Estrogen/progestogen Receptor

Signaling Pathway Map

Research Area

Inhibitory Selectivity
Solubility

Catalog No.	Product Name	Solubility(25°C)
Catalog No.	Product Name	Water	DMSO	Alcohol
S8372	AZD9496	<1 mg/mL	88 mg/mL	88 mg/mL
S5364	DY131	<1 mg/mL	62 mg/mL	<1 mg/mL
S1191	Fulvestrant	<1 mg/mL	100 mg/mL	100 mg/mL
S1972	Tamoxifen Citrate	<1 mg/mL	100 mg/mL	100 mg/mL
S1227	Raloxifene HCl	<1 mg/mL	100 mg/mL	<1 mg/mL
S2606	Mifepristone	<1 mg/mL	85 mg/mL	19 mg/mL
S5437	4,4'-DDE	-1 mg/mL	63 mg/mL	-1 mg/mL
S7855	Brilanestrant (GDC-0810, ARN-810)	<1 mg/mL	89 mg/mL	89 mg/mL
S4896	Elagolix Sodium	100 mg/mL	100 mg/mL	100 mg/mL
S8686	PHTPP	<1 mg/mL	50 mg/mL	84 mg/mL
S2466	Estriol	<1 mg/mL	57 mg/mL	10 mg/mL
S1238	Tamoxifen	<1 mg/mL	74 mg/mL	74 mg/mL
S7839	Endoxifen HCl	<1 mg/mL	74 mg/mL	74 mg/mL
S1709	Estradiol	<1 mg/mL	54 mg/mL	5 mg/mL
S5288	Estropipate	-1 mg/mL	87 mg/mL	-1 mg/mL
S5676	Zearalenone	<1 mg/mL	64 mg/mL	64 mg/mL
S5464	Psoralidin	<1 mg/mL	67 mg/mL	1 mg/mL
S5469	Bavachin	<1 mg/mL	64 mg/mL	45 mg/mL
S4883	Lynestrenol	-1 mg/mL	56 mg/mL	-1 mg/mL
S3929	Liquiritigenin	-1 mg/mL	51 mg/mL	-1 mg/mL
S2604	Dehydroepiandrosterone (DHEA)	<1 mg/mL	57 mg/mL	57 mg/mL
S2450	Equol	<1 mg/mL	48 mg/mL	48 mg/mL
S1727	Levonorgestrel	<1 mg/mL	45 mg/mL	2 mg/mL
S2567	Medroxyprogesterone acetate	<1 mg/mL	12 mg/mL	12 mg/mL
S2473	Hexestrol	<1 mg/mL	42 mg/mL	42 mg/mL
S1705	Progesterone	<1 mg/mL	22 mg/mL	63 mg/mL
S1859	Diethylstilbestrol	<1 mg/mL	54 mg/mL	54 mg/mL
S1625	Ethinyl Estradiol	<1 mg/mL	59 mg/mL	59 mg/mL
S3149	Estradiol valerate	<1 mg/mL	71 mg/mL	<1 mg/mL
S2125	Mestranol	<1 mg/mL	15 mg/mL	25 mg/mL
S4110	Estradiol Benzoate	<1 mg/mL	75 mg/mL	<1 mg/mL
S3167	Altrenogest	<1 mg/mL	62 mg/mL	2 mg/mL
S4046	Estradiol Cypionate	<1 mg/mL	79 mg/mL	55 mg/mL
S4638	Desogestrel	<1 mg/mL	62 mg/mL	62 mg/mL
S3657	Promestriene	3 mg/mL	65 mg/mL	65 mg/mL
S3635	Medroxyprogesterone	<1 mg/mL	68 mg/mL	14 mg/mL
S4674	Hydroxyprogesterone caproate	<1 mg/mL	85 mg/mL	85 mg/mL
S3671	Quinestrol	<1 mg/mL	72 mg/mL	72 mg/mL
S3718	Leuprolide Acetate	100 mg/mL	100 mg/mL	100 mg/mL
S4507	17-Hydroxyprogesterone	<1 mg/mL	66 mg/mL	66 mg/mL
S4673	Etonogestrel	<1 mg/mL	64 mg/mL	64 mg/mL
S7828	Licochalcone A	<1 mg/mL	67 mg/mL	67 mg/mL
S3160	Ethynodiol diacetate	77 mg/mL	77 mg/mL	<1 mg/mL
S2611	Ethisterone	<1 mg/mL	0.05 mg/mL	<1 mg/mL
S5393	Cyclofenil	-1 mg/mL	21 mg/mL	-1 mg/mL
S1776	Toremifene Citrate	<1 mg/mL	100 mg/mL	<1 mg/mL
S2128	Bazedoxifene HCl	<1 mg/mL	101 mg/mL	<1 mg/mL
S2561	Clomifene citrate	<1 mg/mL	120 mg/mL	11 mg/mL
S3081	Ulipristal	<1 mg/mL	83 mg/mL	14 mg/mL
S1914	Pregnenolone	<1 mg/mL	22 mg/mL	22 mg/mL
S2167	Bazedoxifene Acetate	<1 mg/mL	100 mg/mL	25 mg/mL
S4629	Chlorotrianisene	<1 mg/mL	76 mg/mL	<1 mg/mL
S7827	4-Hydroxytamoxifen	<1 mg/mL	77 mg/mL	<1 mg/mL
S2314	Kaempferol	<1 mg/mL	57 mg/mL	3 mg/mL
S4285	Ospemifene	<1 mg/mL	75 mg/mL	71 mg/mL
S1251	Dienogest	<1 mg/mL	62 mg/mL	<1 mg/mL
S1376	Gestodene	<1 mg/mL	62 mg/mL	8 mg/mL
S1377	Drospirenone	<1 mg/mL	73 mg/mL	11 mg/mL
S1665	Estrone	<1 mg/mL	54 mg/mL	<1 mg/mL

