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.
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. [1].
CCG-222740 significantly reduces α-SMA levels in the pancreas of caerulein- stimulated KC mice.[1]
[1] Ana S Leal,et al.Sci Rep.2019; 9(1): 7072.