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Estrogen/progestogen Receptor
Isoform-selective Products
Signaling Pathway
Estrogen/progestogen Receptor Products
- All (103)
- Estrogen/progestogen Receptor Inhibitors (5)
- Estrogen/progestogen Receptor Activators (3)
- Estrogen/progestogen Receptor Antagonists (15)
- Estrogen/progestogen Receptor Agonists (45)
- Estrogen/progestogen Receptor Modulators (24)
- New Estrogen/progestogen Receptor Products
| Catalog No. | Product Name | Information | Product Use Citations | Product Validations |
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| S1191 | Fulvestrant | Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Fulvestrant also induces autophagy and apoptosis and has antitumor activity. |
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| S1238 | Tamoxifen | Tamoxifen is an orally active, selective estrogen receptor modulator (SERM) which exhibits both estrogenic agonist and antagonist effects. It blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. |
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| 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. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1. |
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| S7827 | 4-Hydroxytamoxifen (Afimoxifene) | 4-Hydroxytamoxifen (Afimoxifene) 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. |
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| S1972 | Tamoxifen Citrate | Tamoxifen Citrate is a selective estrogen receptor modulator (SERM). Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy. |
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| S1709 | Estradiol | Estradiol (17β-estradiol, β-Estradiol, E2, 17β-Oestradiol) is a human sex hormone and steroid, and the primary female sex hormone. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway. | ||
| S2128 | Bazedoxifene (WAY-140424) HCl | Bazedoxifene HCl (WAY-140424, TSE-424) 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. |
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| S1227 | Raloxifene HCl | Raloxifene (LY156758, Keoxifene) HCl is a selective and orally active estrogen receptor modulator (SERM), which inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with IC50 of 5.7 nM. |
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| S2561 | Clomifene citrate | Clomifene citrate (NSC 35770, Clomiphene citrate) is a selective estrogen receptor modulator, used in the treatment of ovulation induction. |
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| S2567 | MPA (Medroxyprogesterone acetate) | MPA (Medroxyprogesterone acetate) is a synthetic progestin and act as a potent progesterone receptor agonist, used to treat abnormal menstruation or irregular vaginal bleeding. |
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| S1304 | Megestrol Acetate | Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite. |
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| S4154 | Cholesterol | Cholesterol(Cholesterin) is the principal sterol of all higher animals required to build and maintain membranes. | ||
| 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. |
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| S1859 | Diethylstilbestrol | Diethylstilbestrol (Stilbestrol) is a synthetic nonsteroidal estrogen, used to prevent miscarriage and other pregnancy complications. | ||
| S1776 | Toremifene Citrate (NK 622) | Toremifene Citrate (NK 622, NSC 613680) is an oral selective estrogen receptor modulator (SERM), used in the treatment of advanced breast cancer. |
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| S7839 | Endoxifen HCl | Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2. | ||
| S2167 | Bazedoxifene acetate | Bazedoxifene acetate is a third generation selective estrogen receptor modulator (SERM). |
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| S6651 | G15 | G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER, GPR30) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM. | ||
| S7828 | Licochalcone A | Licochalcone A is an estrogenic flavanoid extracted from licorice root, showing antimalarial, anticancer, antibacterial and antiviral activities. Phase 3. | ||
| S1727 | Levonorgestrel | Levonorgestrel (D-Norgestrel) is a female hormone that prevents ovulation. | ||
| S4110 | Estradiol Benzoate | Estradiol benzoate(β-Estradiol 3-benzoate) is an estradiol analog which binds to the human, murine and chicken ERα with IC50 of 22-28 nM. | ||
| S8372 | AZD9496 | AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models. |
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| S8686 | PHTPP | PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα. | ||
| S1377 | Drospirenone | Drospirenone (ZK 3059) is a synthetic progestin that is an analog to spironolactone. | ||