Isoform-specific Inhibitors

Estrogen/progestogen Receptor Inhibitors (61)
New Estrogen/progestogen Receptor Products

Catalog No.	Information	Product Use Citations	Product Validations
S9506^New	Danazol Danazol is a synthetic steroid with antigonadotropic and anti-estrogenic activities that acts as an anterior pituitary suppressant by inhibiting the pituitary output of gonadotropins.
S8372	AZD9496 AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models.		Kaempferol and ER /PR inhibitor suppress the migration and Rho activity of MCF-7 cells. Notes: (A) MCF-7 ER +/PR+ breast cancer cells were allowed to migrate in response to 20 μmol/L kaempferol and/or 0.1 nmol/L AZD9496 (ER inhibitor) and 200 μmol/L megestrol acetate (PR inhibitor) for 6 h. Results are presented as mean ± SD of 5 independent experiments. (B, C) MCF-7 cells were incubated with 20 μmol/L kaempferol and/or 0.1 nmol/L AZD9496 and 200 μmol/L MA for 1 h, and then subjected to the RhoA (B) and Rac1 (C) activity assays. The relative levels of Rho activity were normalized to the average value of controls. Results are presented as mean ± SD of 3 independent experiments. Abbreviations: AZD, AZD9496; Ctrl, control; ER, estrogen receptor; MA, megestrol acetate; ns, no significance; PR, progesterone receptor.
S5364^New	DY131 DY131 is a potent and selective ERRβ/γ activator. It has no effect on the structurally related receptors ERRalpha or the estrogen receptors alpha and beta (ERalpha/beta).
S1191	Fulvestrant Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay.	Oncogene, 2016, 10.1038/onc Mol Cancer Ther, 2014, 13(1):230-8 Biochim Biophys Acta, 2018, 1863(6):625-638	PTPH1 confers breast cancer cell sensitivity to fulvestrant. E and F, PTPH1 overexpression increases the growth inhibition by fulvestrant. PTPH1 was overexpressed by a Tet-on system or a stable transfection, and resultant cells were incubated with fulvestrant as indicated for about 2 weeks. Colony formed was stained and counted. Results shown are normalized to its own solvent control of Vector and PTPH1-overexpressed cells, respectively (means ± SD; n = 3–5) with insets showing PTPH1 overexpression. *, versus vector or no Tet cells for E and F.
S1972	Tamoxifen Citrate Tamoxifen Citrate is an antagonist of the estrogen receptor by competitive inhibition of estrogen binding.	University of North Texas, 2014, Timothy E. Richardson	Effects of DPN, LY500307, Raloxifene and Tamoxifen on cell viability in BSO-treated FRDA fibroblasts. BSO concentration was 1 mM and all steroid concentrations were 100 nM. Depicted are mean ± SD for n= 8 per group. * indicated p<0.05 versus BSO alone-treated cells.
S1227	Raloxifene HCl Raloxifene is an estrogen antagonist, which inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with IC50 of 5.7 nM.	Nature, 2018, 560(7718):372-376 Med Oncol, 2015, 32(6):577 University of North Texas, 2014, Health Science Center at Fort Worth
S2606	Mifepristone Mifepristone is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively.	Hippocampus, 2014, 24(5):528-40 PLoS One, 2014, 9(8):e105528	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.
S5437^New	4,4'-DDE DDE, a breakdown product of DDT, is an organochlorine pesticide and may behave as a potent androgen receptor antagonist.
S7855^New	Brilanestrant (GDC-0810, ARN-810) Brilanestrant (GDC-0810, ARN-810） is a potent ER-α binder (ER-α, IC50 = 6.1 nM; ER-β, IC50 = 8.8 nM), a full transcriptional antagonist with no agonism and displays good potency and efficacy in ER-α degradation (EC50 = 0.7 nM) and MCF-7 breast cancer cell viability (IC50 = 2.5 nM) assays with good selectivity over other nuclear hormone receptors.
S4896^New	Elagolix Sodium Elagolix Soidum is a potent, selective, orally active, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) with Kd value of 54 pM. Concentration at 10 μM shows no significant activity on ion channels, enzymes, and transporters (inhibition <50%).
