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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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 NWTkbJk4TnWwY4Tpc44h[XO|YYm= M37PVWlvcGmkaYTpc44hd2ZiQ1jPMWsyKGOnbHzzJIV5eHKnc4Ppcoch\2y3Y3;jc5J1cWOxaXSgdoVk\XC2b4KsJGlEPTB;OHWtNFYh|ryP MYCxOVQ2PjJ2Mh?=
T47D-C124 cells NE\wSZBHfW6ldHnvckBie3OjeR?= MoPDNlQhcA>? NYm1cVI4SW62YXfvcol{fCCjY4Tpeol1gSCjdDDwdo9o\XO2ZYLvcoUhemWlZYD0c5IhcW5iaIXtZY4hXDR5RD3DNVI1KGOnbHzzJJRz[W6|ZnXjeIVlKHerdHigcJVkcW[ncnHz[UBo\W6nIHzpcotm\CC2bzDNUXRXKHC{b33veIVzKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YheHKxZ3XzeIVzd26nLXnu[JVk\WRibIXjbYZmemG|ZTD0doFve2GldHn2ZZRqd25iYXP0bZZqfHliYX\0[ZIhOjRiaILzMEBKSzVyPUKuNYUuODVizszN MYSxPVIyPjV2OR?=
neuroblastoma cells MnPYSpVv[3Srb36gZZN{[Xl? MkDYTY4hfmm2cn:gZY51[WexbnnzeEBxd3SnbnP5JIlvKHS{YX7zZYN1cX[jdHnvckBie3OjeTDpckBv\XW{b3LsZZN1d22jIHPlcIx{KGW6cILld5NqdmdiaIXtZY4hWFJvQjDwdo9o\XO2ZYLvcoUhemWlZYD0c5ItKEmFNUC9Nk42\S1yNTFOwG0> NIC4UlcyOTF3MEG3Ni=>
T47D cells NEWydVlHfW6ldHnvckBie3OjeR?= MUi0PEBp MYHBcpRi\2:waYP0JIFkfGm4aYT5JIF1KHC{b3fld5Rmem:wZTDy[YNmeHSxcjDpckBpfW2jbjDUOFdFKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gdJJw\2W|dHXyc45mNWmwZIXj[YQh[WytYXzpcoUheGixc4DoZZRie2ViYXP0bZZqfHliYX\0[ZIhPDhiaILzMEBKSzVyPUSuOYUuODVizszN NIHzWpcyQTJzNkW0PS=>
CV-1 cells MoLMSpVv[3Srb36gZZN{[Xl? NYDKXVVGSW62YXfvcol{fGmlIHHjeIl3cXS7IHHnZYlve3RiaIXtZY4heHKxZ3XzeIVzd26nIILlZ4VxfG:{IFKgLIhRWi2EKTDpckBkdy22cnHud4Zm[3SnZDDDWk0yKGOnbHzzMEBKSzVyPUCuNFAxOThizszN NEnCWIU6PDh2NUGx
HEK293 cells MUfGeY5kfGmxbjDhd5NigQ>? M1jx[GFvfGGpb37pd5Qh[WO2aY\peJkh[WejaX7zeEBodHWlb3PvdpRq[2:rZDDy[YNmeHSxcjCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYomgS3JGNWSncHXu[IVvfCCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGlEPTB;MD6wNFAzQThizszN NUnpTW9sOjZ{MUizOFM>
COS7 cells MYHGeY5kfGmxbjDhd5NigQ>? MVLBcpRi\2:waYP0JIFkfGm4aYT5JIF1KGOub37l[EBodHWlb3PvdpRq[2:rZDDy[YNmeHSxcj3sbYdidmRiYnnu[Ilv\yCmb33hbY4h\XiycnXzd4VlKGmwIHHmdolk[W5iZ4Ll[Y4hdW:wa3X5JGNQWzdiY3XscJMh[nliR1HMOEBtfWOrZnXyZZNmKHKncH;yeIVzKGG|c3H5MEBKSzVyPUCuNFAxPiEQvF2= Ml;rNVg2ODRzM{K=
