetic activity. Orally bioavailable. |
| 运输条件 | Blue Ice |
| 存放说明 | Ambient |
| 纯度 | >98 % |
| 计算分子量 | 212.25 |
| 分子式 | C13H12N2O |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO and to 5 mM in ethanol with gentle warming |
| 参考文献 | Wanget al (2015) A high-throughput chemical screen reveals that harmine-mediated inhibition of DYRK1A increases human pancreatic beta cell replication. Nat.Med. 21 383. PMID: 25751815. Smithet al (2012) Recent advances in the design, synthesis, and biological evaluation of selective DYRK1A inhibitors: a new avenue for a disease modifying treatment of Alzheimer's? ACS Chem.Neurosci. 3 857. PMID: 23173067. Bainet al (2007) The selectivity of protein kinase inhibitors: a further update. Biochem.J. 408 297. PMID: 17850214. Wakiet al (2007) The small molecule harmine is an antidiabetic cell-type-specific regulator of PPARγ expression. Cell Metab. 5 357. PMID: 17488638. |