CCG-232601 Chemical Properties

Boiling point:

683.1±55.0 °C(Predicted)

Density 

1.39±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMF: 30 mg/ml; DMSO: 30 mg/ml; DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml

form 

A crystalline solid

pka

13.69±0.70(Predicted)

color 

White to off-white

CCG-232601 Usage And Synthesis

Description

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 .

Uses

CCG-232601 (compound 8f) is a potent and orally active Rho/MRTF/SRF transcriptional pathway inhibitor. CCG-232601 inhibits the development of Bleomycin-induced dermal fibrosis in mice. CCG-232601 has the potential for the research of antifibrotic for systemic scleroderma[1].

in vivo

References

[1] Hutchings KM, et al. Pharmacokinetic optimitzation of CCG-203971: Novel inhibitors of the Rho/MRTF/SRF transcriptional pathway as potential antifibrotic therapeutics for systemic scleroderma. Bioorg Med Chem Lett. 2017 Apr 15;27(8):1744-1749. DOI:10.1016/j.bmcl.2017.02.070