Mifepristone (RU486) - Moligand™, 10mM in DMSO , Progesterone receptor antagonist, CAS No.84371-65-3, Progesterone receptor antagonist

CAS: 84371-65-3 Cat. No.: M408467 Molecular Weight: 429.59 EC Number: 617-559-7

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

C-1073, RU 38486, Mifegyne | (11β,​17β)​-11-​[4-​(dimethylamino)​phenyl]​-​17-​hydroxy-​17-​(1-​propyn-​1-​yl)​-estra-​4,​9-​dien-​3-​one

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Mifepristone (RU486, C-1073, RU 38486, Mifegyne) is a remarkably active antagonist ofprogesterone receptorandglucocorticoid receptorwithIC50of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cellautophagyandapoptosis, decreasesBcl-2level and increa
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. Mifepristone inhibits ovarian cancer cell growth of SK-OV-3 and OV2008 with IC50 of 6.25 μM and 6.91 μM, respectively. A recent study shows that Mifepristone induces caspase-1 over expression both in differentiated and undifferentiated caspase-1-embryonic stem cells.

In vivo

Mifepristone can impair the growth of SK-OV-3 tumors in immunosuppressed mice at 0.5 mg/day and 1 mg/day. 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.
Cell Data

cell lines：

Concentrations：0-20 μM

Incubation Time：24 hours

Powder Purity:≥99%

Specifications

Synonyms

C-1073, RU 38486, Mifegyne | (11β, ​17β)​-11-​[4-​(dimethylamino)​phenyl]​-​17-​hydroxy-​17-​(1-​propyn-​1-​yl)​-estra-​4, ​9-​dien-​3-​one

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

AGONIST, ANTAGONIST

Mechanism of action

Progesterone receptor antagonist

Product Properties

• ALogP: 3.8

Names and Identifiers

• Isomeric SMILES: CC#C[C@@]1(CC[C@@H]2[C@@]1(C[C@@H](C3=C4CCC(=O)C=C4CC[C@@H]23)C5=CC=C(C=C5)N(C)C)C)O
• WGK Germany: 3
• RTECS: KG2955000
• Molecular Weight: 429.59
• Reaxy-Rn: 24984138
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24984138&ln=

Associated Targets(Human)

NR3C1 Tclin Glucocorticoid receptor (67 Activities)

Discover Target: NR3C1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PGR Tclin Progesterone receptor (57 Activities)

Discover Target: PGR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NR1I2 Tchem Nuclear receptor subfamily 1 group I member 2 (1 Activities)

Discover Target: NR1I2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AR Tclin Androgen receptor (27 Activities)

Discover Target: AR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 30 mg/mL (197.13 mM); Water: Insoluble; Ethanol: Insoluble
• Specific Rotation[α]: 141° (C=0.5,CHCl3)
• Melt Point(°C): 195 °C

References

1. Mingyang Chen, Mengru Bai, Yaodong Yi, Shuanghui Lu, Jun Luo, Ping Li, Hengbin Zhang, Huidi Jiang, Hui Zhou.  (2022)  Upregulation of hepatic CD36 via glucocorticoid receptor activation contributes to dexamethasone-induced liver lipid metabolism disorder in mice.  TOXICOLOGY LETTERS,      [PMID:35589016] [10.1016/j.toxlet.2022.05.003]

2. Qi-qiang Zhang, Xue-mei Di, Xiang Cao, Yonghong Nie, Wen Shuai, Jun Li, Hai Zhang.  (2023)  Analysis of pharmacodynamic components, targets and synergistic action mechanism of Fuyuan Shenghua granule for the treatment of medical-induced incomplete abortion based on network pharmacology.  JOURNAL OF ETHNOPHARMACOLOGY,      [PMID:37659757] [10.1016/j.jep.2023.117118]

3. Sheng Hu, Pei Shen, Bin Chen, Shao-Wen Tian, Yong You.  (2022)  Apelin-13 reduces lipopolysaccharide-induced neuroinflammation and cognitive impairment via promoting glucocorticoid receptor expression and nuclear translocation.  NEUROSCIENCE LETTERS,      [PMID:36038029] [10.1016/j.neulet.2022.136850]

