Mifepristone (RU486)

For research use only.

Catalog No.S2606 Synonyms: C-1073, RU 38486, Mifegyne

14 publications

Mifepristone (RU486) Chemical Structure

CAS No. 84371-65-3

Mifepristone (RU486, C-1073, RU 38486, Mifegyne) 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.

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Selleck's Mifepristone (RU486) has been cited by 14 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 (RU486) purchased from Selleck.

Purity & Quality Control

Choose Selective Estrogen/progestogen Receptor Inhibitors

Biological Activity

Description Mifepristone (RU486, C-1073, RU 38486, Mifegyne) 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

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 MmDCSpVv[3Srb36gZZN{[Xl? NV2yZWVDUW6qaXLpeIlwdiCxZjDDTG8uUzFiY3XscJMh\XiycnXzd4lv\yCpbIXjc4NwenSrY3;p[EBz\WOncITvdkwhUUN3ME24[U0xPiEQvF2= MXuxOVQ2PjJ2Mh?=
T47D-C124 cells M2LqbGZ2dmO2aX;uJIF{e2G7 MWSyOEBp NH\XXphCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IIDyc4dme3Sncn;u[UBz\WOncITvdkBqdiCqdX3hckBVPDeGLVOxNlQh[2WubIOgeJJidnOoZXP0[YQhf2m2aDDseYNq\mW{YYPlJIdmdmVibHnub4VlKHSxIF3NWHYheHKxbX;0[ZIh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBxem:pZYP0[ZJwdmVvaX7keYNm\CCudXPp[oVz[XOnIITyZY5{[WO2aY\heIlwdiCjY4Tpeol1gSCjZoTldkAzPCCqcoOsJGlEPTB;Mj6x[U0xPSEQvF2= M3;HT|E6OjF4NUS5
neuroblastoma cells M3vjZmZ2dmO2aX;uJIF{e2G7 MYfJckB3cXS{bzDhcpRi\2:waYP0JJBwfGWwY4mgbY4hfHKjboPhZ5RqfmG2aX;uJIF{e2G7IHnuJI5mfXKxYnzhd5RwdWFiY3XscJMh\XiycnXzd4lv\yCqdX3hckBRWi2EIIDyc4dme3Sncn;u[UBz\WOncITvdkwhUUN3ME2yMlVmNTB3IN88US=> NXvKU21YOTFzNUCxO|I>
T47D cells NXzFPHM4TnWwY4Tpc44h[XO|YYm= MkfVOFghcA>? Mk\tRY51[WexbnnzeEBi[3Srdnn0fUBifCCycn;n[ZN1\XKxbnWgdoVk\XC2b4KgbY4hcHWvYX6gWFQ4TCClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJJBzd2enc4Tldo9v\S2rbnT1Z4VlKGGua3HsbY5mKHCqb4PwbIF1[XOnIHHjeIl3cXS7IHHmeIVzKDR6IHjyd{whUUN3ME20MlVmNTB3IN88US=> MlW0NVkzOTZ3NEm=
CV-1 cells MoTISpVv[3Srb36gZZN{[Xl? M1zufGFvfGGpb37pd5Rq[yCjY4Tpeol1gSCjZ3HpcpN1KGi3bXHuJJBzd2enc4Tldo9v\SC{ZXPldJRweiCEIDjoVHIuSiliaX6gZ48ufHKjboPm[YN1\WRiQ2[tNUBk\WyuczygTWM2OD1yLkCwNFE5KM7:TR?= NYXVemNmQTR6NEWxNS=>
HEK293 cells M4W0XmZ2dmO2aX;uJIF{e2G7 M1T2N2FvfGGpb37pd5Qh[WO2aY\peJkh[WejaX7zeEBodHWlb3PvdpRq[2:rZDDy[YNmeHSxcjCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYomgS3JGNWSncHXu[IVvfCCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGlEPTB;MD6wNFAzQThizszN M{fDelI3OjF6M{Sz
