CCG-1423 (CCG1423) is a small-molecule inhibitor of RhoA transcriptional signaling and serum response factor (SRF), blocks transcription activated by MKL1, disrupts transcriptional responses of the Rho pathway in cancer.
CCG-1423 blocks transcription activated by MKL1, but not that induced by SRF-VP16 or GAL4-VP16.
CCG-1423 inhibits lysophosphatidic acid-induced DNA synthesis in PC-3 prostate cancer cells, and inhibits the growth of RhoC-overexpressing melanoma lines (A375M2 and SK-Mel-147) at nanomolar concentrations.
CCG-1423 is less active on related lines (A375 and SK-Mel-28) that express lower levels of Rho.
CCG-1423 selectively stimulates apoptosis of the metastasis-prone, RhoC-overexpressing melanoma cell line (A375M2) compared with the parental cell line (A375).
CCG-1423 inhibits Rho-dependent invasion by PC-3 prostate cancer cells, wherea it does not affect the Gαi-dependent invasion by the SKOV-3 ovarian cancer cell line.