| S3081 | Ulipristal Acetate (CDB 2914) | Ulipristal acetate (CDB-2914, HRP 2000, RU 44675) is a selective SPRM for emergency contraception after an unprotected intercourse or contraceptive failure. | ||
| S1625 | Ethinyl Estradiol | Ethinyl Estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills. | ||
| S1914 | Pregnenolone | Pregnenolone(3β-Hydroxy-5-pregnen-20-one) is an endogenous steroid hormone, used in the treatment of fatigue, Alzheimer’s disease, trauma and injuries. | ||
| S3929 | Liquiritigenin | Liquiritigenin (4',7-Dihydroxyflavanone), 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. | ||
| S7855 | Brilanestrant (GDC-0810) | 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. | ||
| S5781 | Raloxifene | Raloxifene (Keoxifene, Pharoxifene, LY-139481, LY-156758, CCRIS-7129) is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. | ||
| S4673 | Etonogestrel | Etonogestrel (Implanon, Nexplanon, 3-Oxodesogestrel, 3-keto-Desogestrel) 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. | ||
| S1598New | Erteberel (LY500307) | LY500307 is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, 32-fold selectivity against estrogen receptor α. Phase 2. | ||
| 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. | ||
| S2466 | Estriol | Estriol (NSC-12169) is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells. | ||
| S3149 | Estradiol valerate | Estradiol(E2V) is a synthetic ester used to treat menopausal symptoms and hormone deficiencies. | ||
| S1665 | Estrone | Estrone is an estrogenic hormone. | ||
| S9520 | Lasofoxifene Tartrate | Lasofoxifene Tartrate is a third-generation, non-steroidal selective estrogen receptor modulator (SERM) which binds with high affinity to the human estrogen receptor-α with IC50 value of 1.5 nM. | ||
| S4046 | Estradiol Cypionate | Estradiol cypionate is the 17 β-cyclopentylpropinate ester of estradiol, which inhibits ET-1 synthesis via estrogen receptor. | ||
| S2301 | Genistin (Genistoside) | Genistin (Genistoside, Genistine, Genistein 7-glucoside, Genistein glucoside) is an isoflavone found in a number of dietary plants like soy and kudzu. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of Estrogen Receptor α (ERα) signaling pathway. | ||
| S8956 | (Z)-4-Hydroxytamoxifen | (Z)-4-Hydroxytamoxifen ((Z)-4-OHT, trans-4-Hydroxytamoxifen, 4-Monohydroxytamoxifen) is a selective modulator of estrogen receptor (SERM) with IC50 of 3.3 nM for the [3H]oestradiol binding to oestrogen receptor. | ||
| S9629 | Elacestrant (RAD1901) Dihydrochloride | Elacestrant (RAD1901) Dihydrochloride is an orally available selective estrogen receptor degrader (SERD) with IC50 of 48 nM and 870 nM for ERα and ERβ, respectively. | ||
| S3449 | GSK5182 | GSK5182, 4-hydroxytamoxifen analog, is a specific inverse agonist of estrogen-related receptor γ (ERRγ) that inhibits pro-inflammatory cytokine-induced catabolic factors. | ||
| S1251 | Dienogest | Dienogest (STS 557) is an orally active synthetic progesterone, used for contraception and the treatment of endometriosis. | ||
| S1376 | Gestodene | Gestodene (SH B 331,WL 70) is a progestogen hormonal contraceptive. | ||
| S2473 | Hexestrol | Hexestrol (Bibenzyl) binds to ERα and ERβ with EC50 of 0.07 nM and 0.175 nM, respectively. | ||
| S2125 | Mestranol | Mestranol is the 3-methyl ether of ethinyl estradiol, which is a potent estrogen receptor agonist and used as oral contraceptives. | ||
| S3167 | Altrenogest | Altrenogest (A35957, RU2267,R2267) is a progestogen structurally related to veterinary steroid trenbolone. | ||
| E0527 | Norgestimate | Norgestimate, a synthetic progesterone analog, is an orally active progestin with highly selective progestational activity and minimal androgenicity. | ||
| S0503 | Estrogen receptor modulator 1 | Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM) with pIC50 of 0.46. Estrogen receptor modulator 1 exhibits potential anti-tumor activity. | ||
| S5872 | Estradiol dipropionate | Estradiol dipropionate (17-Beta-Estradiol-3,17-Dipropionate) is a semisynthetic, steroidal estrogen which has been used in hormone therapy for menopausal symptoms and low estrogen levels in women and in the treatment of gynecological disorders. | ||
| S3617 | (20S)-Protopanaxatriol | (20S)-Protopanaxatriol (g-PPT, 20(S)-APPT), a neuroprotective metabolite of ginsenoside, protopanaxatriol (g-PPT), is a functional ligand for both GR and ERbeta and could modulate endothelial cell functions through the glucocorticoid receptor (GR) and estrogen receptor (ER). | ||
| S9207 | Gypenoside XVII | Gypenoside XVII (GP-17, Gynosaponin S), a ginsenoside found in Panax species, has neuroprotective effects and is widely used to prevent cardiovascular disease.GP-17 treatment predominantly up-regulating the expression of ERα but not ERβ. | ||
| E1301New | Imlunestrant | Imlunestrant(LY3484356) is a potent, orally bioavailable selective estrogen receptor degrader (SERD) that functions as a pure antagonist of estrogen receptor alpha (ERα). It inhibits ER-dependent gene transcription and cell proliferation, resulting in sustained suppression of estrogen-driven growth in ER-positive cells. | ||
