|(S)-CCG-1423 Rho inhibitor|
Sample solution is provided at 25 µL, 10mM.
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|Cas No.||SDF||Download SDF|
|Canonical SMILES||O=C(NO[[email protected]@H](C)C(NC1=CC=C(Cl)C=C1)=O)C2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2|
|Solubility||≤0.25mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide||Storage||Store at -20°C|
|Physical Appearance||A crystalline solid||Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
(S)-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) .
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 .
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 .
The S-isomer of CCG-1423 inhibited MRTF-A-dependent cellular events, including SRF-mediated gene expression and cell migration. The efficacy of (S)-CCG-1423 was more potent than the R-isomer .
 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.
 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.