COS7 cells NY\lW|dOTnWwY4Tpc44h[XO|YYm= MkDaRY51[WexbnnzeEBi[3Srdnn0fUBifCClbH;u[YQh\2y3Y3;jc5J1cWOxaXSgdoVk\XC2b4KtcIlo[W6mIHLpcoRqdmdiZH;tZYlvKGW6cILld5Nm\CCrbjDh[pJq[2GwIHfy[YVvKG2xbnvlfUBEV1N5IHPlcIx{KGK7IFfBUFQhdHWlaX\ldoF{\SC{ZYDvdpRmeiCjc4PhfUwhUUN3ME2wMlAxODZizszN NXq1c2trOTh3MESxN|I>
SW1353 cells M1LVO2Z2dmO2aX;uJIF{e2G7 MXfCbY5lcW6pIHHm[olvcXS7IITvJIdtfWOxY3;yeIlkd2mmIILlZ4VxfG:{IHnuJHNYOTN3MzDj[YxteyCkeTD3bI9t\S2lZXzsJIJqdmSrbnegZZN{[XluIFvpQVAvODByOEKg{txO MXexO|gzOjh7Nx?=
A549 cells NE[5R2xHfW6ldHnvckBie3OjeR?= MXvBcpRi\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJIdtfWOxY3;yeIlkd2mmIILlZ4VxfG:{IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3;yeIlkd2mmLXnu[JVk\WRidILhcpNkemmydHnvckBqdiCqdX3hckBCPTR7IHPlcIx{KGK7IFfSSU1tcW6tZXSgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCLQ{WwQVAvODBzNjFOwG0> Mn;HNVc{OTdzNke=
A549 cells M1\tW2Z2dmO2aX;uJIF{e2G7 MV6xOkBp NH3W[Y9CdnSjZ3;ubZN1KGGldHn2bZR6KGG2IHfseYNw[2:{dHnjc4llKHKnY3XweI9zKGmwIHj1cYFvKEF3NEmgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClb4L0bYNwcWRvaX7keYNm\CC2cnHud4NzcXC2aX;uJIFnfGW{IEG2JIhzeyCkeTDncJVkd2OxcoTpZ49q\CC{ZYPwc45{\SCnbHXt[Y51NWS{aY\lckBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFnDOVA:OC5yMEG2JO69VQ>? MYCxPVIyPzJ6NR?=
rat H4-IIE cells NV;5fFVtTnWwY4Tpc44h[XO|YYm= NIS5TIoyKGh? MnPTRY51[WexbnnzeEBi[3Srdnn0fUBi\2GrboP0JIdtfWOxY3;yeIlkd2mmIILlZ4VxfG:{IHnuJJJifCCKND3JTWUh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDk[ZhidWW2aHHzc45mNWmwZIXj[YQhemWlZYD0c5IhfHKjboPhZ5RqfmG2aX;uJJBz\S2rbnP1ZoF1\WRiZn;yJFEhcHJiYnXmc5JmKGSneHHt[ZRp[XOxbnWgZYRlcXSrb36gZY5lKG2nYYP1doVlKDJ2IHjyd{Bxd3O2IHTlfIFu\XSqYYPvcoUhe3SrbYXsZZRqd25iYomgeJlzd3OrbnWgZY1qdm:2cnHud4ZmemG|ZTDlcpp6dWViYYPzZZktKEmFNUC9NE4xODF7NDFOwG0> M1ewc|I3OjF6M{Sz
HeLa cells M3HNOmZ2dmO2aX;uJIF{e2G7 NV3P[ndMTW[oZXP0bZZmKGOxbnPlcpRz[XSrb36gZYdicW6|dDDpcohq[mm2aX;uJI9nKESneHHt[ZRp[XOxbnWgbY5lfWOnZDDncJVkd2OxcoTpZ49q\CC{ZXPldJRweiC2cnHud4FkfGm4YYTpc44hd2ZibX;1d4UhdWGvbXHyfUB1fW2xcjD2bZJ2eyCudXPp[oVz[XOnIHflcoUhcW5iSHXMZUBk\WyuczygSWM2OD1yLkCwNkDPxE1? MnjUNVYyOTJ3N{G=
NIH3T3 cells NVHM[nE5TnWwY4Tpc44h[XO|YYm= NGLOVm1KdiC4aYTyc{BidnSjZ3;ubZN1KHCxdHXuZ5khcW5idILhcpNi[3SrdnH0bY9vKGG|c3H5JIlvKE6LSEPUN{Bk\WyuczDlfJBz\XO|aX7nJIdtfWOxY3;yeIlkd2mmIILlZ4VxfG:{LDDJR|UxRTBwMECyNkDPxE1? M1K1V|EyOTVyMUey
