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CCG-1423

Cat. No. M8999
CCG-1423 Structure
Size Price Availability Quantity
10mg USD 65  USD65 In stock
50mg USD 200  USD200 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
Cell Experiment
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
Animal models
Formulation
Dosages
Administration
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Johnson LA, et al. Inflamm Bowel Dis. Novel Rho/MRTF/SRF inhibitors block matrix-stiffness and TGF-β-induced fibrogenesis in human colonic myofibroblasts.

[2] Chong NW, et al. PLoS One. STARS is essential to maintain cardiac development and function in vivo via a SRF pathway.

[3] Mae S, et al. Biochem Biophys Res Commun. Combination of small molecules enhances differentiation of mouse embryonic stem cells into intermediate mesoderm through BMP7-positive cells.

[4] Evelyn CR, et al. Mol Cancer Ther. CCG-1423: a small-molecule inhibitor of RhoA transcriptional signaling.

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