(R)-CCG-1423

- Overview
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    Background
    
    (R)-CCG-1423 is a stereoisomer of CCG-1423. CCG-1423 is a Rho inhibitor involved in blocking signaling through myocardin-related transcription factor A (MRTF-A) and serum response factor (SRF) [1]. The Rho family of small GTPases plays an important role in cancer metastasis. Up-regulation of RhoA or RhoC has been associated with a poor clinical outcome. Rho GTPases are important for the actin cytoskeleton. The RhoA family plays an important role in multiple cellular processes central to tumor growth and metastasis [1].CCG-14223 was an inhibitor for Rho/SRF pathway and displayed activity in several in vitro cancer cell functional assays. In PC-3 prostate cancer cells, CCG-1423(< 1 μmol/L) potently inhibited lysophosphatidic acid–induced DNA synthesis. CCG-1423 inhibited the growth of RhoC-overexpressing melanoma lines (A375M2 and SK-Mel-147) at nanomolar concentrations. CCG-1423 selectively stimulated apoptosis of the metastasis-prone, RhoC-overexpressing melanoma cell line (A375M2) when compared with the parental cell line (A375). CCG-1423 inhibited Rho-dependent invasion by PC-3 prostate cancer cells [1]. The R-isomer of CCG-1423 inhibited MRTF-A-dependent cellular events, including SRF-mediated gene expression and cell migration. The efficacy of (R)-CCG-1423 was less potent than the S-isomer [2].
    
    [1] Evelyn C R, Wade S M, Wang Q, et al. CCG-1423: a small-molecule inhibitor of RhoA transcriptional signaling[J]. Molecular cancer therapeutics, 2007, 6(8): 2249-2260.
    [2] Watanabe B, Minami S, Ishida H, et al. Stereospecific inhibitory effects of ccg-1423 on the cellular events mediated by myocardin-related transcription factor a[J]. PloS one, 2015, 10(8): e0136242.
- Properties
  - Alternative Name
    
    (R)-N-((1-((4-chlorophenyl)amino)-1-oxopropan-2-yl)oxy)-3,5-bis(trifluoromethyl)benzamide
    
    Molecular Formula
    
    C18H13ClF6N2O3
    
    Molecular Weight
    
    454.8
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤0.25mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

(R)-CCG-1423

Background

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