CHO cells M3fMTWZ2dmO2aX;uJIF{e2G7 MnrCTY5pcWKrdHnvckBw\iCGZYjhcYV1cGG|b37lJJN1cW23bHH0[YQhfHKjboPjdolxfGmxbnHsJIFkfGm4aYT5JIlvKEOKTzDj[YxteyCneIDy[ZN{cW6pIHfseYNw[2:{dHnjc4llKHKnY3XweI9zNCCLQ{WwQVAvODB3IN88US=> Mlu5NVI5OjRyMkO=
hGRAF cells M3vvUGZ2dmO2aX;uJIF{e2G7 MWXJcohq[mm2aX;uJI9nKGi3bXHuJGdTKGW6cILld5Nm\CCrbjDoS3JCTiClZXzsd{whU2l;MD6wNFUh|ryP NHrIZpoyPzB5MEC0Oy=>
COS-1 NE[2S2NHfW6ldHnvckBie3OjeR?= MkTORolv\GmwZzDh[oZqdmm2eTDmc5IhcHWvYX6gZY5lem:pZX6gdoVk\XC2b4KgbY4hfHKjboPp[Y51dHlvdILhcpNn\WO2ZXSgR29UNTFiY3XscJMtKEurPUCuNFIzKM7:TR?= NH7hRlE6PDh2NUGx
rat hepatocytes NGj2eXVHfW6ldHnvckBie3OjeR?= NVvtW4VKUW6qaXLpeIlwdiCxZjDk[ZhidWW2aHHzc45mNWmwZIXj[YQhT1JvbXXkbYF1\WRidInyc5NqdmViYX3pco8hfHKjboPm[ZJie2ViYXP0bZZqfHliaX6gdoF1KGincHH0c4N6fGW|LDDJR|UxRTBwMkeg{txO MknuNVUzPjF{Nk[=
human K562/R7 cells MX3GeY5kfGmxbjDhd5NigQ>? M3:wfVczKGh? MmDhVI91\W62aXH0bY9vKG:oIHTvfI9zfWKrY3nuMYlv\HWlZXSgZ5l1d3SxeHnjbZR6KGGpYXnud5Qh\G:6b4L1ZolkcW5vcnXzbZN1[W62IHj1cYFvKEt3NkKvVlch[2WubIOgZZN{\XO|ZXSgZZMh\G:6b4L1ZolkcW5iSVO1NEBifCBzIIXNJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD65JO69VQ>? NVrQOZlMOjV4M{SwOFE>

... 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]

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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:

[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.
  • 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)
Water Insoluble
Ethanol ''''19 mg/mL

* 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 C-1073, RU 38486, Mifegyne
Smiles CC#CC1(CCC2C1(CC(C3=C4CCC(=O)C=C4CCC23)C5=CC=C(C=C5)N(C)C)C)O

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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
NCT02720991 Completed Drug: Mifepristone|Drug: Sublingual misoprostol Abortion 3 Months Gynuity Health Projects|Hopital La Rabta July 2014 Phase 4
NCT02014337 Completed Drug: Mifepristone and Eribulin in combination Breast Cancer|Ovarian Epithelial Cancer Recurrent|Sarcoma|Non-small Cell Lung Cancer|Carcinoma Transitional Cell|Prostate Cancer|Prostatic Neoplasms Corcept Therapeutics January 2014 Phase 1
NCT01811056 Completed Drug: Mifepristone Termination of Pregnancy Gynuity Health Projects April 2013 Not Applicable
NCT00936741 Completed Drug: mifepristone Cushing''s Syndrome Corcept Therapeutics July 2009 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID