E2401New |
SPP-86
|
|
|
|
S1304 |
Megestrol Acetate
|
Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite. |
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Hum Cell, 2021, 34(6):1911-1918
-
Hum Cell, 2021, 10.1007/s13577-021-00639-4
|
|
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. |
|
|
S8372 |
AZD9496
|
AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models. |
-
Breast Cancer Res Treat, 2020, 10.1007/s10549-020-05575-9
-
Onco Targets Ther, 2017, 10:4809-4819
|
|
S9506 |
Danazol
|
Danazol (WIN-17757, 2,3-Isoxazolethisterone) is a synthetic steroid with antigonadotropic and anti-estrogenic activities that acts as an anterior pituitary suppressant by inhibiting the pituitary output of gonadotropins. |
|
|
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. |
|
|
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). |
|
|
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. |
|
|
E0361New |
Enclomiphene Citrate
|
Enclomiphene citrate is the trans isomer of clomiphene citrate and acts as a non-steroidal estrogen receptor antagonist.
|
|
|
S0851 |
G-1
|
G-1 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. |
|
|
S1191 |
Fulvestrant (ICI-182780)
|
Fulvestrant (ICI-182780, ZD 9238, ZM 182780) 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. |
-
Mol Cancer Ther, 2022, 21(1):48-57
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
J Food Biochem, 2022, 10.1111/jfbc.14163
|
|
S2466 |
Estriol
|
Estriol (NSC-12169) is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells. |
-
Mol Cell, 2019, 75(6):1103-1116.e9
|
|
S2606 |
Mifepristone (RU486)
|
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 and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1. |
-
Nat Commun, 2021, 12(1):7041
-
Exp Eye Res, 2021, S0014-4835(21)00331-6
-
Oncol Rep, 2021, 46(3)202
|
|
S6651 |
G15 (GRB-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. |
-
Steroids, 2021, 177:108935
-
Cell Biochem Funct, 2020, 38(1):38-46
|
|
S7839 |
Endoxifen HCl
|
Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.
|
-
Blood Cancer J, 2022, 12(3):36
-
J Mol Cell Biol, 2021, mjab018
-
ACS Omega, 2021, 6(42):27654-27667
|
|
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. |
-
Breast Cancer Res Treat, 2020, 10.1007/s10549-020-05575-9
-
Nat Genet, 2019, 51(2):207-216
|
|
S8686 |
PHTPP
|
PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα. |
-
J Cancer, 2022, 13(5):1573-1587
-
Brain Res, 2021, 1768:147580
-
Ecotoxicol Environ Saf, 2020, 208:111429
|
|
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. |
|
|
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. |
|
|
E0707New |
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. |
|
|
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. |
|
|
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. |
|
|
S1625 |
Ethinyl Estradiol
|
Ethinyl Estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills. |
-
Hum Mol Genet, 2020, ddaa244
-
Regul Toxicol Pharmacol, 2020, S0273-2300(20)30246-4
|
|
S1705 |
Progesterone (NSC 9704)
|
Progesterone (NSC 9704, NSC 64377, Pregn-4-ene-3,20-dione) 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. |
-
Stem Cells Transl Med, 2022, 11(5):552-565
-
Thorac Cancer, 2020, 10.1111/1759-7714.13528
-
Mol Cell, 2019, 75(6):1103-1116.e9
|
|
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. |
-
Cell Chem Biol, 2022, S2451-9456(22)00006-X
-
Sci Adv, 2021, 7(43):eabh1022
-
Cancer Lett, 2021, 513:36-49
|
|
S1727 |
Levonorgestrel
|
Levonorgestrel (D-Norgestrel) is a female hormone that prevents ovulation. |
-
J Control Release, 2021, S0168-3659(21)00550-2
-
Nat Cancer, 2020, 1(2):235-248
|
|
S1858 |
Dienestrol
|
Dienestrol(Restrol) is a synthetic, non-steroidal estrogen. It is an estrogen receptor agonist. |
|
|
S1859 |
Diethylstilbestrol
|
Diethylstilbestrol (Stilbestrol) is a synthetic nonsteroidal estrogen, used to prevent miscarriage and other pregnancy complications. |
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Hum Cell, 2021, 34(6):1911-1918
-
Hum Cell, 2021, 10.1007/s13577-021-00579-z
|
|
S2125 |
Mestranol
|
