| 产品描述： | JH-II-127 is an orally active, highly potent, selective and brain-permeable LRRK2 inhibitor, with IC50s of 6, 2 and 48 nM for wild-type LRRK2 and LRRK2-G2019S and mutant LRRK2-A2016T. JH-II-127 inhibits Ser935 phosphorylation in all tissues of mice, including the brain. JH-II-127 can be used in the study of parkinson's syndrome |
| 靶点： |
LRRK2 |
| 体外研究： |
JH-II-127 (0.03, 0.1, 0.3, 1, 3 µM; 90 min) inhibits LRRK2 in HEK293 cells. JH-II-127 (0.3, 1, 3 µM; 90 min) inhibits endogenously expressed LRRK2 in mouse Swiss 3T3 cells. Western Blot Analysis Cell Line: HEK293 cells (expressing GFP-LRRK2, GFP-LRRK2[G2019S], GFP-LRRK2[G2019S + A2016T], and GFP-LRRK2[A2016T], respectively) Concentration: 0.03, 0.1, 0.3, 1, 3 µM Incubation Time: 90 min Result: Induced a dose-dependent inhibition of Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2[G2019S] stably transfected into HEK293 cells.Inhibited phosphorylation of Ser910 and Ser935 at approximately 0.3 μM for wild-type LRRK2 and LRRK2[G2019S].Induced dephosphorylation of Ser910 and Ser935 at a concentration of 0.3-1 μM in the drug-resistant LRRK2[A2016T + G2019S] and LRRK2[A2016T] mutants. Western Blot Analysis Cell Line: Mouse Swiss 3T3 cells Concentration: 0.03, 0.1, 0.3, 1, 3 µM Incubation Time: 90 min Result: Induced similar dose-dependent Ser935 dephosphorylation of endogenous LRRK2. |
| 体内研究： |
JH-II-127 (100 mg/kg; i.p.; single) results in near complete dephosphorylation of Ser935 of LRRK2 in all tissues including brain |
| 参考文献： |
1. Hatcher JM, et al. Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett. 2015 Apr 7;6(5):584-9. |
| 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 |
2.399 ml |
11.994 ml |
23.988 ml |
| 5 mM |
0.48 ml |
2.399 ml |
4.798 ml |
| 10 mM |
0.24 ml |
1.199 ml |
2.399 ml |
| 50 mM |
0.048 ml |
0.24 ml |
0.48 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)
北京