| S6927 | Dihydroresveratrol | Dihydroresveratrol is a natural product possessing significant biological activities. Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. | ||
| E0937 | Segesterone acetate | Segesterone acetate (Nestoron, ST-1435) is a synthetic progestin that binds to the progesterone receptor with EC50 of 50.3 nM. | ||
| E4845New | Ulipristal | Ulipristal(Deacetyl CDB-2914, CDB-3236) is a selective modulator of progesterone receptors used in a single dose as an emergency postcoital contraceptive. | ||
| S6601 | (±)-Equol | (±)-Equol, an isoflavandiol estrogen, is a metabolite of the soy isoflavones, daidzin and daidzein. | ||
| E0532 | Menotropin | Menotropin (Human Menopausal Gonadotrophin) is a hormonally active medication for the treatment of fertility disturbances, which are extracted from the urine of postmenopausal women. | ||
| E0361 | Enclomiphene Citrate | Enclomiphene citrate is the trans isomer of clomiphene citrate and acts as a non-steroidal estrogen receptor antagonist. |
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| S4629 | Chlorotrianisene | Chlorotrianisene (tri-p-anisylchloroethylene, TACE, CTA) is a synthetic, non-steroidal estrogen. It is a selective estrogen receptor modulator. | ||
| S8746 | H3B-5942 | H3B-5942 is a selective and irreversible estrogen receptor covalent antagonist, inactivates both ERα WT and ERα mutation. The Ki values are 1 nM and 0.41 nM, respectively. | ||
| S5676 | Zearalenone | Zearalenone (F2 toxin, RAL) is a non-steroidal estrogenic mycotoxin that acts by binding the estrogen receptor (ER). | ||
| E1903New | SLU-PP-332 | SLU-PP-332 is an agonist of pan-Estrogen Receptor/ERR with EC50 values of 98nM, 230nM, and 430 nM for ERRα, ERRβ, and ERRγ, respectively with the highest potency for ERRα. SLUPP-332 amplifies mitochondrial function and cellular respiration in skeletal muscle cell lines and also offers opportunities for researching metabolic ailments and enhancing muscle functionality. | ||
| S5288 | Estropipate | Estropipate (Piperazine estrone sulfate, Estrone sulfate piperazine salt, Pipestrone) 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. | ||
| S9862 | Vepdegestrant (ARV471) | Vepdegestrant (ARV471) is an orally bioavailable estrogen receptor-targeting (ER-targeting) PROTAC for the treatment of patients with locally advanced or metastatic ER+/HER2- breast cancer. | ||
| E0940 | Propyl pyrazole triol (PPT) | Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. | ||
| S5738 | Megestrol | Megestrol, a synthetic progestin, is approved for the treatment of anorexia, cachexia, or an unexplained significant weight loss in patients with an acquired immunodeficiency syndrome diagnosis. Megestrol acetate (Megace) is one of the first progestational agents to be evaluated for use in the hormonal therapy of advanced breast cancer. | ||
| S5785 | Norethindrone acetate | Norethindrone acetate (19-Norethindrone acetate, NA) is a common synthetic hormone used in oral contraceptives. Norethindrone acetate is a well-tolerated, effective option to manage pain and bleeding for all stages of endometriosis. | ||
| S4638 | Desogestrel | Desogestrel (Cerazette, Desogen, Desogestrelum, Org-2969) is a synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents. | ||
| S0358 | GSK4716 | GSK4716 is a selective agonist of Estrogen-Related Orphan Nuclear Receptors ERR and ERRγ with an IC50 of 2 µM in the ERRγ FRET assay. | ||
| S8687New | MPP dihydrochloride | Methyl-piperidino-pyrazole (MPP) dihydrochloride is a highly selective antagonist for estrogen receptor alpha (ERα), with an affinity 200 times greater than for estrogen receptor beta (ERβ). It inhibits 17β-estradiol binding to ERα by inducing conformational changes that alter the receptor’s binding site and also increases the energy required for genistein's interaction with ERα. | ||
| 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. | ||
| 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. |
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| S5219 | Allylestrenol | Allylestrenol is an orally active progestagen of the 19-nortestosterone series resembling progesterone. | ||
| S1858 | Dienestrol | Dienestrol(Restrol) is a synthetic, non-steroidal estrogen. It is an estrogen receptor agonist. | ||
| S4883 | Lynestrenol | Lynestrenol (Ethinylestrenol) is a synthetic progestational hormone, an agonist of the progesterone receptor and has weak androgenic and estrogenic activity. | ||
| E0707 | Nomegestrol Acetate | Nomegestrol Acetate is a potent, highly selective progestogen, which is characterized as a full agonist at the progesterone receptor, with no or minimal binding to other steroid receptors, including the androgen and glucocorticoid receptors. | ||
