Mifepristone

Catalog No.S2606 Synonyms: RU486, C-1073

Mifepristone Chemical Structure

Molecular Weight(MW): 429.59

Mifepristone is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively.

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In DMSO USD 230 In stock
USD 60 In stock
USD 190 In stock
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Cited by 5 Publications

1 Customer Review

  • Myogenic differentiation assay to determine the GR specificity of DEX by using RU-486 (10 uM). Immunofluorescence detection of MyHC (red) and DAPI counterstaining of nuclei (blue) was used to detect myotubes. The scale bar is 50 um.

    PLoS One 2014 9(8), e105528. Mifepristone purchased from Selleck.

Purity & Quality Control

Choose Selective Estrogen/progestogen Receptor Inhibitors

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.
Features Mifepristone is the first approved medication for patients with endogenous cushing's syndrome.
Targets
Progesterone receptor [1]
(T47D cells)
Glucocorticoid receptor [1]
(A549 cells)
0.2 nM 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, 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO-K1 cells NG\aRllHfW6ldHnvckBie3OjeR?= MUPJcohq[mm2aX;uJI9nKEOKTz3LNUBk\WyuczDlfJBz\XO|aX7nJIdtfWOxY3;yeIlkd2mmIILlZ4VxfG:{LDDJR|UxRTinLUC2JO69VQ>? NHLR[HUyPTR3NkK0Ni=>
T47D-C124 cells MUDGeY5kfGmxbjDhd5NigQ>? NHz5Om4zPCCq M1rxSmFvfGGpb37pd5Qh[WO2aY\peJkh[XRicILv[4V{fGW{b37lJJJm[2WydH;yJIlvKGi3bXHuJHQ1P0RvQ{GyOEBk\WyuczD0doFve2[nY4Tl[EB4cXSqIHz1Z4ln\XKjc3Wg[4Vv\SCuaX7r[YQhfG9iTV3UWkBxem:vb4TldkBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJJBzd2enc4Tldo9v\S2rbnT1Z4VlKGy3Y3nm[ZJie2VidILhcpNi[3SrdnH0bY9vKGGldHn2bZR6KGGodHXyJFI1KGi{czygTWM2OD1{LkHlMVA2KM7:TR?= Ml7rNVkzOTZ3NEm=
neuroblastoma cells MlX0SpVv[3Srb36gZZN{[Xl? MoTaTY4hfmm2cn:gZY51[WexbnnzeEBxd3SnbnP5JIlvKHS{YX7zZYN1cX[jdHnvckBie3OjeTDpckBv\XW{b3LsZZN1d22jIHPlcIx{KGW6cILld5NqdmdiaIXtZY4hWFJvQjDwdo9o\XO2ZYLvcoUhemWlZYD0c5ItKEmFNUC9Nk42\S1yNTFOwG0> MWexNVE2ODF5Mh?=
T47D cells M4DyWGZ2dmO2aX;uJIF{e2G7 MojkOFghcA>? NF\4W5lCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IIDyc4dme3Sncn;u[UBz\WOncITvdkBqdiCqdX3hckBVPDeGIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YheHKxZ3XzeIVzd26nLXnu[JVk\WRiYXzrZYxqdmVicHjvd5Bp[XSjc3WgZYN1cX[rdImgZYZ1\XJiNEigbJJ{NCCLQ{WwQVQvPWVvMEWg{txO MkDONVkzOTZ3NEm=
CV-1 cells M4XoNmZ2dmO2aX;uJIF{e2G7 NUH6UmZYSW62YXfvcol{fGmlIHHjeIl3cXS7IHHnZYlve3RiaIXtZY4heHKxZ3XzeIVzd26nIILlZ4VxfG:{IFKgLIhRWi2EKTDpckBkdy22cnHud4Zm[3SnZDDDWk0yKGOnbHzzMEBKSzVyPUCuNFAxOThizszN MlvMPVQ5PDVzMR?=
HEK293 cells MWXGeY5kfGmxbjDhd5NigQ>? MXrBcpRi\2:waYP0JIFkfGm4aYT5JIFo[Wmwc4Sg[4x2[2:lb4L0bYNwcWRicnXj[ZB1d3JiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{KGK7IFfSSU1l\XCnbnTlcpQhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDJR|UxRTBwMECwNlk5KM7:TR?= NVnjc4RpOjZ{MUizOFM>
COS7 cells NVm0V2N6TnWwY4Tpc44h[XO|YYm= NVvVTpduSW62YXfvcol{fCCjY4Tpeol1gSCjdDDjcI9v\WRiZ3z1Z49kd3K2aXPvbYQhemWlZYD0c5IudGmpYX7kJIJqdmSrbneg[I9u[WmwIHX4dJJme3OnZDDpckBi\nKrY3HuJIdz\WWwIH3vcotmgSCFT2O3JINmdGy|IHL5JGdCVDRibIXjbYZmemG|ZTDy[ZBwenSncjDhd5NigSxiSVO1NF0xNjByME[g{txO MmfhNVg2ODRzM{K=
