Mifepristone (RU486)

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

For research use only.

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.

Mifepristone (RU486) Chemical Structure

CAS No. 84371-65-3

Selleck's Mifepristone (RU486) has been cited by 17 publications

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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 MlPDSpVv[3Srb36gZZN{[Xl? NWPaXnlnUW6qaXLpeIlwdiCxZjDDTG8uUzFiY3XscJMh\XiycnXzd4lv\yCpbIXjc4NwenSrY3;p[EBz\WOncITvdkwhUUN3ME24[U0xPiEQvF2= Ml[3NVU1PTZ{NEK=
T47D-C124 cells NFvvbYFHfW6ldHnvckBie3OjeR?= NFnn[3IzPCCq M3TjZ2FvfGGpb37pd5Qh[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?= MWOxPVIyPjV2OR?=
neuroblastoma cells MkC5SpVv[3Srb36gZZN{[Xl? MlLQTY4hfmm2cn:gZY51[WexbnnzeEBxd3SnbnP5JIlvKHS{YX7zZYN1cX[jdHnvckBie3OjeTDpckBv\XW{b3LsZZN1d22jIHPlcIx{KGW6cILld5NqdmdiaIXtZY4hWFJvQjDwdo9o\XO2ZYLvcoUhemWlZYD0c5ItKEmFNUC9Nk42\S1yNTFOwG0> MX:xNVE2ODF5Mh?=
T47D cells MXfGeY5kfGmxbjDhd5NigQ>? MXm0PEBp MVXBcpRi\2:waYP0JIFkfGm4aYT5JIF1KHC{b3fld5Rmem:wZTDy[YNmeHSxcjDpckBpfW2jbjDUOFdFKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gdJJw\2W|dHXyc45mNWmwZIXj[YQh[WytYXzpcoUheGixc4DoZZRie2ViYXP0bZZqfHliYX\0[ZIhPDhiaILzMEBKSzVyPUSuOYUuODVizszN NWnRUIZlOTl{MU[1OFk>
CV-1 cells MkHhSpVv[3Srb36gZZN{[Xl? MXTBcpRi\2:waYP0bYMh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDwdo9o\XO2ZYLvcoUhemWlZYD0c5IhSiBqaGDSMWIqKGmwIHPvMZRz[W6|ZnXjeIVlKEOYLUGgZ4VtdHNuIFnDOVA:OC5yMECxPEDPxE1? MXq5OFg1PTFz
HEK293 cells NWruNlhiTnWwY4Tpc44h[XO|YYm= M{fHZmFvfGGpb37pd5Qh[WO2aY\peJkh[WejaX7zeEBodHWlb3PvdpRq[2:rZDDy[YNmeHSxcjCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYomgS3JGNWSncHXu[IVvfCCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGlEPTB;MD6wNFAzQThizszN MYGyOlIyQDN2Mx?=
COS7 cells M2fQNmZ2dmO2aX;uJIF{e2G7 Mn32RY51[WexbnnzeEBi[3Srdnn0fUBifCClbH;u[YQh\2y3Y3;jc5J1cWOxaXSgdoVk\XC2b4KtcIlo[W6mIHLpcoRqdmdiZH;tZYlvKGW6cILld5Nm\CCrbjDh[pJq[2GwIHfy[YVvKG2xbnvlfUBEV1N5IHPlcIx{KGK7IFfBUFQhdHWlaX\ldoF{\SC{ZYDvdpRmeiCjc4PhfUwhUUN3ME2wMlAxODZizszN NFKydmUyQDVyNEGzNi=>
SW1353 cells NXnjeWtCTnWwY4Tpc44h[XO|YYm= MXHCbY5lcW6pIHHm[olvcXS7IITvJIdtfWOxY3;yeIlkd2mmIILlZ4VxfG:{IHnuJHNYOTN3MzDj[YxteyCkeTD3bI9t\S2lZXzsJIJqdmSrbnegZZN{[XluIFvpQVAvODByOEKg{txO MW[xO|gzOjh7Nx?=
A549 cells M{XL[WZ2dmO2aX;uJIF{e2G7 NUWySGpMSW62YXfvcol{fCCjY4Tpeol1gSCjdDDoeY1idiCpbIXjc4NwenSrY3;p[EBz\WOncITvdkBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINwenSrY3;p[E1qdmS3Y3XkJJRz[W6|Y4LpdJRqd25iaX6gbJVu[W5iQUW0PUBk\WyuczDifUBIWkVvbHnub4VlKGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygTWM2OD1yLkCwNVYh|ryP M33CZ|E4OzF5MU[3
A549 cells M3vDTWZ2dmO2aX;uJIF{e2G7 M17HUFE3KGh? NV7NW|NnSW62YXfvcol{fCCjY4Tpeol1gSCjdDDncJVkd2OxcoTpZ49q\CC{ZXPldJRweiCrbjDoeY1idiCDNUS5JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3;yeIlkd2mmLXnu[JVk\WRidILhcpNkemmydHnvckBi\nSncjCxOkBpenNiYomg[4x2[2:lb4L0bYNwcWRicnXzdI9ve2ViZXzlcYVvfC2mcnn2[Y4hdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDJR|UxRTBwMECxOkDPxE1? NFP2V44yQTJzN{K4OS=>
