An inhibitor of the Rho/MRTF/SRF transcriptional pathway
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CCG-232601 is an inhibitor of the Rho/MRTF/SRF transcriptional pathway and a derivative of CCG-203971 . CCG-232601 inhibits MRTF-dependent transcription in HEK293T cells (IC50 = 0.55 µM in a luciferase reporter assay). It also reduces expression of α-smooth muscle actin (α-SMA) in TGF-β-stimulated human dermal fibroblasts to 31% of control when used at a concentration of 10 µM. CCG-232601 (50 mg/kg) inhibits increases in dermal thickness and hydroxyproline content in a mouse model of dermal fibrosis induced by bleomycin .
3'-Azido-3'-deoxythymidine β-D-glucuronide (sodium salt)
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