CCG-222740 is a Rho/MRTF pathway inhibitor. CCG-222740 decreases the activation of stellate cells in vitro and in vivo, by reducing the levels of alpha smooth muscle actin(α-SMA) expression.
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Product Description
Information
CCG-222740 CCG-222740 is a Rho/MRTF pathway inhibitor. CCG-222740 decreases the activation of stellate cells in vitro and in vivo, by reducing the levels of alpha smooth muscle actin(α-SMA) expression.
Targets
Rho ; α-SMA
In vitro
CCG-222740 increases the protein levels of p27 and decreased cyclin D1. CCG-222740 treatment decreased cell viability of CAFs, with an IC50 of~10 μM, as measured by the MTT assay. In pancreatic cancer, CAFs are one of the main producers of matrix proteins, including several collagen isoforms. The Rho/MRTF pathway inhibitor CCG-222740 decreases the levels of collagens I, 2a and IV, as well as α-SMA in the CAFsIn cancer cells. CCG-222740 treatment leads to the exclusion of MRTF from the nucleus. .
In vivo
CCG-222740 significantly reduces α-SMA levels in the pancreas of caerulein- stimulated KC mice.
This compound belongs to the class of organic compounds known as 1-benzoylpiperidines. These are compounds containing a piperidine ring substituted at the 1-position with a benzoyl group.
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1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