rat H4-IIE cells NEnONnpHfW6ldHnvckBie3OjeR?= M2HyeVEhcA>? M2CzcmFvfGGpb37pd5Qh[WO2aY\peJkh[WejaX7zeEBodHWlb3PvdpRq[2:rZDDy[YNmeHSxcjDpckBz[XRiSEStTWlGKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[g[IV5[W2ndHjhd49v\S2rbnT1Z4VlKHKnY3XweI9zKHS{YX7zZYN1cX[jdHnvckBxemVvaX7jeYJifGWmIH\vdkAyKGi{IHLl[o9z\SCmZYjhcYV1cGG|b37lJIFl\Gm2aX;uJIFv\CCvZXHzeZJm\CB{NDDodpMheG:|dDDk[ZhidWW2aHHzc45mKHO2aX31cIF1cW:wIHL5JJR6em:|aX7lJIFucW6xdILhcpNn\XKjc3Wg[Y57gW2nIHHzd4F6NCCLQ{WwQVAvODBzOUSg{txO MmrVNlYzOTh|NEO=
HeLa cells M33RbWZ2dmO2aX;uJIF{e2G7 MoTCSYZn\WO2aY\lJINwdmOnboTyZZRqd25iYXfhbY5{fCCrbnjpZol1cW:wIH;mJGRmgGGvZYToZZNwdmViaX7keYNm\CCpbIXjc4NwenSrY3;p[EBz\WOncITvdkB1emGwc3HjeIl3[XSrb36gc4YhdW:3c3WgcYFudWG{eTD0eY1weiC4aYL1d{BtfWOrZnXyZZNmKGenbnWgbY4hUGWOYTDj[YxteyxiRVO1NF0xNjByMjFOwG0> MlnmNVYyOTJ3N{G=
NIH3T3 cells M1zZZmZ2dmO2aX;uJIF{e2G7 MWDJckB3cXS{bzDhcpRi\2:waYP0JJBwfGWwY4mgbY4hfHKjboPhZ5RqfmG2aX;uJIF{e2G7IHnuJG5KUDOWMzDj[YxteyCneIDy[ZN{cW6pIHfseYNw[2:{dHnjc4llKHKnY3XweI9zNCCLQ{WwQVAvODB{MjFOwG0> NGrJdWgyOTF3MEG3Ni=>
CHO cells M4nte2Z2dmO2aX;uJIF{e2G7 MV7Jcohq[mm2aX;uJI9nKESneHHt[ZRp[XOxbnWgd5RqdXWuYYTl[EB1emGwc3PybZB1cW:wYXygZYN1cX[rdImgbY4hS0iRIHPlcIx{KGW6cILld5NqdmdiZ3z1Z49kd3K2aXPvbYQhemWlZYD0c5ItKEmFNUC9NE4xODVizszN MWixNlgzPDB{Mx?=
hGRAF cells Mk\ySpVv[3Srb36gZZN{[Xl? M1vsOWlvcGmkaYTpc44hd2ZiaIXtZY4hT1JiZYjwdoV{e2WmIHnuJIhIWkGIIHPlcIx{NCCNaU2wMlAxPSEQvF2= NIf1NW4yPzB5MEC0Oy=>
COS-1 NYHRWpIzTnWwY4Tpc44h[XO|YYm= NHP6OFVDcW6maX7nJIFn\mmwaYT5JIZweiCqdX3hckBidmS{b3flckBz\WOncITvdkBqdiC2cnHud4lmdnSueT30doFve2[nY4Tl[EBEV1NvMTDj[YxteyxiS3m9NE4xOjJizszN MXK5OFg1PTFz
rat hepatocytes NV;CV4VxTnWwY4Tpc44h[XO|YYm= NIjUe|dKdmirYnn0bY9vKG:oIHTlfIFu\XSqYYPvcoUucW6mdXPl[EBIWi2vZXTpZZRm\CC2eYLvd4lv\SCjbXnuc{B1emGwc3\ldoF{\SCjY4Tpeol1gSCrbjDyZZQhcGWyYYTvZ5l1\XNuIFnDOVA:OC5{NzFOwG0> MXGxOVI3OTJ4Nh?=
human K562/R7 cells NWTacWNnTnWwY4Tpc44h[XO|YYm= MWG3NkBp M3LhVnBwfGWwdHnheIlwdiCxZjDkc5hwenWkaXPpck1qdmS3Y3XkJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGSxeH;yeYJq[2mwLYLld4l{fGGwdDDoeY1idiCNNU[yM3I4KGOnbHzzJIF{e2W|c3XkJIF{KGSxeH;yeYJq[2mwIFnDOVAh[XRiMTD1UUBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuPUDPxE1? MoS4NlU3OzRyNEG=
Assay
Methods Test Index PMID
Western blot p-AKT / AKT / p-ERK / ERK ; MMP-2 / MMP-9 / COX-2 / VEGF 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 (from reference)

Kinase Assay:

[1]

  • 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]

  • 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.

Animal Research:

[2]

  • 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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 429.59
Formula

C29H35NO2

CAS No. 84371-65-3
Storage 3 years -20°C powder
2 years -80°C in solvent
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 December 31 2021 --
NCT05062174 Not yet recruiting Drug: Mifepristone 200 MG|Procedure: Prophylactic mastectomy BRCA1 Mutation|High-grade Serous Ovarian Cancer|TNBC - Triple-Negative Breast Cancer Indiana University|Breast Cancer Research Foundation October 1 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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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