Mifepristone (RU486, C-1073, RU 38486, Mifegyne) is a remarkably active antagonist ofprogesterone receptorandglucocorticoid receptorwithIC50of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cellautophagyandapoptosis, decreasesBcl-2level and increa In vitro
Mifepristone inhibit corticoid-induced transcription from a glucocorticoid response element (GRE)-linked luciferase reporter gene in the human lung carcinoma cell line A549. Moreover, Mifepristone also blocks progesterone induction of alkaline phosphatase activity in the human breast cancer cell line T47D. Mifepristone inhibits ovarian cancer cell growth of SK-OV-3 and OV2008 with IC50 of 6.25 μM and 6.91 μM, respectively. A recent study shows that Mifepristone induces caspase-1 over expression both in differentiated and undifferentiated caspase-1-embryonic stem cells.
In vivo
Mifepristone can impair the growth of SK-OV-3 tumors in immunosuppressed mice at 0.5 mg/day and 1 mg/day. Mifepristone inhibits the prostate weight significantly in the highest doses in vivo, and inhibits growth of the prostate gland produced by dihydrotestosterone (DHT) to a greater extent than the induction of atrophy and cell death in rats. Cell Data
