For research use only.
Catalog No.S2606 Synonyms: RU486, C-1073
CAS No. 84371-65-3
Mifepristone (RU486, C-1073) is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.
Selleck's Mifepristone has been cited by 12 publications
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|Description||Mifepristone (RU486, C-1073) is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.|
|Features||Mifepristone is the first approved medication for patients with endogenous cushing|
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. 
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. 
Glucocorticoid receptor (GR) antagonist activity, Progesterone receptor (PR) antagonist activity:T47D alkaline phosphatase assay: T47D human breast cancer cells are plated in 96-well tissue culture plates at 104 cells per well in assay medium [RPMI medium without phenol red containing 5% (v/v) charcoal-treated FBS and 1% (v/v) penicillin–streptomycin]. Two days later, the medium is decanted and Mifepristone or control is added at a final concentration of 0.1% (v/v) dimethylsulfoxide in fresh assay medium. Twenty-four hours later, an alkaline phosphatase assay is performed using a SEAP kit. The medium is decanted and the cells are fixed for 30 minutes at room temperature with 5% (v/v) formalin. The cells are washed once at room temperature with Hanks
-  Jiang W, et al. Bioorg Med Chem, 2006, 14(19), 6726-6732.
-  Goyeneche AA, et al. Clin Cancer Res, 2007, 13(11), 3370-3379.
-  Wang Y, et al. Stem Cells, 2012, 30(2), 169-179.
|In vitro||DMSO||85 mg/mL (197.86 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03258372||Completed||Drug: Mifepristone||Healthy||Corcept Therapeutics||August 16 2017||Phase 1|
|NCT03259542||Completed||Drug: Mifepristone 300 MG|Drug: Itraconazole 100 MG||Drug Interaction Potentiation|Healthy||Corcept Therapeutics||August 9 2017||Phase 1|
|NCT02985229||Completed||Drug: Mifepristone|Drug: Misoprostol||Medical Abortion||Gynuity Health Projects||October 2016||Phase 3|
|NCT02745093||Unknown status||Drug: Mifepristone|Drug: Misoprostol||Medical Abortion||Ibis Reproductive Health|Marie Stopes International||September 2016||Phase 4|
|NCT02570204||Completed||Behavioral: Self-assessment||Medical Abortion||Gynuity Health Projects||September 2015||Not Applicable|
|NCT02720991||Completed||Drug: Mifepristone|Drug: Sublingual misoprostol||Abortion 3 Months||Gynuity Health Projects|Hopital La Rabta||July 2014||Phase 4|
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