Name: Mifepristone
Brand: Selleck Chemicals
SKU: S2606
Rating: 5 (27 reviews)

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

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

Mifepristone Related Products

Related Targets	Estrogen receptor Progesterone receptor ERR	Click to Expand
Related Compound Libraries	FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Exosome Secretion Related Compound Library Human Hormone Related Compound Library	Click to Expand

Signaling Pathway

Estrogen/progestogen Receptor Signaling Pathway

Choose Selective Estrogen/progestogen Receptor Inhibitors

Cell Data

Cell Lines	Assay Type	Incubation Time	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
Click to View More Cell Line Experimental Data

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
Kinase Assay	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
Experimental Result Images	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

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Chemical Information & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

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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In vivo
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