| 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 (17α-Hydroxyprogesterone hexanoate, 17α-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. | ||
| S0143 | WAY-200070 | WAY-200070 is a selective estrogen receptor β (ERRβ) agonist with an IC50 of 2.3 nM. | ||
| S3671 | Quinestrol | Quinestrol (Ethinylestradiol 3-cyclopentyl ether, EE2CPE, W-3566) is a synthetic, steroidal estrogen which is used in hormone replacement therapy and occasionally to treat breast cancer and prostate cancer. | ||
| S8958 | Camizestrant (AZD9833) | Camizestrant (AZD9833) is an orally available and selective estrogen receptor (ER) antagonist with antineoplastic activity. | ||
| S4097 | Dydrogesterone | Dydrogesterone (NSC 92336) is an orally active progestogen which acts directly on the uterus, producing a complete secretory endometrium in an estrogen-primed uterus. | ||
| S0407 | XCT790 | XCT-790 (Compound 12) is a potent and selective inverse agonist for estrogen-related receptor α (ERRα) with IC50 of 0.37 μM. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ. XCT-790 (Compound 12) significantly inhibits in vivo tumor growth and angiogenesis, and induces apoptosis. | ||
| S5910 | Alpha-Estradiol | Alpha-Estradiol (α-Estradiol, 17 alpha-Estradiol, Alfatradiol, Epiestradiol, Epiestrol, Alora, 17 α-E2), a natural, non-feminizing stereoisomer, a hormonally almost inactive isomer of physiological 17 beta-estradiol (17 β-E2), is a weak inhibitor of estrogen. | ||
| S5364 | 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). | ||
| S9609 | Amcenestrant (SAR439859) | Amcenestrant (SAR439859, compound 43d) is an orally available and nonsteroidal selective estrogen receptor degrader (SERD) with potential antineoplastic activity. SAR439859 is a potent estrogen receptor (ER) antagonist with EC50 of 0.2 nM for ERα degradation. | ||
| S0851 | G-1 (LNS 8801) | G-1 (LNS 8801) is a nonsteroidal and selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with Ki of 11 nM. | ||
| 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. | ||
| S9122 | 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. | ||
| E2401 | SPP-86 | SPP-86, a potent and selective cell permeable inhibitor of rearranged during transfection (RET) tyrosine kinase with an IC50 of 8 nM, inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells. | ||
| S4418 | Phenol Red sodium salt | Phenol Red sodium salt (Phenolsulfonephthalein sodium salt) is used ubiquitously as a pH indicator in tissue culture media ranging from 6.8 (yellow) to 8.2 (red). Phenol red binds to the estrogen receptor of MCF-7 human breast cancer cells. | ||
| S4440 | 2-Phenylacetamide | 2-Phenylacetamide, the main compound isolated from the seeds of Lepidium apetalum Willd (LA) with estrogenic activities, increases the expression of Estrogen receptorα (ERα), ERβ and GPR30 in the uterus and MCF-7 cells. | ||
| S5464 | 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. | ||
| E1842New | Palazestrant | Palazestrant(OP-1250) is an orally bioavailable complete antagonist of estrogen receptor (ER) that blocks ER activity. It exhibits antiproliferative and antitumor activity in ER-positive (ER+) breast cancer models. | ||
| S3160 | Ethynodiol diacetate | Ethynodiol diacetate (8080 CB,Ethynodiol acetate) is one of the first synthetic progestogens used in contraceptive pills. | ||
| E4947New | Estrone sulfate sodium | Estrone sulfate (Estrone 3-sulfate sodium salt, Premarin), an inactive form of estrogen, serves as a major circulating estrogen in the plasma. It is converted into the active form, estrone (E1), through the action of steroid sulfatase (STS. Estrone sulfate is commonly used in breast cancer research. | ||
| S4285 | Ospemifene | Ospemifene(FC-1271a) is a non-hormonal selective estrogen receptor modulator (SERM), used for the treatment of dyspareunia. | ||
| S2611 | Ethisterone | Ethisterone(17α-Ethynyltestosterone) is a progestogen hormone being considered to treat prostate cancer. | ||
| S6810 | Diarylpropionitrile (DPN) | Diarylpropionitrile (DPN) is a non-steroidal estrogen receptor β (ERβ) agonist with EC50 of 0.85 nM, 72-fold more selective for ERβ than ERα. | ||
| E4621New | BHPI | BHPI is a potent noncompetitive inhibitor of estrogen receptor α (ERα), which disrupts the protective estrogen–ERα-mediated activation of the unfolded protein response (UPR), leading to sustained UPR activation. It specifically inhibits the growth of drug-resistant ERα-positive breast and ovarian cancer cells and induces significant tumor regression in a mouse xenograft model of breast cancer. | ||
| S5393 | Cyclofenil | Cyclofenil is a selective estrogen receptor modulator showing a higher affinity for ERβ than Erα. | ||
| S5469 | Bavachin | Bavachin (Corylifolin) is a phytoestrogen purified from natural herbal plants such as Psoralea corylifolia. It acts as a weak phytoestrogen by binding and activating the ER. | ||
