| (S)-CCG-1423Rho inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
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| Cas No. | SDF | Download SDF | |
| Chemical Name | (S)-N-((1-((4-chlorophenyl)amino)-1-oxopropan-2-yl)oxy)-3,5-bis(trifluoromethyl)benzamide | ||
| Canonical SMILES | O=C(NO[C@@H](C)C(NC1=CC=C(Cl)C=C1)=O)C2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2 | ||
| Formula | C18H13ClF6N2O3 | M.Wt | 454.8 |
| 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) [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 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 [2].
References:[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.
