CCG-1423, a selective RhoA pathway inhibitor, suppresses SRF-mediated transcription.

LRRK2 (G2019S):1.85 nM, LRRK2 (WT):1.28 nM

在H9c2细胞中,CCG-1423抑制MRTF核定位,并完全阻断STARS近端报告基因活性。在人结肠肌成纤维细胞中,CCG-1423抑制TGF-β诱导的纤维增生。小鼠胚胎干细胞在CCG-1423与LY294002作用下,分化为中间中胚层。在RhoC过表达的黑色素瘤细胞(A375M2 和 SK-Mel-147)中,CCG-1423能够选择性抑制细胞增殖。

Cells in normal culture medium are plated (2,000 per well) in a 96-well plate coated with laminin. After attachment, the medium is replaced with serum-free medium (0% FBS) with 30 μmol/L LPA with or without 300 nM CCG-1423. Fresh LPA with or without CCG-1423 is added at day 5 to ensure that LPA and compound are present throughout the experiment. On day 8, WST-1 reagent is added to the wells for 1 h and absorbance at 450 nm is read using a Victor plate reader.(Only for Reference)