| S1304 | Megestrol Acetate | Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite. |
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| S8372 | AZD9496 | AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models. |
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| S5910 | Alpha-Estradiol | Alpha-Estradiol (α-Estradiol, 17 alpha-Estradiol, Alfatradiol, Epiestradiol, Epiestrol, Alora, 17 α-E2), a natural, non-feminizing stereoisomer, a hormonally almost inactive isomer of physiological 17 beta-estradiol (17 β-E2), is a weak inhibitor of estrogen. | ||
| E2401 | SPP-86 | SPP-86, a potent and selective cell permeable inhibitor of rearranged during transfection (RET) tyrosine kinase with an IC50 of 8 nM, inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells. | ||
| E4621New | BHPI | BHPI is a potent noncompetitive inhibitor of estrogen receptor α (ERα), which disrupts the protective estrogen–ERα-mediated activation of the unfolded protein response (UPR), leading to sustained UPR activation. It specifically inhibits the growth of drug-resistant ERα-positive breast and ovarian cancer cells and induces significant tumor regression in a mouse xenograft model of breast cancer. | ||
| S9207 | Gypenoside XVII | Gypenoside XVII (GP-17, Gynosaponin S), a ginsenoside found in Panax species, has neuroprotective effects and is widely used to prevent cardiovascular disease.GP-17 treatment predominantly up-regulating the expression of ERα but not ERβ. | ||
| S5364 | 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). | ||
| S4440 | 2-Phenylacetamide | 2-Phenylacetamide, the main compound isolated from the seeds of Lepidium apetalum Willd (LA) with estrogenic activities, increases the expression of Estrogen receptorα (ERα), ERβ and GPR30 in the uterus and MCF-7 cells. | ||
| S1191 | Fulvestrant | Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Fulvestrant also induces autophagy and apoptosis and has antitumor activity. |
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| 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. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1. |
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| S7839 | Endoxifen HCl | Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2. | ||
| S6651 | G15 | G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER, GPR30) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM. | ||
| S8686 | PHTPP | PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα. | ||
| S7855 | Brilanestrant (GDC-0810) | 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. | ||
| S2466 | Estriol | Estriol (NSC-12169) is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells. | ||
| E1301New | Imlunestrant | Imlunestrant(LY3484356) is a potent, orally bioavailable selective estrogen receptor degrader (SERD) that functions as a pure antagonist of estrogen receptor alpha (ERα). It inhibits ER-dependent gene transcription and cell proliferation, resulting in sustained suppression of estrogen-driven growth in ER-positive cells. | ||
| E0361 | Enclomiphene Citrate | Enclomiphene citrate is the trans isomer of clomiphene citrate and acts as a non-steroidal estrogen receptor antagonist. |
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| S8746 | H3B-5942 | H3B-5942 is a selective and irreversible estrogen receptor covalent antagonist, inactivates both ERα WT and ERα mutation. The Ki values are 1 nM and 0.41 nM, respectively. | ||
| S8687New | MPP dihydrochloride | Methyl-piperidino-pyrazole (MPP) dihydrochloride is a highly selective antagonist for estrogen receptor alpha (ERα), with an affinity 200 times greater than for estrogen receptor beta (ERβ). It inhibits 17β-estradiol binding to ERα by inducing conformational changes that alter the receptor’s binding site and also increases the energy required for genistein's interaction with ERα. | ||
| S8958 | Camizestrant (AZD9833) | Camizestrant (AZD9833) is an orally available and selective estrogen receptor (ER) antagonist with antineoplastic activity. | ||
| S9609 | Amcenestrant (SAR439859) | Amcenestrant (SAR439859, compound 43d) is an orally available and nonsteroidal selective estrogen receptor degrader (SERD) with potential antineoplastic activity. SAR439859 is a potent estrogen receptor (ER) antagonist with EC50 of 0.2 nM for ERα degradation. | ||
| S0851 | G-1 (LNS 8801) | G-1 (LNS 8801) is a nonsteroidal and selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with Ki of 11 nM. | ||
| E1842New | Palazestrant | Palazestrant(OP-1250) is an orally bioavailable complete antagonist of estrogen receptor (ER) that blocks ER activity. It exhibits antiproliferative and antitumor activity in ER-positive (ER+) breast cancer models. | ||
| S1709 | Estradiol | Estradiol (17β-estradiol, β-Estradiol, E2, 17β-Oestradiol) is a human sex hormone and steroid, and the primary female sex hormone. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway. | ||