SW1353 cells MlvySpVv[3Srb36gZZN{[Xl? MoHrRolv\GmwZzDh[oZqdmm2eTD0c{BodHWlb3PvdpRq[2:rZDDy[YNmeHSxcjDpckBUXzF|NUOgZ4VtdHNiYomge4hwdGVvY3XscEBjcW6maX7nJIF{e2G7LDDLbV0xNjByMEiyJO69VQ>? M4e4VFE4QDJ{OEm3
A549 cells NUXuSVZkTnWwY4Tpc44h[XO|YYm= NHvGSnlCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IHj1cYFvKGeudXPvZ49zfGmlb3nkJJJm[2WydH;yJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZ49zfGmlb3nkMYlv\HWlZXSgeJJidnOlcnnweIlwdiCrbjDoeY1idiCDNUS5JINmdGy|IHL5JGdTTS2uaX7r[YQhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDJR|UxRTBwMECxOkDPxE1? MoDCNVc{OTdzNke=
A549 cells M3vkOWZ2dmO2aX;uJIF{e2G7 NHLJd|gyPiCq NWKyTYN2SW62YXfvcol{fCCjY4Tpeol1gSCjdDDncJVkd2OxcoTpZ49q\CC{ZXPldJRweiCrbjDoeY1idiCDNUS5JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3;yeIlkd2mmLXnu[JVk\WRidILhcpNkemmydHnvckBi\nSncjCxOkBpenNiYomg[4x2[2:lb4L0bYNwcWRicnXzdI9ve2ViZXzlcYVvfC2mcnn2[Y4hdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDJR|UxRTBwMECxOkDPxE1? MVuxPVIyPzJ6NR?=
rat H4-IIE cells NIOzWYxHfW6ldHnvckBie3OjeR?= M3m5blEhcA>? NYTXO5VwSW62YXfvcol{fCCjY4Tpeol1gSCjZ3HpcpN1KGeudXPvZ49zfGmlb3nkJJJm[2WydH;yJIlvKHKjdDDIOE1KUUViY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBl\XijbXX0bIF{d26nLXnu[JVk\WRicnXj[ZB1d3JidILhcpNi[3SrdnH0bY9vKHC{ZT3pcoN2[mG2ZXSg[o9zKDFiaIKgZoVnd3KnIHTlfIFu\XSqYYPvcoUh[WSmaYTpc44h[W6mIH3lZZN2emWmIEK0JIhzeyCyb4P0JIRmgGGvZYToZZNwdmVic4TpcZVt[XSrb36gZpkhfHm{b4PpcoUh[W2rbn;0doFve2[ncnHz[UBmdnq7bXWgZZN{[XluIFnDOVA:OC5yMEG5OEDPxE1? NXXFWIVoOjZ{MUizOFM>
HeLa cells NVToRmJvTnWwY4Tpc44h[XO|YYm= NEjLVYZG\m[nY4TpeoUh[2:wY3XueJJifGmxbjDh[4FqdnO2IHnubIljcXSrb36gc4YhTGW6YX3leIhie2:wZTDpcoR2[2WmIHfseYNw[2:{dHnjc4llKHKnY3XweI9zKHS{YX7zZYN1cX[jdHnvckBw\iCvb4Xz[UBu[W2vYYL5JJR2dW:{II\pdpV{KGy3Y3nm[ZJie2ViZ3Xu[UBqdiCKZVzhJINmdGy|LDDFR|UxRTBwMECyJO69VQ>? MlftNVYyOTJ3N{G=
NIH3T3 cells NXTFdmtHTnWwY4Tpc44h[XO|YYm= MVnJckB3cXS{bzDhcpRi\2:waYP0JJBwfGWwY4mgbY4hfHKjboPhZ5RqfmG2aX;uJIF{e2G7IHnuJG5KUDOWMzDj[YxteyCneIDy[ZN{cW6pIHfseYNw[2:{dHnjc4llKHKnY3XweI9zNCCLQ{WwQVAvODB{MjFOwG0> MVqxNVE2ODF5Mh?=
CHO cells NF;iU|hHfW6ldHnvckBie3OjeR?= MX;Jcohq[mm2aX;uJI9nKESneHHt[ZRp[XOxbnWgd5RqdXWuYYTl[EB1emGwc3PybZB1cW:wYXygZYN1cX[rdImgbY4hS0iRIHPlcIx{KGW6cILld5NqdmdiZ3z1Z49kd3K2aXPvbYQhemWlZYD0c5ItKEmFNUC9NE4xODVizszN NGXSWnIyOjh{NECyNy=>
hGRAF cells MVzGeY5kfGmxbjDhd5NigQ>? NFqyPXpKdmirYnn0bY9vKG:oIHj1cYFvKEeUIHX4dJJme3OnZDDpckBpT1KDRjDj[YxteyxiS3m9NE4xODVizszN NH76fXQyPzB5MEC0Oy=>
COS-1 M3zMVWZ2dmO2aX;uJIF{e2G7 M3jyS2JqdmSrbnegZYZncW6rdImg[o9zKGi3bXHuJIFv\HKxZ3XuJJJm[2WydH;yJIlvKHS{YX7zbYVvfGy7LYTyZY5{\mWldHXkJGNQWy1zIHPlcIx{NCCNaU2wMlAzOiEQvF2= MmnRPVQ5PDVzMR?=
rat hepatocytes MUnGeY5kfGmxbjDhd5NigQ>? M4DQSGlvcGmkaYTpc44hd2ZiZHX4ZY1mfGijc3;u[U1qdmS3Y3XkJGdTNW2nZHnheIVlKHS7cn;zbY5mKGGvaX7vJJRz[W6|ZnXyZZNmKGGldHn2bZR6KGmwIILheEBp\XCjdH;jfZRmeyxiSVO1NF0xNjJ5IN88US=> NILRRW0yPTJ4MUK2Oi=>
human K562/R7 cells M{f5XGZ2dmO2aX;uJIF{e2G7 NFzMWJo4OiCq NUD6NWtuWG:2ZX70bYF1cW:wIH;mJIRwgG:{dXLpZ4lvNWmwZIXj[YQh[3m2b4TvfIlkcXS7IHHnZYlve3RiZH;4c5J2[mmlaX6tdoV{cXO2YX70JIh2dWGwIFu1OlIwWjdiY3XscJMh[XO|ZYPz[YQh[XNiZH;4c5J2[mmlaX6gTWM2OCCjdDCxJJVOKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE46KM7:TR?= MV6yOVY{PDB2MR?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AKT / AKT / p-ERK / ERK ; 