4. Mengru Bai, Mingyang Chen, Qingquan Zeng, Shuanghui Lu, Ping Li, Zhiyuan Ma, Nengming Lin, Caihong Zheng, Hui Zhou, Su Zeng, Dongli Sun, Huidi Jiang.  (2022)  Up-regulation of hepatic CD36 by increased corticosterone/cortisol levels via GR leads to lipid accumulation in liver and hypertriglyceridaemia during pregnancy.  BRITISH JOURNAL OF PHARMACOLOGY,  179  (17): (4440-4456).  [PMID:35491243] [10.1111/bph.15863]

5. Yao Xin-peng, Jiao Ting-ying, Jiang Yi-ming, Fan Shi-cheng, Zhao Ying-yuan, Yang Xiao, Gao Yue, Li Fei, Zhou Yan-ying, Chen Pan-pan, Huang Min, Bi Hui-chang.  (2021)  PXR mediates mifepristone-induced hepatomegaly in mice.  ACTA PHARMACOLOGICA SINICA,  43  (1): (146-156).  [PMID:33782543] [10.1038/s41401-021-00633-4]

6. Chang Shu, Teng-Fei Li, Duo Li, Zhong-Qiu Li, Xing-Hua Xia.  (2020)  Barcode signal amplifying strategy for sensitive and accurate protein detection on LC-MS/MS.  ANALYST,  146  (5): (1725-1733).  [PMID:33459316] [10.1039/D0AN01948H]

7. Meng Zhang, Yiqing Ye, Zhengyun Chen, Xiaodong Wu, Yue Chen, Pengfei Zhao, Mengdan Zhao, Caihong Zheng.  (2024)  Targeting Delivery of Mifepristone to Endometrial Dysfunctional Macrophages for Endometriosis Therapy.  Acta Biomaterialia,      [PMID:39341437] [10.1016/j.actbio.2024.09.037]

8. Lihong Sheng, Jianpeng Gao, Qingyuan Wei, Ye Gong, Zhi-Xiang Xu.  (2024)  The glial UDP-glycosyltransferase Ugt35b regulates longevity by maintaining lipid homeostasis in Drosophila.  Cell Reports,      [PMID:39723892] [10.1016/j.celrep.2024.115099]

9. Caiqun Huang.  (2024)  Toll-like receptor 4 (TLR4) deficiency impedes Toxoplasma gondii excreted-secreted antigens (ESA)-induced abortion.  PLACENTA,      [PMID:38824786] [10.1016/j.placenta.2024.05.137]

10. Yonghua Hu, Xujin Yang, Chenmei Ma, Zhen Wang, Xin Yuan, Man He, Penghai Zhang, Yi Tao.  (2025)  Therapeutic Effect and Mechanism of Da-Huang-Zhe-Chong Pills on Uterine Fibroids Using Liquid Chromatography Combined With Mass Spectrometry Metabolomics.  BIOMEDICAL CHROMATOGRAPHY,  39  (5): (e70083).  [PMID:40207468] [10.1002/bmc.70083]

11. Xuanhan Zhang, Chenpeng Zuo, Jiaqi Liu, Xiao Jing, Ziyi Zhao, Jing Yang, Zhijun Wang, Xin Qi.  (2025)  Stress signaling via glucocorticoid receptor disrupts ovarian development in Japanese eel (Anguilla japonica) through HPI-HPG axis crosstalk.  GENERAL AND COMPARATIVE ENDOCRINOLOGY,      [PMID:41077224] [10.1016/j.ygcen.2025.114825]

12. Caiqun Huang, Ying Lyu, E Fen Cheng.  (2026)  Toll-Like Receptor 4/p65 Signalling Pathway Mediates Recurrent Spontaneous Abortion by Regulating Forkhead Box Protein P3.  Clinical and Experimental Obstetrics & Gynecology,  53  (1):   [PMID:] [10.31083/CEOG45730]

13. Yujie Peng, Meng Zhang, Libo Zhu, Wenqiang Qian, Jingjing Yan, Huidi Jiang, Yu Xin, Ying Zhang, Dongli Sun, Weidong Fei, Mengdan Zhao.  (2026)  Synergistic RU486 and olaparib therapy enhances apoptosis in endometriosis by simultaneously targeting hormonal signalling and DNA repair.  BRITISH JOURNAL OF PHARMACOLOGY,      [PMID:41707660] [10.1111/bph.70360]