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Mifepristone (RU486) Progesterone Receptor Antagonist

Name: Mifepristone (RU486)
Brand: Selleck Chemicals
SKU: S2606
Availability: InStock
Rating: 5 (35 reviews)

Cat.No.S2606

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 (RU486) can be used to induce animal models of Spontaneous Abortion.

Chemical Structure

Molecular Weight: 429.59

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 100.00%

100.00

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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description
CHO-K1 cells	Function assay		Inhibition of CHO-K1 cells expressing glucocorticoid receptor, IC50=8e-06 μM
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
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
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
CV-1 cells	Function assay		Antagonistic activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells, IC50=0.00018 μM
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
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
SW1353 cells	Function assay		Binding affinity to glucocorticoid receptor in SW1353 cells by whole-cell binding assay, Ki=0.00082 μM
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
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
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
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
NIH3T3 cells	Function assay		In vitro antagonist potency in transactivation assay in NIH3T3 cells expressing glucocorticoid receptor, IC50=0.0022 μM
CHO cells	Function assay		Inhibition of Dexamethasone stimulated transcriptional activity in CHO cells expressing glucocorticoid receptor, IC50=0.005 μM
hGRAF cells	Function assay		Inhibition of human GR expressed in hGRAF cells, Ki=0.005 μM
COS-1	Function assay		Binding affinity for human androgen receptor in transiently-transfected COS-1 cells, Ki=0.022 μM
rat hepatocytes	Function assay		Inhibition of dexamethasone-induced GR-mediated tyrosine amino transferase activity in rat hepatocytes, IC50=0.27 μM
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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	429.59	Formula	C₂₉H₃₅NO₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	84371-65-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	C-1073, RU 38486			Smiles	CC#CC1(CCC2C1(CC(C3=C4CCC(=O)C=C4CCC23)C5=CC=C(C=C5)N(C)C)C)O

Solubility

In vitro
Batch:

DMSO : 85 mg/mL (197.86 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 85 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.500mg/ml (10.48mM)	Taking the 1 mL working solution as an example, add 50 μL of 90 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	6.000mg/ml (13.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 120 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.530mg/ml (1.23mM)	Taking the 1 mL working solution as an example, add 50 μL of 10.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features	Mifepristone is the first approved medication for patients with endogenous cushing
Targets/IC₅₀/Ki	Bcl-2 ^[5] Progesterone receptor ^[1] (T47D cells) 0.2 nM Glucocorticoid receptor ^[1] (A549 cells) 2.6 nM
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, this compound also blocks progesterone induction of alkaline phosphatase activity in the human breast cancer cell line T47D. ^[1] It 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 this chemical 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 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
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] This compound 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]
References	[1] https://pubmed.ncbi.nlm.nih.gov/16806946/ [2] https://pubmed.ncbi.nlm.nih.gov/17545545/ [3] https://pubmed.ncbi.nlm.nih.gov/22131096/ [4] https://pubmed.ncbi.nlm.nih.gov/17466516/ [5] https://pubmed.ncbi.nlm.nih.gov/31262976/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-AKT / AKT / p-ERK / ERK MMP-2 / MMP-9 / COX-2 / VEGF		28938623

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06394999	Not yet recruiting	Female Contraception	Leiden University Medical Center\|Karolinska Institutet\|Women on Waves\|Children''s Investment Fund Foundation	September 2024	Phase 3
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

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