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 (IC = 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 .
CCG-232601 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.
体外研究
CCG-232601 inhibits SRE.L activity with an IC50 of 0.55 µM.
体内研究
CCG-232601 (50 mg/kg; i.g.; intracutaneous injections of bleomycin; daily for 14 days) inhibits bleomycin-induced skin fibrosis in mice.
分子式
C24H20ClF2N3O2
分子量
455.88
CAS号
1922099-21-5
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO: 40 mg/mL (87.74 mM; Need ultrasonic and warming)