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    CCG-1423
    CCG-1423

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1567
    CAS #: 285986-88-1Purity ≥98%

    Description: CCG-1423 is a novel, potent and specific small-molecule inhibitor of RhoA signaling pathway, which inhibits SRF-mediated transcription. CCG-1423 displays activity in several in vitro cancer cell functional assays. CCG-1423 potently (<1 mumol/L) inhibits lysophosphatidic acid-induced DNA synthesis in PC-3 prostate cancer cells, and whereas it inhibits the growth of RhoC-overexpressing melanoma lines (A375M2 and SK-Mel-147) at nanomolar concentrations, it is less active on related lines (A375 and SK-Mel-28) that express lower levels of Rho. 

    References: Mol Cancer Ther. 2007 Aug;6(8):2249-60; Biochem Biophys Res Commun. 2010 Mar 19;393(4):877-82.

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    Molecular Weight (MW)454.75
    FormulaC18H13ClF6N2O3
    CAS No.285986-88-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 90 mg/mL (197.9 mM)
    Water: <1 mg/mL
    Ethanol: 4 mg/mL (8.8 mM)
    Other infoChemical Name: N-((1-((4-chlorophenyl)amino)-1-oxopropan-2-yl)oxy)-3,5-bis(trifluoromethyl)benzamide
    InChi Key: DSMXVSGJIDFLKP-UHFFFAOYSA-N
    InChi Code: InChI=1S/C18H13ClF6N2O3/c1-9(15(28)26-14-4-2-13(19)3-5-14)30-27-16(29)10-6-11(17(20,21)22)8-12(7-10)18(23,24)25/h2-9H,1H3,(H,26,28)(H,27,29)
    SMILES Code: O=C(NOC(C)C(NC1=CC=C(Cl)C=C1)=O)C2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2
    SynonymsCCG1423; CCG-1423; CCG 1423


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    In Vitro

    In vitro activity: 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.


    Kinase Assay: CCG-1423 has nanomolar to low micromolar potency as well as selectivity toward Rho-overexpressing and invasive cancer cell lines for inhibition of DNA synthesis, cell growth, and/or invasion. Caspase-3 activation in the highly metastatic RhoC-overexpressing A375M2 melanoma cell line was enhanced by CCG-1423 whereas a smaller increase was seen with the parental A375 cell line, whereas just the opposite pattern was seen with daunorubicin.


    Cell Assay: 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.

    In VivoPharmacological SRF inhibition by CCG-1423 reduced nuclear MKL1 and improved glucose uptake and tolerance in insulin-resistant mice in vivo.
    Animal modelInsulin-resistant mice
    Formulation & DosageN/A
    ReferencesMol Cancer Ther. 2007 Aug;6(8):2249-60; Biochem Biophys Res Commun. 2010 Mar 19;393(4):877-82.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     CCG-1423


    Forskolin-inhibits CCN1 expression via an MKL1 and SRF-dependent mechanism. J Mol Cell Cardiol. 2014 Nov 18;79C:157-168.

     CCG-1423


    Binding of SRF to the STARS promoter. C. The SRF inhibitor CCG-1423 (1 µM) abolished STARS −365/+60 promoter-reporter activity in H9c2 cells (n = 3 experiments, in triplicates).   2012;7(7):e40966.



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