CCG-1423

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Technical Data

Molecular Weight 454.75 Storage powder
Formula

C18H13ClF6N2O3

in solvent
CAS No. 285986-88-1 Synonyms N/A
Solubility (25°C) * In vitro DMSO 90 mg/mL (197.91 mM)
Ethanol 4 mg/mL warmed (8.79 mM)
Water Insoluble
In vivo
* <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.
Chemical Name N-(1-(4-chlorophenylamino)-1-oxopropan-2-yloxy)-3,5-bis(trifluoromethyl)benzamide

Biological Activity

Description CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription.
Targets
RhoA [1]
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. [1] CCG-1423 in combination with LY294002 enhances differentiation of mouse embryonic stem cells into intermediate mesoderm through BMP7-positive cells. [2] In H9c2 cells, CCG-1423 inhibits MRTF nuclear localization, and completely blocks STARS proximal reporter activity. [3] CCG-1423, as a Rho/MRTF/SRF pathway inhibitor, also represses both matrix-stiffness and TGF-beta-induced fibrogenesis in human colonic myofibroblasts. [4]
In vivo
Features  

Protocol (Only for Reference)

Cell Assay: [1]

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.
Concentrations 300 nM
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.
 

References

Customer Product Validation

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.

CCG-1423 has been referenced in 1 publications.

PLEASE KEEP THE PRODUCT UNDER -20°C FOR LONG-TERM STORAGE.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.

Specific storage and handling information for each product is indicated on the product datasheet. Most Selleck products are stable under the recommended conditions. Products are sometimes shipped at a temperature that differs from the recommended storage temperature. Short-term storage of many products are stable in the short-term at temperatures that differ from that required for long-term storage.
We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt of the product, follow the storage recommendations on the product data sheet.

Chemical Structure

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