- Inhibitory Selectivity
|Catalog No.||Product Name||Solubility(25°C)|
|S9506||Danazol||-1 mg/mL||67 mg/mL||-1 mg/mL|
|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|
|S5808||Relugolix||<1 mg/mL||61 mg/mL||<1 mg/mL|
|S5437||4,4'-DDE||-1 mg/mL||63 mg/mL||-1 mg/mL|
|S4896||Elagolix Sodium||100 mg/mL||100 mg/mL||100 mg/mL|
|S7855||Brilanestrant (GDC-0810, ARN-810)||<1 mg/mL||89 mg/mL||89 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|
|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|
|S3929||Liquiritigenin||-1 mg/mL||51 mg/mL||-1 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|
|S5781||Raloxifene||<1 mg/mL||95 mg/mL||10 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|
|s9122||Tectorigenin||-1 mg/mL||60 mg/mL||-1 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|
- Estrogen/progestogen Receptor Inhibitors (63)
- New Estrogen/progestogen Receptor Products
|Catalog No.||Information||Product Use Citations||Product Validations|
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.
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.
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).
Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay.
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.
Tamoxifen Citrate is an antagonist of the estrogen receptor by competitive inhibition of estrogen binding.
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.
Raloxifene is an estrogen antagonist, which inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with IC50 of 5.7 nM.
a, Quantification of sterol levels in OPCs (oligodendrocyte progenitor cells) treated with the indicated molecules at 2 μM.
Mifepristone is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively.
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.
Relugolix is a selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) with an IC50 of 0.12 nM.
DDE, a breakdown product of DDT, is an organochlorine pesticide and may behave as a potent androgen receptor antagonist.
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%).
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.
PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα.
Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
Tamoxifen is an antagonist of the estrogen receptor in breast tissue.
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.
Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.
Estradiol, or more precisely, 17β-estradiol, is a human sex hormone and steroid, and the primary female sex hormone.
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.
Zearalenone is a non-steroidal estrogenic mycotoxin that acts by binding the estrogen receptor (ER).
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.
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.
Lynestrenol is a synthetic progestational hormone, an agonist of the progesterone receptor and has weak androgenic and estrogenic activity.
Dehydroepiandrosterone is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.
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.
Levonorgestrel is a female hormone that prevents ovulation.
Medroxyprogesterone acetate (MPA) is a synthetic progestin and act as a potent progesterone receptor agonist, used to treat abnormal menstruation or irregular vaginal bleeding.
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.
Hexestrol binds to ERα and ERβ with EC50 of 0.07 nM and 0.175 nM, respectively.
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.
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).
Diethylstilbestrol is a synthetic nonsteroidal estrogen, used to prevent miscarriage and other pregnancy complications.
Ethinyl Estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.
Estradiol is a synthetic ester used to treat menopausal symptoms and hormone deficiencies.
Mestranol is the 3-methyl ether of ethinyl estradiol, which is a potent estrogen receptor agonist and used as oral contraceptives.
Estradiol benzoate is an estradiol analog which binds to the human, murine and chicken ERα with IC50 of 22-28 nM.
Altrenogest is a progestogen structurally related to veterinary steroid trenbolone.
Estradiol cypionate is the 17 β-cyclopentylpropinate ester of estradiol, which inhibits ET-1 synthesis via estrogen receptor.
Desogestrel is a synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents.
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.
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.
Medroxyprogesterone (MP) is a synthetic pregnane steroid and a derivative of progesterone. It is a potent progesterone receptor agonist.
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.
Quinestrol is a synthetic, steroidal estrogen which is used in hormone replacement therapy and occasionally to treat breast cancer and prostate cancer.
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.
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.
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.
Licochalcone A is an estrogenic flavanoid extracted from licorice root, showing antimalarial, anticancer, antibacterial and antiviral activities. Phase 3.
Ethynodiol diacetate is one of the first synthetic progestogens used in contraceptive pills.
Ethisterone is a progestogen hormone being considered to treat prostate cancer.
Raloxifene is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women.
Cyclofenil is a selective estrogen receptor modulator showing a higher affinity for ERβ than Erα.
Toremifene Citrate is an oral selective estrogen receptor modulator (SERM), used in the treatment of advanced breast cancer.
Representative images of OPCs treated for 72 h with the indicated small molecules. All molecules were used at 300 nM. Scale bar, 100 μm.
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.
Clomifene Citrate is a selective estrogen receptor modulator, used in the treatment of ovulation induction.
(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.
Ulipristal is a selective SPRM for emergency contraception after an unprotected intercourse or contraceptive failure.
Pregnenolone is an endogenous steroid hormone, used in the treatment of fatigue, Alzheimer’s disease, trauma and injuries.
Bazedoxifene Acetate is a third generation selective estrogen receptor modulator (SERM).
Chlorotrianisene is a synthetic, non-steroidal estrogen. It is a selective estrogen receptor modulator.
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.
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.
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.
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).
Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM), used for the treatment of dyspareunia.
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.
Dienogest is an orally active synthetic progesterone, used for contraception and the treatment of endometriosis.
Gestodene is a progestogen hormonal contraceptive.
Drospirenone is a synthetic progestin that is an analog to spironolactone.
Estrone is an estrogenic hormone.