SW1353 cells NXTwc5RITnWwY4Tpc44h[XO|YYm= Mlm0Rolv\GmwZzDh[oZqdmm2eTD0c{BodHWlb3PvdpRq[2:rZDDy[YNmeHSxcjDpckBUXzF|NUOgZ4VtdHNiYomge4hwdGVvY3XscEBjcW6maX7nJIF{e2G7LDDLbV0xNjByMEiyJO69VQ>? M{S0e|E4QDJ{OEm3
A549 cells MlrzSpVv[3Srb36gZZN{[Xl? Mn7ZRY51[WexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBodHWlb3PvdpRq[2:rZDDy[YNmeHSxcjDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPvdpRq[2:rZD3pcoR2[2WmIITyZY5{[3KrcITpc44hcW5iaIXtZY4hSTV2OTDj[YxteyCkeTDHVmUudGmwa3XkJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiSVO1NF0xNjByMU[g{txO MVixO|MyPzF4Nx?=
A549 cells MUTGeY5kfGmxbjDhd5NigQ>? NIHZcIIyPiCq MYjBcpRi\2:waYP0JIFkfGm4aYT5JIF1KGeudXPvZ49zfGmlb3nkJJJm[2WydH;yJIlvKGi3bXHuJGE2PDliY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBkd3K2aXPvbYQucW6mdXPl[EB1emGwc3PybZB1cW:wIHHmeIVzKDF4IHjyd{BjgSCpbIXjc4NwenSrY3;p[EBz\XOyb37z[UBmdGWvZX70MYRzcX[nbjDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUC9NE4xODF4IN88US=> NUHsNm5ZOTl{MUeyPFU>
rat H4-IIE cells MnvxSpVv[3Srb36gZZN{[Xl? NXrjXYFrOSCq MY\BcpRi\2:waYP0JIFkfGm4aYT5JIFo[Wmwc4Sg[4x2[2:lb4L0bYNwcWRicnXj[ZB1d3JiaX6gdoF1KEh2LVnJSUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHTlfIFu\XSqYYPvcoUucW6mdXPl[EBz\WOncITvdkB1emGwc3HjeIl3[XSrb36gdJJmNWmwY4XiZZRm\CCob4KgNUBpeiCkZX\vdoUh\GW6YX3leIhie2:wZTDh[IRqfGmxbjDhcoQhdWWjc4Xy[YQhOjRiaILzJJBwe3RiZHX4ZY1mfGijc3;u[UB{fGmvdXzheIlwdiCkeTD0fZJwe2mwZTDhcYlvd3S{YX7z[oVz[XOnIHXufplu\SCjc4PhfUwhUUN3ME2wMlAxOTl2IN88US=> MWGyOlIyQDN2Mx?=
HeLa cells MXvGeY5kfGmxbjDhd5NigQ>? NH\RXGVG\m[nY4TpeoUh[2:wY3XueJJifGmxbjDh[4FqdnO2IHnubIljcXSrb36gc4YhTGW6YX3leIhie2:wZTDpcoR2[2WmIHfseYNw[2:{dHnjc4llKHKnY3XweI9zKHS{YX7zZYN1cX[jdHnvckBw\iCvb4Xz[UBu[W2vYYL5JJR2dW:{II\pdpV{KGy3Y3nm[ZJie2ViZ3Xu[UBqdiCKZVzhJINmdGy|LDDFR|UxRTBwMECyJO69VQ>? NVjNTYdqOTZzMUK1O|E>
NIH3T3 cells NFjLTZRHfW6ldHnvckBie3OjeR?= M2LVUGlvKH[rdILvJIFvfGGpb37pd5QheG:2ZX7jfUBqdiC2cnHud4FkfGm4YYTpc44h[XO|YYmgbY4hVkmKM2SzJINmdGy|IHX4dJJme3Orbneg[4x2[2:lb4L0bYNwcWRicnXj[ZB1d3JuIFnDOVA:OC5yMEKyJO69VQ>? NIX5OIYyOTF3MEG3Ni=>
CHO cells NF7TfWlHfW6ldHnvckBie3OjeR?= MlPHTY5pcWKrdHnvckBw\iCGZYjhcYV1cGG|b37lJJN1cW23bHH0[YQhfHKjboPjdolxfGmxbnHsJIFkfGm4aYT5JIlvKEOKTzDj[YxteyCneIDy[ZN{cW6pIHfseYNw[2:{dHnjc4llKHKnY3XweI9zNCCLQ{WwQVAvODB3IN88US=> MWqxNlgzPDB{Mx?=