Mestranol is the 3-methyl ether of ethinyl estradiol, which is a potent estrogen receptor agonist and used as oral contraceptives. |
|
|
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
|
|
S2473 |
Hexestrol
|
Hexestrol (Bibenzyl) binds to ERα and ERβ with EC50 of 0.07 nM and 0.175 nM, respectively. |
|
|
S2567 |
Medroxyprogesterone acetate (NSC-26386)
|
Medroxyprogesterone acetate (MPA, NSC-26386, Medroxyprogesterone 17-acetate, Farlutin) is a synthetic progestin and act as a potent progesterone receptor agonist, used to treat abnormal menstruation or irregular vaginal bleeding. |
-
Front Oncol, 2021, 11:665832
-
Research Square, 2020, 10.21203/rs.3.rs-30247/v1
-
EBioMedicine, 2019, 44:563-573
|
|
S2604 |
Dehydroepiandrosterone (DHEA)
|
Dehydroepiandrosterone (DHEA, Prasterone, Dehydroisoandrosterone) is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist. |
-
Stem Cell Rev Rep, 2021, 10.1007/s12015-021-10239-2
-
J Chromatogr B Analyt Technol Biomed Life Sci, 2021, 1186:123002
-
SSRN, 2021, 10.2139/ssrn.3886996
|
|
S2611 |
Ethisterone
|
Ethisterone is a progestogen hormone being considered to treat prostate cancer. |
|
|
S3149 |
Estradiol valerate
|
Estradiol is a synthetic ester used to treat menopausal symptoms and hormone deficiencies. |
|
|
S3160 |
Ethynodiol diacetate
|
Ethynodiol diacetate (8080 CB) is one of the first synthetic progestogens used in contraceptive pills. |
|
|
S3167 |
Altrenogest
|
Altrenogest (A35957, RU2267) is a progestogen structurally related to veterinary steroid trenbolone. |
|
|
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. |
|
|
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). |
|
|
S3635 |
Medroxyprogesterone
|
Medroxyprogesterone (MP) is a synthetic pregnane steroid and a derivative of progesterone. It is a potent progesterone receptor agonist. |
|
|
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. |
|
|
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. |
|
|
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. |
-
Mol Med Rep, 2021, 24(4)686
-
Mol Med Rep, 2021, 24(4)686
|
|
S4046 |
Estradiol Cypionate
|
Estradiol cypionate is the 17 β-cyclopentylpropinate ester of estradiol, which inhibits ET-1 synthesis via estrogen receptor. |
-
Autophagy, 2016, 12(9):1593-613
|
|
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. |
|
|
S4110 |
Estradiol Benzoate
|
Estradiol benzoate is an estradiol analog which binds to the human, murine and chicken ERα with IC50 of 22-28 nM. |
-
Front Pharmacol, 2022, 13:841941
-
Nutr Metab (Lond), 2021, 18(1):63
|
|
S4154 |
Cholesterol
|
Cholesterol is the principal sterol of all higher animals required to build and maintain membranes. |
-
Nat Commun, 2022, 13(1):791
-
EMBO Mol Med, 2022, 14(2):e14903
-
EMBO Rep, 2021, e52537
|
|
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. |
|
|
S4638 |
Desogestrel
|
Desogestrel (Cerazette, Desogen, Desogestrelum, Org-2969) is a synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents. |
|
|
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. |
|
|
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. |
|
|
S4883 |
Lynestrenol
|
Lynestrenol (Ethinylestrenol) is a synthetic progestational hormone, an agonist of the progesterone receptor and has weak androgenic and estrogenic activity. |
|
|
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. |
|
|
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. |
|
|
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. |
|
|
S5676 |
Zearalenone
|
Zearalenone (F2 toxin, RAL) is a non-steroidal estrogenic mycotoxin that acts by binding the estrogen receptor (ER). |
-
Cell Res, 2022, 10.1038/s41422-022-00668-0
|
|
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. |
|
|
S6601 |
(±)-Equol
|
(±)-Equol, an isoflavandiol estrogen, is a metabolite of the soy isoflavones, daidzin and daidzein. |
|
|
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. |
|
|
S7828 |
Licochalcone A
|
Licochalcone A is an estrogenic flavanoid extracted from licorice root, showing antimalarial, anticancer, antibacterial and antiviral activities. Phase 3.
