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产品价格:电议      采购度:1594      原产地:美洲
发布时间:2021/7/24 0:37:19 所属地区:上海 上海市
简要描述:
LRRK2-IN-1 是一种有效的,选择性的 LRRK2 抑制剂,作用于 LRRK2 (G2019S) 和 LRRK2 (WT),IC50 值分别为 6 nM 和 13 nM。
标签:lrrk2-in-1
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CAS No. : 1234480-84-2
MCE 站:LRRK2-IN-1
产品活性:LRRK2-IN-1 是一种有效的,选择性的 LRRK2 抑制剂,作用于 LRRK2 (G2019S) 和 LRRK2 (WT),IC50 值分别为 6 nM 和 13 nM。
In Vitro: Wild-type and G2019S transduction results in 2.5 fold higher TR-FRET signal which can be inhibited by LRRK2-IN-1 in a dose-dependent manner with IC50 values of 0.08 ?M and 0.03 ?M, respectively. LRRK2-IN-1 possessed an IC50 of 45 nM for inhibition of DCLK2 and exhibits an IC50 of greater than 1 ?M when evaluated in biochemical assays for AURKB, CHEK2, MKNK2, MYLK, NUAK1, and PLK1. LRRK2-IN-1 is confirmed to inhibit MAPK7 with an EC50 of 160 nM. LRRK2-IN-1 induces a dose dependent inhibition of Ser910 and Ser935 phosphorylation accompanied by loss of 14-3-3 binding to both wild type LRRK2 and LRRK2[G2019S] stably transfected into HEK293 cells. LRRK2-IN-1 is moderately cytotoxic with IC50 of 49.3 ?M in HepG2 cells. LRRK2-IN-1 exhibits genotoxicity in the presence and absence of S9 at 15.6 and 3.9 ?M, respectively. LRRK2-IN-1 inhibits proliferation, migration, and induces cell death with hallmarks of apoptosis of HCT116 and AsPC-1 cells.
In Vivo: LRRK2-IN-1 (100 mg/kg, i.p.) induces dephosphorylation of LRRK2 in the kidney of the mice. Peritumoral injection of LRRK2-IN-1 (100 mg/kg) results in a significant decrease in tumor volume and weight of AsPC-1 tumor xenografts.
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更新时间:2024/1/2 10:14:29
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