| 产品描述： | INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC50s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a Ki value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells |
| 靶点： |
DYRK1A;DYRK1B |
| 体外研究： |
INDY (0.3-30 μM；20 小时) 在 3 μM 时轻度抑制 tau 磷酸化，在 30 μM 时几乎完全抑制。 INDY 有效逆转异常的 tau 磷酸化并挽救由 Dyrk1A (双特异性酪氨酸-(Y)-磷酸化调节激酶 1A) 过表达诱导的受抑制的 NFAT (活化 T 细胞核因子) 信号。 Western Blot Analysis Cell Line: COS7 cells transfected with either EGFP-Dyrk1A and EGFP-tau Concentration: 0.3, 1, 3, 10, 30 μM Incubation Time: 20 hours Result: Mildly inhibited tau-phosphorylation at 3 μM, and nearly completely inhibited at 30 μM. |
| 体内研究： |
ProINDY (2.5 μM) 明显恢复非洲爪蟾胚胎的正常发育 |
| 参考文献： |
1. Ogawa Y, et al. Development of a novel selective inhibitor of the Down syndrome-related kinase Dyrk1A. Nat Commun. 2010 Oct 5;1:86. 2. Pozo N, et al. Inhibition of DYRK1A destabilizes EGFR and reduces EGFR-dependent glioblastomagrowth. J Clin Invest. 2013 Jun;123(6):2475-87. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
4.25 ml |
21.249 ml |
42.499 ml |
| 5 mM |
0.85 ml |
4.25 ml |
8.5 ml |
| 10 mM |
0.425 ml |
2.125 ml |
4.25 ml |
| 50 mM |
0.085 ml |
0.425 ml |
0.85 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