PubMed: 28938623     


SDF-1 was incapable of altering expression of Akt and ERK, but promoted Akt and ERK phosphorylation. Mifepristone suppressed the expression of Akt, ERK, p-Akt and p-ERK in a concentration-dependent manner, resulting in the decline of the p-Akt/Akt and p-ERK/ERK ratios. The immunoblot images and the related quantitative analysis were showed on the upper panel and lower panel, respectively.

MMP-2 / MMP-9 / COX-2 / VEGF ; 

PubMed: 28938623     


Mifepristone downregulated SDF-1-elevated protein levels of MMP-2, MMP-9, COX-2 and VEGF in a concentration-dependent manner. The immunoblot images and the related quantitative analysis were showed on the upper panel and lower panel, respectively.

28938623
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]

Protocol

Kinase Assay:[1]
- Collapse

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' buffered saline solution. Equal volumes (0.05 mL) of dilution buffer, assay buffer, and 1:20 substrate/enhancer mixture are then added. After 1-hour incubation in the dark at room temperature, the lysate is transferred to a white 96-well plate and luminescence is read using a LuminoSkan Ascen. A549 reporter assay: A549 human lung carcinoma cells are washed with OPTI-MEM I. The medium is removed and lipid–DNA complex solution (1.5 μg/mL of GRE-luciferase reporter DNA in 8.5 mL OPTI-MEM I plus 6 μL/mL DMRIE-C reagent in 8.5 mL OPTI-MEM I, combined, mixed and incubated at room temperature for 40 minutes) is overlayed onto the cells in a T160 flask. The cells are incubated for 16 hours at 37 °C in a CO2 incubator. The DNA-containing medium is removed and 30 mL of growth medium containing 5% (v/v) charcoal-treated fetal bovine serum is added. After 5-6 hours, the cells are seeded in 96-well plates and incubated overnight at 37 °C. Mifepristone is then added to each well followed by dexamethasone as a corticoid challenge. The cells are incubated for 24 hours. Luciferase assay buffer is added to each well and the cells are incubated for 30 minutes at room temperature. Luciferase activity is measured in a DYNEX Microlite plate on a TopCount.
Cell Research:[2]
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  • 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.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: SK-OV-3 ovarian cancer cells are injected into immunosuppressed mice.
  • Formulation: Constant release pellets (Innovative Research of America)
  • Dosages: 0.5 or 1 mg/day
  • Administration: Implanted s.c. with pellets
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 85 mg/mL (197.86 mM)
Ethanol 19 mg/mL (44.22 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 429.59
Formula

C29H35NO2

CAS No. 84371-65-3
Storage powder
in solvent
Synonyms RU486, C-1073

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID