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抑制剂描述:

产品名称:LRRK2-IN-1

产品别名:见爱必信官网

英文别名:LRRK2-IN-1

靶点:LRRK2

CAS:1234480-84-2

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

LRRK2-IN-1 inhibits both wild-type and G2019S mutant LRRK2 kinase activity with IC50 values of 13 nM and 6 nM , respectively with 0.1 mM ATP in the assay.

溶解性:DMSO : 57 mg/mL (100 mM)
Ethanol : 57 mg/mL (100 mM)

体外研究:

In HEK 293 cells stably expressing GFP-LRRK2[G2019S], LRRK2-IN-1 alters the cytoplasmic localization of LRRK2. In human-derived neuroblastoma SHSY5Y cells and mouse Swiss 3T3 cells, LRRK2-IN-1 induces a similar dose-dependent Ser910 and Ser935 dephosphorylation and loss of 14-3-3 binding to endogenous LRRK2. In transgenic C. elegans expressing human R1441C- and G2019S-LRRK2, LRRK2-IN1 rescues the behavioral deficit characteristic of dopaminergic impairment. In mouse fibroblasts, LRRK2-IN1 reduces cell motility. In AsPC-1 and HCT116 cell lines, LRRK2-IN-1 shows anti-proliferative and pro-apoptotic properties, induces G1 and G2/M cell cycle arrest and inhibits DCLK1 mRNA and protein expression.

体内研究:In wild type male C57BL/6 mice, LRRK2-IN-1 (100 mg/kg, i.p.) inhibits Ser910 and Ser935 dephosphorylation of LRRK2 in the kidney, while no effects in the brain.

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