Mifepristone (RU486)

For research use only.

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

15 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.

Selleck's Mifepristone (RU486) has been cited by 15 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 MUjGeY5kfGmxbjDhd5NigQ>? M{mwd2lvcGmkaYTpc44hd2ZiQ1jPMWsyKGOnbHzzJIV5eHKnc4Ppcoch\2y3Y3;jc5J1cWOxaXSgdoVk\XC2b4KsJGlEPTB;OHWtNFYh|ryP MmTMNVU1PTZ{NEK=
T47D-C124 cells MUHGeY5kfGmxbjDhd5NigQ>? MkjxNlQhcA>? Mnm1RY51[WexbnnzeEBi[3Srdnn0fUBifCCycn;n[ZN1\XKxbnWgdoVk\XC2b4KgbY4hcHWvYX6gWFQ4TC2FMUK0JINmdGy|IITyZY5{\mWldHXkJJdqfGhibIXjbYZmemG|ZTDn[Y5mKGyrbnvl[EB1dyCPTWTWJJBzd22xdHXyJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gdJJw\2W|dHXyc45mNWmwZIXj[YQhdHWlaX\ldoF{\SC2cnHud4FkfGm4YYTpc44h[WO2aY\peJkh[W[2ZYKgNlQhcHK|LDDJR|UxRTJwMXWtNFUh|ryP MVexPVIyPjV2OR?=
neuroblastoma cells M4Dmd2Z2dmO2aX;uJIF{e2G7 NHXOWVRKdiC4aYTyc{BidnSjZ3;ubZN1KHCxdHXuZ5khcW5idILhcpNi[3SrdnH0bY9vKGG|c3H5JIlvKG6ndYLvZoxie3SxbXGgZ4VtdHNiZYjwdoV{e2mwZzDoeY1idiCSUj3CJJBzd2enc4Tldo9v\SC{ZXPldJRweixiSVO1NF0zNjWnLUC1JO69VQ>? NIPTfpMyOTF3MEG3Ni=>
T47D cells M1zoOmZ2dmO2aX;uJIF{e2G7 M{PWd|Q5KGh? MmDuRY51[WexbnnzeEBi[3Srdnn0fUBifCCycn;n[ZN1\XKxbnWgdoVk\XC2b4KgbY4hcHWvYX6gWFQ4TCClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJJBzd2enc4Tldo9v\S2rbnT1Z4VlKGGua3HsbY5mKHCqb4PwbIF1[XOnIHHjeIl3cXS7IHHmeIVzKDR6IHjyd{whUUN3ME20MlVmNTB3IN88US=> MkS5NVkzOTZ3NEm=
CV-1 cells MoPlSpVv[3Srb36gZZN{[Xl? NH7MfFdCdnSjZ3;ubZN1cWNiYXP0bZZqfHliYXfhbY5{fCCqdX3hckBxem:pZYP0[ZJwdmVicnXj[ZB1d3JiQjCobHBTNUJrIHnuJINwNXS{YX7z[oVkfGWmIFPWMVEh[2WubIOsJGlEPTB;MD6wNFAyQCEQvF2= MoXmPVQ5PDVzMR?=
HEK293 cells MnyxSpVv[3Srb36gZZN{[Xl? M1exe2FvfGGpb37pd5Qh[WO2aY\peJkh[WejaX7zeEBodHWlb3PvdpRq[2:rZDDy[YNmeHSxcjCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYomgS3JGNWSncHXu[IVvfCCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGlEPTB;MD6wNFAzQThizszN NF;BdIwzPjJzOEO0Ny=>
COS7 cells MYnGeY5kfGmxbjDhd5NigQ>? NVThR|RVSW62YXfvcol{fCCjY4Tpeol1gSCjdDDjcI9v\WRiZ3z1Z49kd3K2aXPvbYQhemWlZYD0c5IudGmpYX7kJIJqdmSrbneg[I9u[WmwIHX4dJJme3OnZDDpckBi\nKrY3HuJIdz\WWwIH3vcotmgSCFT2O3JINmdGy|IHL5JGdCVDRibIXjbYZmemG|ZTDy[ZBwenSncjDhd5NigSxiSVO1NF0xNjByME[g{txO NYmzPI9MOTh3MESxN|I>
SW1353 cells M3HvfGZ2dmO2aX;uJIF{e2G7 MUnCbY5lcW6pIHHm[olvcXS7IITvJIdtfWOxY3;yeIlkd2mmIILlZ4VxfG:{IHnuJHNYOTN3MzDj[YxteyCkeTD3bI9t\S2lZXzsJIJqdmSrbnegZZN{[XluIFvpQVAvODByOEKg{txO NIHsOXoyPzh{Mki5Oy=>
A549 cells NUP4fZpjTnWwY4Tpc44h[XO|YYm= M4LleGFvfGGpb37pd5Qh[WO2aY\peJkh[XRiaIXtZY4h\2y3Y3;jc5J1cWOxaXSgdoVk\XC2b4KgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDjc5J1cWOxaXStbY5lfWOnZDD0doFve2O{aYD0bY9vKGmwIHj1cYFvKEF3NEmgZ4VtdHNiYomgS3JGNWyrbnvl[EBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFnDOVA:OC5yMEG2JO69VQ>? NYHaSotXOTd|MUexOlc>