S8686^New	PHTPP PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα.
S2466	Estriol Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
S1238	Tamoxifen Tamoxifen is an antagonist of the estrogen receptor in breast tissue.	Oncotarget, 2015, 6(4):2315-30 University of North Texas, 2014, Timothy E. Richardson	E, Analysis of BrCSC viability upon treatment with tamoxifen (tam) and fulvestrant (fulv) at the indicated doses. The experiments were performed in triplicates. ** P<0.01.
S7839	Endoxifen HCl Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.
S1709	Estradiol Estradiol, or more precisely, 17β-estradiol, is a human sex hormone and steroid, and the primary female sex hormone.
S5288^New	Estropipate Estropipate is a natural estrogenic substance composed of estrone sulfate and piperazine and is used mainly in menopausal hormone therapy in the treatment of menopausal symptoms.
S5676^New	Zearalenone Zearalenone is a non-steroidal estrogenic mycotoxin that acts by binding the estrogen receptor (ER).
S5464^New	Psoralidin Psoralidin, a naturally occurring coumestan isolated from the fractions of organic solvents such as ethylacetate, hexane, or n-butanol of the seed extract of Psoralea corylifolia L., has a variety of biological activities such as anticancer, antioxidant, antibacterial, antidepressant, anti-inflammatory activities, and regulation of insulin signaling. It is an agonist for both estrogen receptor (ER)α and ERβ with binding affinities (IC50s) of 1.03 and 24.6 μM, respectively.
S5469^New	Bavachin Bavachin is a phytoestrogen purified from natural herbal plants such as Psoralea corylifolia. It acts as a weak phytoestrogen by binding and activating the ER.
S4883^New	Lynestrenol Lynestrenol is a synthetic progestational hormone, an agonist of the progesterone receptor and has weak androgenic and estrogenic activity.
S3929^New	Liquiritigenin Liquiritigenin, the most active estrogenic compound from the root of Glycyrrhizae uralensis Fisch, selectively binds to ERβ with an IC50 value of 7.5 μM and activates multiple ER regulatory elements and native target genes with Erβ but not ERα.
S2604	Dehydroepiandrosterone (DHEA) Dehydroepiandrosterone is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.
S2450	Equol Equol ,a metabolite of soybeans, is an important isoflavone in humans，specifically binds to 5α-DHT, has a modest affinity for recombinant estrogen receptor ERβ. Phase 2.	ACS Chem Biol, 2015, 10.1021/cb5009487
S1727	Levonorgestrel Levonorgestrel is a female hormone that prevents ovulation.
S2567	Medroxyprogesterone acetate Medroxyprogesterone acetate (MPA) is a synthetic progestin and act as a potent progesterone receptor agonist, used to treat abnormal menstruation or irregular vaginal bleeding.	Mol Pain, 2015, 10.1186/s12990-015-0050-1	The analgesic effect of koumine was reversed in sciatic nerve chronic constriction injury rats by intrathecal treatment with medroxyprogesterone acetate. Medroxyprogesterone acetate (MPA) or dimethyl sulfoxide (DMSO, vehicle) was administered via an intrathecal catheter 10 days after sciatic nerve chronic constriction injury (CCI) surgery. After 30 min, koumine (7 mg kg−1 bw) or normal saline (NS) was administered by subcutaneous (s.c.) injection. The mechanical withdrawal threshold (MWT) of the hind paws was measured 1 h after completion of the drug or vehicle administration. The data are presented as the mean ± SEM (n = 6 per group) and were analyzed by one-way ANOVA followed by Bonferroni post hoc test at each time point. *P < 0.05 vs. the DMSO + NS group; # P < 0.05 vs. the DMSO + koumine group.
S2473	Hexestrol Hexestrol binds to ERα and ERβ with EC50 of 0.07 nM and 0.175 nM, respectively.