hGRAF cells M17CUmZ2dmO2aX;uJIF{e2G7 NVvTRnh2UW6qaXLpeIlwdiCxZjDoeY1idiCJUjDlfJBz\XO|ZXSgbY4hcEeUQV[gZ4VtdHNuIFvpQVAvODB3IN88US=> MUmxO|A4ODB2Nx?=
COS-1 NXPk[WRzTnWwY4Tpc44h[XO|YYm= NUnMfmhOSmmwZHnu[{Bi\m[rbnn0fUBnd3JiaIXtZY4h[W6mcn;n[Y4hemWlZYD0c5IhcW5idILhcpNq\W62bImteJJidnOoZXP0[YQhS0:VLUGgZ4VtdHNuIFvpQVAvODJ{IN88US=> MY[5OFg1PTFz
rat hepatocytes M37XZWZ2dmO2aX;uJIF{e2G7 M3\G[mlvcGmkaYTpc44hd2ZiZHX4ZY1mfGijc3;u[U1qdmS3Y3XkJGdTNW2nZHnheIVlKHS7cn;zbY5mKGGvaX7vJJRz[W6|ZnXyZZNmKGGldHn2bZR6KGmwIILheEBp\XCjdH;jfZRmeyxiSVO1NF0xNjJ5IN88US=> NVnUNIVKOTV{NkGyOlY>
human K562/R7 cells NGTxdHhHfW6ldHnvckBie3OjeR?= MXy3NkBp M1H4NXBwfGWwdHnheIlwdiCxZjDkc5hwenWkaXPpck1qdmS3Y3XkJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGSxeH;yeYJq[2mwLYLld4l{fGGwdDDoeY1idiCNNU[yM3I4KGOnbHzzJIF{e2W|c3XkJIF{KGSxeH;yeYJq[2mwIFnDOVAh[XRiMTD1UUBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuPUDPxE1? NH7je|QzPTZ|NEC0NS=>

... Click to View More Cell Line Experimental Data

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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • 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
Synonyms RU486, C-1073

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00043654 Completed Bipolar Disorder National Institute of Mental Health (NIMH)|National Institutes of Health Clinical Center (CC) August 7, 2002 Phase 2
NCT03052400 Recruiting Type 2 Diabetes Mellitus|Insulin Resistance Charles Drew University of Medicine and Science February 3, 2017 Phase 2
NCT01419535 Recruiting Endocrine Disease|Diabetes Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|National Institutes of Health Clinical Center (CC) July 29, 2011 Phase 1|Phase 2
NCT02019706 Recruiting Cushing Syndrome Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|National Institutes of Health Clinical Center (CC) November 26, 2013 Phase 2
NCT01294319 Completed Cortisol Resistance|Negative Feedback|ACTH|Mineralcorticoid|Glucocorticoid Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|National Institutes of Health Clinical Center (CC) January 24, 2011 Phase 2
NCT03044093 Recruiting Second Trimester Abortion Rambam Health Care Campus January 2017 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID