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|Solubility (25°C) *||In vitro||DMSO||90 mg/mL (197.91 mM)|
|Ethanol||4 mg/mL warmed (8.79 mM)|
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Description||CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription.|
|In vitro||CCG-1423 selectively inhibits SRF-mediated transcription activated by Rho pathway signaling, and specifically inhibits LPA-stimulated DNA synthesis. CCG-1423 also selectively inhibits the proliferation of RhoC-overexpressing melanoma cells (A375M2 and SK-Mel-147), and strongly suppresses the Rho-dependent invasion by PC-3 cells.  CCG-1423 in combination with LY294002 enhances differentiation of mouse embryonic stem cells into intermediate mesoderm through BMP7-positive cells.  In H9c2 cells, CCG-1423 inhibits MRTF nuclear localization, and completely blocks STARS proximal reporter activity.  CCG-1423, as a Rho/MRTF/SRF pathway inhibitor, also represses both matrix-stiffness and TGF-beta-induced fibrogenesis in human colonic myofibroblasts. |
|Cell lines||Melanoma lines that overexpress RhoC (A375M2 and SK-Mel-147), low RhoC-expressing lines (A375 and SK-Mel-28), transformed (SW962, PC-3, and SKOV-3) and nontransformed (WI-38) cell lines.|
|Incubation Time||72 hours|
|Method||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.|
Data from [Data independently produced by , , Cell Signal, 2017, 31:87-95]
Cells were treated with CCG-1423 for 48 h. CCG-1423 blocked the nuclear translocation of MRTF-A.
Data from [Data independently produced by , , Cellular Signalling, 2017, 31:87-95.]
CCG-1423 blocked the nuclear translocation of MRTF-A.
Transcription of HOTAIR is regulated by RhoC-MRTF-A-SRF signaling pathway in human breast cancer cells. [He H, et al. Cell Signal, 2017, 31:87-95]PubMed: 28069441
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