| S2567 | MPA (Medroxyprogesterone acetate) | MPA (Medroxyprogesterone acetate) is a synthetic progestin and act as a potent progesterone receptor agonist, used to treat abnormal menstruation or irregular vaginal bleeding. |
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| S4154 | Cholesterol | Cholesterol(Cholesterin) is the principal sterol of all higher animals required to build and maintain membranes. | ||
| 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. |
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| S1859 | Diethylstilbestrol | Diethylstilbestrol (Stilbestrol) is a synthetic nonsteroidal estrogen, used to prevent miscarriage and other pregnancy complications. | ||
| S7828 | Licochalcone A | Licochalcone A is an estrogenic flavanoid extracted from licorice root, showing antimalarial, anticancer, antibacterial and antiviral activities. Phase 3. | ||
| S1727 | Levonorgestrel | Levonorgestrel (D-Norgestrel) is a female hormone that prevents ovulation. | ||
| S4110 | Estradiol Benzoate | Estradiol benzoate(β-Estradiol 3-benzoate) is an estradiol analog which binds to the human, murine and chicken ERα with IC50 of 22-28 nM. | ||
| S1625 | Ethinyl Estradiol | Ethinyl Estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills. | ||
| S3929 | Liquiritigenin | Liquiritigenin (4',7-Dihydroxyflavanone), 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. | ||
| S4673 | Etonogestrel | Etonogestrel (Implanon, Nexplanon, 3-Oxodesogestrel, 3-keto-Desogestrel) 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. | ||
| S1598New | Erteberel (LY500307) | LY500307 is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, 32-fold selectivity against estrogen receptor α. Phase 2. | ||
| 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. | ||
| S3149 | Estradiol valerate | Estradiol(E2V) is a synthetic ester used to treat menopausal symptoms and hormone deficiencies. | ||
| S4046 | Estradiol Cypionate | Estradiol cypionate is the 17 β-cyclopentylpropinate ester of estradiol, which inhibits ET-1 synthesis via estrogen receptor. | ||
| S9629 | Elacestrant (RAD1901) Dihydrochloride | Elacestrant (RAD1901) Dihydrochloride is an orally available selective estrogen receptor degrader (SERD) with IC50 of 48 nM and 870 nM for ERα and ERβ, respectively. | ||
| S3449 | GSK5182 | GSK5182, 4-hydroxytamoxifen analog, is a specific inverse agonist of estrogen-related receptor γ (ERRγ) that inhibits pro-inflammatory cytokine-induced catabolic factors. | ||
| S2473 | Hexestrol | Hexestrol (Bibenzyl) binds to ERα and ERβ with EC50 of 0.07 nM and 0.175 nM, respectively. | ||
| S2125 | Mestranol | Mestranol is the 3-methyl ether of ethinyl estradiol, which is a potent estrogen receptor agonist and used as oral contraceptives. | ||
| S3167 | Altrenogest | Altrenogest (A35957, RU2267,R2267) is a progestogen structurally related to veterinary steroid trenbolone. | ||
| S5872 | Estradiol dipropionate | Estradiol dipropionate (17-Beta-Estradiol-3,17-Dipropionate) is a semisynthetic, steroidal estrogen which has been used in hormone therapy for menopausal symptoms and low estrogen levels in women and in the treatment of gynecological disorders. | ||
| S3617 | (20S)-Protopanaxatriol | (20S)-Protopanaxatriol (g-PPT, 20(S)-APPT), a neuroprotective metabolite of ginsenoside, protopanaxatriol (g-PPT), is a functional ligand for both GR and ERbeta and could modulate endothelial cell functions through the glucocorticoid receptor (GR) and estrogen receptor (ER). | ||
| S6601 | (±)-Equol | (±)-Equol, an isoflavandiol estrogen, is a metabolite of the soy isoflavones, daidzin and daidzein. | ||
| S5676 | Zearalenone | Zearalenone (F2 toxin, RAL) is a non-steroidal estrogenic mycotoxin that acts by binding the estrogen receptor (ER). | ||
| E1903New | SLU-PP-332 | SLU-PP-332 is an agonist of pan-Estrogen Receptor/ERR with EC50 values of 98nM, 230nM, and 430 nM for ERRα, ERRβ, and ERRγ, respectively with the highest potency for ERRα. SLUPP-332 amplifies mitochondrial function and cellular respiration in skeletal muscle cell lines and also offers opportunities for researching metabolic ailments and enhancing muscle functionality. | ||
| S5288 | Estropipate | Estropipate (Piperazine estrone sulfate, Estrone sulfate piperazine salt, Pipestrone) 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. | ||
| E0940 | Propyl pyrazole triol (PPT) | Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. | ||
| S4638 | Desogestrel | Desogestrel (Cerazette, Desogen, Desogestrelum, Org-2969) is a synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents. | ||
| S0358 | GSK4716 | GSK4716 is a selective agonist of Estrogen-Related Orphan Nuclear Receptors ERR and ERRγ with an IC50 of 2 µM in the ERRγ FRET assay. | ||
| 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. | ||
| S1858 | Dienestrol | Dienestrol(Restrol) is a synthetic, non-steroidal estrogen. It is an estrogen receptor agonist. | ||