S1705	Progesterone Progesterone is an endogenous steroid hormone involved in the menstrual cycle, pregnancy, and embryogenesis of humans and other species. A potent agonist of the nuclear progesterone receptor (nPR) with Kd of 1 nM; An agonist of the membrane progesterone receptors(mPRs); An antagonist of the σ1 receptor.	Am J Cancer Res, 2015, 5(10):3210-20	SPOP inhibits progesterone-induced S phase entry and Erk1/2 activation. (A) T47D cells were transfected with control or Myc-SPOP constructs. After 24 hr, cells were treated with the vehicle ethanol (EtOH) or progesterone (10 nM) for 24 hr. The cell cycle percentages was determined by PI staining and FACS; (B) T47D cells were transfected with control siRNAs or SPOP-specific siRNAs. After 48 hr, cells were treated and analyzed as in (A); (C) T47D cells were transfected with control or Myc-SPOP constructs. After 24 hr, cells were treated with the vehicle ethanol (EtOH) or progesterone (10 nM) for indicated times. Cell lysates were prepared for WB analyses; (D) T47D cells were transfected with control or SPOP-specific siRNA. After 48 hr, cells were treated and analyzed as in (C).
S1859	Diethylstilbestrol Diethylstilbestrol is a synthetic nonsteroidal estrogen, used to prevent miscarriage and other pregnancy complications.
S1625	Ethinyl Estradiol Ethinyl Estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.
S3149	Estradiol valerate Estradiol is a synthetic ester used to treat menopausal symptoms and hormone deficiencies.
S2125	Mestranol Mestranol is the 3-methyl ether of ethinyl estradiol, which is a potent estrogen receptor agonist and used as oral contraceptives.
S4110	Estradiol Benzoate Estradiol benzoate is an estradiol analog which binds to the human, murine and chicken ERα with IC50 of 22-28 nM.
S3167	Altrenogest Altrenogest is a progestogen structurally related to veterinary steroid trenbolone.
S4046	Estradiol Cypionate Estradiol cypionate is the 17 β-cyclopentylpropinate ester of estradiol, which inhibits ET-1 synthesis via estrogen receptor.
S4638	Desogestrel Desogestrel is a synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents.
S3657	Promestriene Promestriene (3-propyl ethyl, 17B-methyl estradiol) is a synthetic estrogen analog that has been reported to significantly improve the symptoms of vaginal atrophy caused by estrogen deprivation in topical application.
S3635	Medroxyprogesterone Medroxyprogesterone (MP) is a synthetic pregnane steroid and a derivative of progesterone. It is a potent progesterone receptor agonist.
S4674	Hydroxyprogesterone caproate Hydroxyprogesterone Caproate is a synthetic progestational agent. It binds to and activates nuclear progesterone receptors in the reproductive system and inhibits ovulation and an alteration in the cervical mucus and endometrium.
S3671	Quinestrol Quinestrol is a synthetic, steroidal estrogen which is used in hormone replacement therapy and occasionally to treat breast cancer and prostate cancer.
S3718	Leuprolide Acetate Leuprolide acetate is a synthetic nonapeptide that is a potent gonadotropin-releasing hormone receptor (GnRHR) agonist used for diverse clinical applications, including the treatment of prostate cancer, endometriosis, uterine fibroids, central precocious puberty and in vitro fertilization techniques.
S4507	17-Hydroxyprogesterone 17-Hydroxyprogesterone (17-OHP) is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
S4673	Etonogestrel Etonogestrel is a synthetic form of the naturally occurring female sex hormone progesterone. It binds to the cytoplasmic progesterone receptors in the reproductive system and subsequently activates progesterone receptor mediated gene expression.
S7828	Licochalcone A Licochalcone A is an estrogenic flavanoid extracted from licorice root, showing antimalarial, anticancer, antibacterial and antiviral activities. Phase 3.
S3160	Ethynodiol diacetate Ethynodiol diacetate is one of the first synthetic progestogens used in contraceptive pills.
S2611	Ethisterone Ethisterone is a progestogen hormone being considered to treat prostate cancer.
S5393^New	Cyclofenil Cyclofenil is a selective estrogen receptor modulator showing a higher affinity for ERβ than Erα.