A549 cells Ml;xSpVv[3Srb36gZZN{[Xl? NGGybXUyPiCq NUjxNXZDSW62YXfvcol{fCCjY4Tpeol1gSCjdDDncJVkd2OxcoTpZ49q\CC{ZXPldJRweiCrbjDoeY1idiCDNUS5JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3;yeIlkd2mmLXnu[JVk\WRidILhcpNkemmydHnvckBi\nSncjCxOkBpenNiYomg[4x2[2:lb4L0bYNwcWRicnXzdI9ve2ViZXzlcYVvfC2mcnn2[Y4hdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDJR|UxRTBwMECxOkDPxE1? NYXLWVM3OTl{MUeyPFU>
rat H4-IIE cells MmTtSpVv[3Srb36gZZN{[Xl? MU[xJIg> MkDNRY51[WexbnnzeEBi[3Srdnn0fUBi\2GrboP0JIdtfWOxY3;yeIlkd2mmIILlZ4VxfG:{IHnuJJJifCCKND3JTWUh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDk[ZhidWW2aHHzc45mNWmwZIXj[YQhemWlZYD0c5IhfHKjboPhZ5RqfmG2aX;uJJBz\S2rbnP1ZoF1\WRiZn;yJFEhcHJiYnXmc5JmKGSneHHt[ZRp[XOxbnWgZYRlcXSrb36gZY5lKG2nYYP1doVlKDJ2IHjyd{Bxd3O2IHTlfIFu\XSqYYPvcoUhe3SrbYXsZZRqd25iYomgeJlzd3OrbnWgZY1qdm:2cnHud4ZmemG|ZTDlcpp6dWViYYPzZZktKEmFNUC9NE4xODF7NDFOwG0> MV[yOlIyQDN2Mx?=
HeLa cells M3;3cmZ2dmO2aX;uJIF{e2G7 MmD2SYZn\WO2aY\lJINwdmOnboTyZZRqd25iYXfhbY5{fCCrbnjpZol1cW:wIH;mJGRmgGGvZYToZZNwdmViaX7keYNm\CCpbIXjc4NwenSrY3;p[EBz\WOncITvdkB1emGwc3HjeIl3[XSrb36gc4YhdW:3c3WgcYFudWG{eTD0eY1weiC4aYL1d{BtfWOrZnXyZZNmKGenbnWgbY4hUGWOYTDj[YxteyxiRVO1NF0xNjByMjFOwG0> MWqxOlEyOjV5MR?=
NIH3T3 cells MkTJSpVv[3Srb36gZZN{[Xl? NWTrcVA4UW5idnn0do8h[W62YXfvcol{fCCyb4TlcoN6KGmwIITyZY5{[WO2aY\heIlwdiCjc4PhfUBqdiCQSVizWFMh[2WubIOg[ZhxemW|c3nu[{BodHWlb3PvdpRq[2:rZDDy[YNmeHSxcjygTWM2OD1yLkCwNlIh|ryP MXSxNVE2ODF5Mh?=
CHO cells Mny2SpVv[3Srb36gZZN{[Xl? MmrNTY5pcWKrdHnvckBw\iCGZYjhcYV1cGG|b37lJJN1cW23bHH0[YQhfHKjboPjdolxfGmxbnHsJIFkfGm4aYT5JIlvKEOKTzDj[YxteyCneIDy[ZN{cW6pIHfseYNw[2:{dHnjc4llKHKnY3XweI9zNCCLQ{WwQVAvODB3IN88US=> NXTnXXA1OTJ6MkSwNlM>
hGRAF cells NGLGO|hHfW6ldHnvckBie3OjeR?= MkXmTY5pcWKrdHnvckBw\iCqdX3hckBIWiCneIDy[ZN{\WRiaX6gbGdTSUZiY3XscJMtKEurPUCuNFA2KM7:TR?= NGHqc|kyPzB5MEC0Oy=>
COS-1 NV\SUnM4TnWwY4Tpc44h[XO|YYm= MlHYRolv\GmwZzDh[oZqdmm2eTDmc5IhcHWvYX6gZY5lem:pZX6gdoVk\XC2b4KgbY4hfHKjboPp[Y51dHlvdILhcpNn\WO2ZXSgR29UNTFiY3XscJMtKEurPUCuNFIzKM7:TR?= M1\sfFk1QDR3MUG=
rat hepatocytes NInkU4NHfW6ldHnvckBie3OjeR?= MnzPTY5pcWKrdHnvckBw\iCmZYjhcYV1cGG|b37lMYlv\HWlZXSgS3IudWWmaXH0[YQhfHm{b4PpcoUh[W2rbn:geJJidnOoZYLhd4Uh[WO2aY\peJkhcW5icnH0JIhmeGG2b3P5eIV{NCCLQ{WwQVAvOjdizszN MXWxOVI3OTJ4Nh?=
human K562/R7 cells MWXGeY5kfGmxbjDhd5NigQ>? MmrYO|IhcA>? NF3UPWhRd3SnboTpZZRqd25ib3[g[I95d3K3YnnjbY4ucW6mdXPl[EBkgXSxdH;4bYNqfHliYXfhbY5{fCCmb4jvdpVjcWOrbj3y[ZNqe3SjboSgbJVu[W5iS{W2Nk9TPyClZXzsd{Bie3Onc4Pl[EBieyCmb4jvdpVjcWOrbjDJR|UxKGG2IEGgeW0h[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlkh|ryP NFrMdlYzPTZ|NEC0NS=>

... 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
NCT04905251 Not yet recruiting Drug: Mifepristone-Misoprostol Medical Abortion Linepharma International LTD July 15 2021 --
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID