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CCG-1423 is a small-molecule inhibitor of RhoA transcriptional signaling. 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.
In H9c2 cells, CCG-1423 inhibits MRTF nuclear localization, and completely blocks STARS proximal reporter activity. In vivo, pharmacological SRF inhibition by CCG-1423 reduced nuclear MKL1 and improved glucose uptake and tolerance in insulin-resistant mice.
J Nanobiotechnology. 2024 May 3;22(1):219.
Migrasomes from adipose derived stem cells enrich CXCL12 to recruit stem cells via CXCR4/RhoA for a positive feedback loop mediating soft tissue regeneration
CCG-1423 purchased from AbMole
Cell Experiment | |
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Cell lines | Overexpress RhoC melanoma lines (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 |
Preparation 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. |
Concentrations | 300 nM |
Incubation time | 72 hours |
Animal Experiment | |
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Animal models | |
Formulation | |
Dosages | |
Administration |
Molecular Weight | 454.75 |
Formula | C18H13ClF6N2O3 |
CAS Number | 285986-88-1 |
Solubility (25°C) | DMSO: ≥ 40 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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