| 产品描述: | CZC-54252 hydrochloride is a selective inhibitor of LRRK2 with IC50s of 1.85 nM and 1.28 nM for wild-type and G2019S LRRK2. CZC-54252 hydrochloride has a neuroprotective activity and attenuates G2019S LRRK2-induced human neuronal injury with an EC50 of 1 nM |
| 靶点: |
G2019S LRRK2:1.85 nM (IC50), Wild-type LRRK2:1.28 nM (IC50) |
| 体外研究: |
CZC-54252 hydrochloride(1.6 nM) fully reverses G2019S LRRK2-induced human neuronal injury to wild-type levels. CZC-54252 hydrochloride inhibits the recombinant human wild-type LRRK2 with an IC50 ranging from 1 to 5 nM. CZC-54252 hydrochloride inhibits the G2019S mutant with an IC50 ranging from 2 to 7 nM in a TF-FRET assay |
| 参考文献: |
1. Nigel Ramsden, et al. Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson's disease-related toxicity in human neurons. ACS Chem Biol. 2011 Oct 21;6(10):1021-8. 2. Ramsden N, et al. Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson's disease-related toxicity in human neurons. ACS Chem Biol. 2011 Oct 21;6(10):1021-8. |
| 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 |
1.847 ml |
9.234 ml |
18.469 ml |
| 5 mM |
0.369 ml |
1.847 ml |
3.694 ml |
| 10 mM |
0.185 ml |
0.923 ml |
1.847 ml |
| 50 mM |
0.037 ml |
0.185 ml |
0.369 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。 |