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首页-小分子抑制剂&激动剂-Autophagy-LRRK2-HG-10-102-01
HG-10-102-01

Chemical Structure : HG-10-102-01

CAS No.: 1351758-81-0

HG-10-102-01

货号: PC-22264Not For Human Use, Lab Use Only.

HG-10-102-01 is a potent and selective inhibitor of wild-type LRRK2 and LRRK2 G2019S mutant with IC50 of 20.3 nM and 3.2 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

HG-10-102-01 is a potent and selective inhibitor of wild-type LRRK2 and LRRK2 G2019S mutant with IC50 of 20.3 nM and 3.2 nM, respectively.
HG-10-102-01 is capable of inhibiting LRRK2 phosphorylation in mouse brain.
HG-10-102-01 maintains inhibition of the A2016T mutation (IC50=153.7 nM), which induces dramatic resistance to LRRK2-IN-1.
HG-10-102-01 (0.03-1 uM) induced a dose-dependent inhibition of Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2[G2019S] stably transfected into HEK293 cells.
HG-10-102-01 also induced dephosphorylation of Ser910 and Ser935 at a concentration of 1-3 μM in the drug-resistant LRRK2[A2016T + G2019S] and LRRK2[A2016T] mutants.
HG-10-102-01 is capable of inhibiting Ser910 and Ser935 phosphorylation in mouse brain following intraperitoneal delivery of doses as low as 50 mg/kg.

物理化学性质&存储条件

分子量 377.83
分子式 C17H20ClN5O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(4-((5-chloro-4-(methylamino)pyrimidin-2-yl)amino)-3-methoxyphenyl)(morpholino)methanone

参考文献

1. Choi HG, et al. ACS Med Chem Lett. 2012 Aug 9;3(8):658-662.

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