| S4883 | Lynestrenol | Lynestrenol (Ethinylestrenol) is a synthetic progestational hormone, an agonist of the progesterone receptor and has weak androgenic and estrogenic activity. | ||
| E0707 | Nomegestrol Acetate | Nomegestrol Acetate is a potent, highly selective progestogen, which is characterized as a full agonist at the progesterone receptor, with no or minimal binding to other steroid receptors, including the androgen and glucocorticoid receptors. | ||
| 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 (17α-Hydroxyprogesterone hexanoate, 17α-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. | ||
| S0143 | WAY-200070 | WAY-200070 is a selective estrogen receptor β (ERRβ) agonist with an IC50 of 2.3 nM. | ||
| S3671 | Quinestrol | Quinestrol (Ethinylestradiol 3-cyclopentyl ether, EE2CPE, W-3566) is a synthetic, steroidal estrogen which is used in hormone replacement therapy and occasionally to treat breast cancer and prostate cancer. | ||
| S4097 | Dydrogesterone | Dydrogesterone (NSC 92336) is an orally active progestogen which acts directly on the uterus, producing a complete secretory endometrium in an estrogen-primed uterus. | ||
| S0407 | XCT790 | XCT-790 (Compound 12) is a potent and selective inverse agonist for estrogen-related receptor α (ERRα) with IC50 of 0.37 μM. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ. XCT-790 (Compound 12) significantly inhibits in vivo tumor growth and angiogenesis, and induces apoptosis. | ||
| 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. | ||
| S5464 | 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. | ||
| S3160 | Ethynodiol diacetate | Ethynodiol diacetate (8080 CB,Ethynodiol acetate) is one of the first synthetic progestogens used in contraceptive pills. | ||
| S2611 | Ethisterone | Ethisterone(17α-Ethynyltestosterone) is a progestogen hormone being considered to treat prostate cancer. | ||
| S6810 | Diarylpropionitrile (DPN) | Diarylpropionitrile (DPN) is a non-steroidal estrogen receptor β (ERβ) agonist with EC50 of 0.85 nM, 72-fold more selective for ERβ than ERα. | ||
| S5469 | Bavachin | Bavachin (Corylifolin) is a phytoestrogen purified from natural herbal plants such as Psoralea corylifolia. It acts as a weak phytoestrogen by binding and activating the ER. | ||
| S1238 | Tamoxifen | Tamoxifen is an orally active, selective estrogen receptor modulator (SERM) which exhibits both estrogenic agonist and antagonist effects. It blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. |
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| S7827 | 4-Hydroxytamoxifen (Afimoxifene) | 4-Hydroxytamoxifen (Afimoxifene) 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. |
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| S1972 | Tamoxifen Citrate | Tamoxifen Citrate is a selective estrogen receptor modulator (SERM). Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy. |
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| S2128 | Bazedoxifene (WAY-140424) HCl | Bazedoxifene HCl (WAY-140424, TSE-424) 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. |
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| S1227 | Raloxifene HCl | Raloxifene (LY156758, Keoxifene) HCl is a selective and orally active estrogen receptor modulator (SERM), which inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with IC50 of 5.7 nM. |
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| S2561 | Clomifene citrate | Clomifene citrate (NSC 35770, Clomiphene citrate) is a selective estrogen receptor modulator, used in the treatment of ovulation induction. |
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| S1776 | Toremifene Citrate (NK 622) | Toremifene Citrate (NK 622, NSC 613680) is an oral selective estrogen receptor modulator (SERM), used in the treatment of advanced breast cancer. |
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| S2167 | Bazedoxifene acetate | Bazedoxifene acetate is a third generation selective estrogen receptor modulator (SERM). |
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| S3081 | Ulipristal Acetate (CDB 2914) | Ulipristal acetate (CDB-2914, HRP 2000, RU 44675) is a selective SPRM for emergency contraception after an unprotected intercourse or contraceptive failure. | ||
| S1914 | Pregnenolone | Pregnenolone(3β-Hydroxy-5-pregnen-20-one) is an endogenous steroid hormone, used in the treatment of fatigue, Alzheimer’s disease, trauma and injuries. | ||
| S5781 | Raloxifene | Raloxifene (Keoxifene, Pharoxifene, LY-139481, LY-156758, CCRIS-7129) is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. | ||
| S9520 | Lasofoxifene Tartrate | Lasofoxifene Tartrate is a third-generation, non-steroidal selective estrogen receptor modulator (SERM) which binds with high affinity to the human estrogen receptor-α with IC50 value of 1.5 nM. | ||
