Home Endocrinology & Hormones Estrogen/progestogen Receptor antagonist - Glucocorticoid Receptor antagonist - Bcl-2 inhibitor - Autophagy activator - Apoptosis related activator Mifepristone For research use only.

Mifepristone

Synonyms: RU486, C-1073, RU 38486, RU-486

Mifepristone 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.

Mifepristone Chemical Structure

Mifepristone Chemical Structure

CAS: 84371-65-3

Selleck's Mifepristone has been cited by 27 Publications

1 Customer Review

Purity & Quality Control

Batch: Purity: 100.00%
100.00

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO-K1 cells Function assay Inhibition of CHO-K1 cells expressing glucocorticoid receptor, IC50=8e-06 μM 15456242
T47D-C124 cells Function assay 24 h Antagonist activity at progesterone receptor in human T47D-C124 cells transfected with luciferase gene linked to MMTV promoter assessed as inhibition of progesterone-induced luciferase transactivation activity after 24 hrs, IC50=2.1e-05 μM 19216549
neuroblastoma cells Function assay In vitro antagonist potency in transactivation assay in neuroblastoma cells expressing human PR-B progesterone receptor, IC50=2.5e-05 μM 11150172
T47D cells Function assay 48 h Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity after 48 hrs, IC50=4.5e-05 μM 19216549
CV-1 cells Function assay Antagonistic activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells, IC50=0.00018 μM 9484511
HEK293 cells Function assay Antagonist activity against glucocorticoid receptor (unknown origin) expressed in HEK293 cells by GRE-dependent luciferase reporter gene assay, IC50=0.000298 μM 26218343
COS7 cells Function assay Antagonist activity at cloned glucocorticoid receptor-ligand binding domain expressed in african green monkey COS7 cells by GAL4 luciferase reporter assay, IC50=0.0006 μM 18504132
SW1353 cells Function assay Binding affinity to glucocorticoid receptor in SW1353 cells by whole-cell binding assay, Ki=0.00082 μM 17822897
A549 cells Function assay Antagonist activity at human glucocorticoid receptor assessed as inhibition of corticoid-induced transcription in human A549 cells by GRE-linked luciferase reporter gene assay, IC50=0.0016 μM 17317167
A549 cells Function assay 16 h Antagonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of corticoid-induced transcription after 16 hrs by glucocorticoid response element-driven luciferase reporter gene assay, IC50=0.0016 μM 19217285
rat H4-IIE cells Function assay 1 h Antagonist activity against glucocorticoid receptor in rat H4-IIE cells assessed as inhibition of dexamethasone-induced receptor transactivation pre-incubated for 1 hr before dexamethasone addition and measured 24 hrs post dexamethasone stimulation by tyrosine aminotransferase enzyme assay, IC50=0.00194 μM 26218343
HeLa cells Function assay Effective concentration against inhibition of Dexamethasone induced glucocorticoid receptor transactivation of mouse mammary tumor virus luciferase gene in HeLa cells, EC50=0.002 μM 16112571
NIH3T3 cells Function assay In vitro antagonist potency in transactivation assay in NIH3T3 cells expressing glucocorticoid receptor, IC50=0.0022 μM 11150172
CHO cells Function assay Inhibition of Dexamethasone stimulated transcriptional activity in CHO cells expressing glucocorticoid receptor, IC50=0.005 μM 12824023
hGRAF cells Function assay Inhibition of human GR expressed in hGRAF cells, Ki=0.005 μM 17070047
COS-1 Function assay Binding affinity for human androgen receptor in transiently-transfected COS-1 cells, Ki=0.022 μM 9484511
rat hepatocytes Function assay Inhibition of dexamethasone-induced GR-mediated tyrosine amino transferase activity in rat hepatocytes, IC50=0.27 μM 15261266
human K562/R7 cells Function assay 72 h Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay, IC50=0.9 μM 25634041
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Biological Activity

Description Mifepristone 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
Targets
Bcl-2 [5] Progesterone receptor [1]
(T47D cells)		 Glucocorticoid receptor [1]
(A549 cells)
0.2 nM 2.6 nM
In vitro
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. [1] Mifepristone inhibits ovarian cancer cell growth of SK-OV-3 and OV2008 with IC50 of 6.25 μM and 6.91 μM, respectively. [2] A recent study shows that Mifepristone induces caspase-1 over expression both in differentiated and undifferentiated caspase-1-embryonic stem cells. [3]
Kinase Assay 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
Cell Research Cell lines OV2008 and SK-OV-3 cells
Concentrations 0-20 μM
Incubation Time 24 hours
Method

Cell growth is evaluated in various ovarian cancer cell lines that are subjected to dose-response or time course treatments. Media containing each of the doses of fresh steroids is replaced every 24 hours. Control groups of cells are treated with vehicle ethanol at a final concentration of less than 0.05%. Number of viable cells is evaluated by trypsinization and counting in a hemocytometer chamber using trypan blue dye exclusion. Experiments are conducted in media without phenol red and supplemented with charcoal extracted fetal bovine serum, or media containing unextracted serum and having phenol red. Similar results are obtained with both media preparations; therefore, after performing the growth curves, all subsequent experiments are conducted using media with unextracted serum and in the presence of phenol red. When indicated, the proliferation IC50s are calculated using software designed to study drug interaction.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-AKT / AKT / p-ERK / ERK MMP-2 / MMP-9 / COX-2 / VEGF 28938623
In Vivo
In vivo

Mifepristone can impair the growth of SK-OV-3 tumors in immunosuppressed mice at 0.5 mg/day and 1 mg/day. [2] 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. [4]
Animal Research Animal Models SK-OV-3 ovarian cancer cells are injected into immunosuppressed mice.
Dosages 0.5 or 1 mg/day
Administration Implanted s.c. with pellets
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05177510 Recruiting Labor Induced Chelsea and Westminster NHS Foundation Trust August 25 2023 Phase 3
NCT04905251 Recruiting Medical Abortion Linepharma International LTD February 22 2022 --
NCT05062174 Withdrawn BRCA1 Mutation|High-grade Serous Ovarian Cancer|TNBC - Triple-Negative Breast Cancer Indiana University|Breast Cancer Research Foundation November 1 2021 --
NCT04588688 Terminated Central Adrenal Insufficiency|Mifepristone Tobias Else|Corcept Therapeutics|University of Michigan May 5 2021 Phase 2
NCT03659045 Completed Abortion-Related Disorders Assistance Publique Hopitaux De Marseille January 15 2019 Not Applicable
NCT03258372 Completed Healthy Corcept Therapeutics August 16 2017 Phase 1

Chemical lnformation & Solubility

Molecular Weight 429.59 Formula

C29H35NO2
CAS No. 84371-65-3 SDF Download Mifepristone SDF
Smiles CC#CC1(CCC2C1(CC(C3=C4CCC(=O)C=C4CCC23)C5=CC=C(C=C5)N(C)C)C)O
Storage (From the date of receipt)

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DMSO : 85 mg/mL ( (197.86 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 85 mg/mL

Water : Insoluble


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