产品信息
抗原名称
DCLK1,DCLK2,LRRK2 (A2016T),LRRK2 (G2019S), LRRK2 (WT)
商品描述
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.
分子量
570.69
纯度
>98%
可溶性
DMSO : 57 mg/mL (100 mM)
Ethanol : 57 mg/mL (100 mM)
Ethanol : 57 mg/mL (100 mM)
外观
Powder
In vitro(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.
In vivo(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.
背景
别名
LRRK2-IN-1；LRRK2 inhibitor
分子式
C31H38N8O3
CAS号
1234480-84-2
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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