S1776	Toremifene Citrate Toremifene Citrate is an oral selective estrogen receptor modulator (SERM), used in the treatment of advanced breast cancer.	Nature, 2018, 560(7718):372-376 J Biomed Res, 2016, 30(5):393-410	D: Marginal degradation of MGMT in MCF7 cells treated with toremifene, a SERM. MGMT: O6-methylguanine DNA-methyltransferase; C: control.
S2128	Bazedoxifene HCl Bazedoxifene HCl is a novel, non-steroidal, indole-based estrogen receptor modulator (SERM) binding to both ERα and ERβ with IC50 of 23 nM and 89 nM, respectively.	J Med Chem, 2014, 57(3):632-41 J Med Chem, 2014, 57(3):632-41 PLoS One, 2016, 24;11(3):e0151182
S2561	Clomifene citrate Clomifene Citrate is a selective estrogen receptor modulator, used in the treatment of ovulation induction.	Oncotarget, 2017, 8(27):44255-44265	(a) Inhibitory activities of IDH1R132H enzyme lead to decreased production of D-2HG in IDH1R132H mutant HT1080 cells after treatment with clomifene for 48 h, and D-2HG was measured by LC/MS method. (b) HT1080 cells were treated for 24 h in the different concentrations of clomifene and then processed for FACS by using Annexin V/propidium iodide staining. (c) Treatment of clomifene significantly reduced methylation levels of histone lysine residues in HT1080 cells. All data are the average of results from triplicate experiments.
S3081	Ulipristal Ulipristal is a selective SPRM for emergency contraception after an unprotected intercourse or contraceptive failure.
S1914	Pregnenolone Pregnenolone is an endogenous steroid hormone, used in the treatment of fatigue, Alzheimer’s disease, trauma and injuries.
S2167	Bazedoxifene Acetate Bazedoxifene Acetate is a third generation selective estrogen receptor modulator (SERM).
S4629	Chlorotrianisene Chlorotrianisene is a synthetic, non-steroidal estrogen. It is a selective estrogen receptor modulator.
S7827	4-Hydroxytamoxifen 4-Hydroxytamoxifen is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer. It activates on-target modification frequency for intein-Cas9 variants.	Oncogene, 2017, 36(16):2255-2264 Oncogene, 2016, 10.1038/onc.2016.379	CDK4/6 inhibitor resistance promotes diminished ER expression and activity. (a and b) Proliferation of MCF-7 and MR cells in the presence of different concentrations of ICI (a) or 4-hydroxytamoxifen (4-OHT) (b) was measured by the alamarBlue assay and plotted as % inhibition of proliferation against log concentration of inhibitor. Each data point represents the average value±s.d. of six replicates obtained in three independent experiments.
S2314	Kaempferol Kaempferol, a natural flavonol, functions as an ERRα and ERRγ inverse agonist. It inhibits topoisomerase I catalyzed DNA religation and may also inhibit the activity of fatty acid synthase.	Food Funct, 2015, 6(8):2824-33 Cytotechnology, 2016, 68(4):1633-40	Total cellular protein was harvested after 8 days and the protein levels of adipogenic factors were measured using western blot analysis with specific antibodies (B).
S4285	Ospemifene Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM), used for the treatment of dyspareunia.
S9122^New	Tectorigenin Tectorigenin (TEC) is an isoflavone isolated from various medicinal plants, such as Pueraria thunbergiana Benth, Belamcanda chinensis, and Iris unguicularis. It has been reported to exert pharmacological actions, including antitumor and antibacterial effects, free radical neutralization, and selective estrogen receptor modulation.
S1251	Dienogest Dienogest is an orally active synthetic progesterone, used for contraception and the treatment of endometriosis.
S1376	Gestodene Gestodene is a progestogen hormonal contraceptive.
S1377	Drospirenone Drospirenone is a synthetic progestin that is an analog to spironolactone.
S1665	Estrone Estrone is an estrogenic hormone.

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Estrogen/progestogen Receptor

Signaling Pathway Map

Research Area

Isoform-specific Inhibitors