| S2301 | Genistin (Genistoside) | Genistin (Genistoside, Genistine, Genistein 7-glucoside, Genistein glucoside) is an isoflavone found in a number of dietary plants like soy and kudzu. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of Estrogen Receptor α (ERα) signaling pathway. | ||
| S8956 | (Z)-4-Hydroxytamoxifen | (Z)-4-Hydroxytamoxifen ((Z)-4-OHT, trans-4-Hydroxytamoxifen, 4-Monohydroxytamoxifen) is a selective modulator of estrogen receptor (SERM) with IC50 of 3.3 nM for the [3H]oestradiol binding to oestrogen receptor. | ||
| S0503 | Estrogen receptor modulator 1 | Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM) with pIC50 of 0.46. Estrogen receptor modulator 1 exhibits potential anti-tumor activity. | ||
| S6927 | Dihydroresveratrol | Dihydroresveratrol is a natural product possessing significant biological activities. Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. | ||
| E4845New | Ulipristal | Ulipristal(Deacetyl CDB-2914, CDB-3236) is a selective modulator of progesterone receptors used in a single dose as an emergency postcoital contraceptive. | ||
| S4629 | Chlorotrianisene | Chlorotrianisene (tri-p-anisylchloroethylene, TACE, CTA) is a synthetic, non-steroidal estrogen. It is a selective estrogen receptor modulator. | ||
| S5738 | Megestrol | Megestrol, a synthetic progestin, is approved for the treatment of anorexia, cachexia, or an unexplained significant weight loss in patients with an acquired immunodeficiency syndrome diagnosis. Megestrol acetate (Megace) is one of the first progestational agents to be evaluated for use in the hormonal therapy of advanced breast cancer. | ||
| 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. |
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| S9122 | 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. | ||
| S4418 | Phenol Red sodium salt | Phenol Red sodium salt (Phenolsulfonephthalein sodium salt) is used ubiquitously as a pH indicator in tissue culture media ranging from 6.8 (yellow) to 8.2 (red). Phenol red binds to the estrogen receptor of MCF-7 human breast cancer cells. | ||
| S4285 | Ospemifene | Ospemifene(FC-1271a) is a non-hormonal selective estrogen receptor modulator (SERM), used for the treatment of dyspareunia. | ||
| S5393 | Cyclofenil | Cyclofenil is a selective estrogen receptor modulator showing a higher affinity for ERβ than Erα. | ||
| S1598New | Erteberel (LY500307) | LY500307 is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, 32-fold selectivity against estrogen receptor α. Phase 2. | ||
| E1301New | Imlunestrant | Imlunestrant(LY3484356) is a potent, orally bioavailable selective estrogen receptor degrader (SERD) that functions as a pure antagonist of estrogen receptor alpha (ERα). It inhibits ER-dependent gene transcription and cell proliferation, resulting in sustained suppression of estrogen-driven growth in ER-positive cells. | ||
| E4845New | Ulipristal | Ulipristal(Deacetyl CDB-2914, CDB-3236) is a selective modulator of progesterone receptors used in a single dose as an emergency postcoital contraceptive. | ||
| E1903New | SLU-PP-332 | SLU-PP-332 is an agonist of pan-Estrogen Receptor/ERR with EC50 values of 98nM, 230nM, and 430 nM for ERRα, ERRβ, and ERRγ, respectively with the highest potency for ERRα. SLUPP-332 amplifies mitochondrial function and cellular respiration in skeletal muscle cell lines and also offers opportunities for researching metabolic ailments and enhancing muscle functionality. | ||
| S8687New | MPP dihydrochloride | Methyl-piperidino-pyrazole (MPP) dihydrochloride is a highly selective antagonist for estrogen receptor alpha (ERα), with an affinity 200 times greater than for estrogen receptor beta (ERβ). It inhibits 17β-estradiol binding to ERα by inducing conformational changes that alter the receptor’s binding site and also increases the energy required for genistein's interaction with ERα. | ||
| E1842New | Palazestrant | Palazestrant(OP-1250) is an orally bioavailable complete antagonist of estrogen receptor (ER) that blocks ER activity. It exhibits antiproliferative and antitumor activity in ER-positive (ER+) breast cancer models. | ||
| E4947New | Estrone sulfate sodium | Estrone sulfate (Estrone 3-sulfate sodium salt, Premarin), an inactive form of estrogen, serves as a major circulating estrogen in the plasma. It is converted into the active form, estrone (E1), through the action of steroid sulfatase (STS. Estrone sulfate is commonly used in breast cancer research. | ||
| E4621New | BHPI | BHPI is a potent noncompetitive inhibitor of estrogen receptor α (ERα), which disrupts the protective estrogen–ERα-mediated activation of the unfolded protein response (UPR), leading to sustained UPR activation. It specifically inhibits the growth of drug-resistant ERα-positive breast and ovarian cancer cells and induces significant tumor regression in a mouse xenograft model of breast cancer. |
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