|
-
Biomed Res Int, 2022, 2022:5687832
-
Environ Toxicol, 2021, 10.1002/tox.23422
|
|
S9629New |
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. |
|
|
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. |
|
|
S1227 |
Raloxifene HCl
|
Raloxifene (LY156758, Keoxifene) HCl 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. |
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
-
Hum Cell, 2021, 10.1007/s13577-021-00639-4
|
|
S1238 |
Tamoxifen (ICI 46474)
|
Tamoxifen (ICI 46474, (Z)-Tamoxifen, trans-Tamoxifen) is a selective estrogen receptor modulator (SERM). Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis. |
-
Blood Cancer J, 2022, 12(3):36
-
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
-
Cancers (Basel), 2021, 13(9)2116
|
|
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. |
-
Endocrinology, 2021, 162(10)bqab142
-
bioRxiv, 2020, 2020/9/20.4.7.30734
-
J Virol, 2019, 93(8)
|
|
S1914 |
Pregnenolone
|
Pregnenolone is an endogenous steroid hormone, used in the treatment of fatigue, Alzheimer’s disease, trauma and injuries. |
-
J Sep Sci, 2019, 42(10):1833-1841
-
Phytother Res, 2018, 32(6):996-1003
|
|
S1972 |
Tamoxifen (ICI 46474) Citrate
|
Tamoxifen Citrate (ICI 46474) 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. |
-
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
-
Cancers (Basel), 2021, 13(9)2116
-
Cell Death Dis, 2021, 12(6):619
|
|
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. |
-
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
-
Cell Chem Biol, 2021, S2451-9456(21)00400-1
-
Transl Oncol, 2021, 14(11):101192
|
|
S2167 |
Bazedoxifene (TSE-424) acetate
|
Bazedoxifene Acetate (WAY-140424, TSE-424) is a third generation selective estrogen receptor modulator (SERM). |
-
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
-
Transl Oncol, 2021, 14(11):101192
-
Mol Cancer Ther, 2020, 7 pii: molcanther
|
|
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. |
-
Acta Biomater, 2021, S1742-7061(21)00586-9
|
|
S2314 |
Kaempferol (NSC 407289)
|
Kaempferol (NSC 407289, Robigenin), 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. |
-
Molecules, 2021, 26(5)1210
-
Eur J Pharmacol, 2021, 907:174251
-
Nat Metab, 2021, 10.1038/s42255-021-00479-4
|
|
S2561 |
Clomifene citrate
|
Clomifene citrate (NSC 35770, Clomiphene citrate) is a selective estrogen receptor modulator, used in the treatment of ovulation induction. |
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Hum Cell, 2021, 34(6):1911-1918
-
Hum Cell, 2021, 10.1007/s13577-021-00579-z
|
|
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. |
-
J Clin Endocrinol Metab, 2019, 104(12):6256-6264
-
Cell Prolif, 2017, 50(5)
|
|
S4285 |
Ospemifene
|
Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM), used for the treatment of dyspareunia.
|
|
|
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. |
|
|
S4629 |
Chlorotrianisene
|
Chlorotrianisene (tri-p-anisylchloroethylene, TACE, CTA) is a synthetic, non-steroidal estrogen. It is a selective estrogen receptor modulator. |
|
|
S5393 |
Cyclofenil
|
Cyclofenil is a selective estrogen receptor modulator showing a higher affinity for ERβ than Erα. |
|
|
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. |
|
|
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. |
-
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
-
Drug Test Anal, 2020, 10.1002/dta.2917
|
|
S6927New |
Dihydroresveratrol
|
Dihydroresveratrol is a natural product possessing significant biological activities. Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. |
|
|
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. |
-
Nucleic Acids Res, 2022, 50(5):2836-2853
-
Sci Adv, 2021, 7(43):eabh1022
-
Nat Commun, 2021, 12(1):6020
|
|
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. |
|
|
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. |
|
|
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. |
-
Mol Cancer Res, 2021, 19(6):1026-1039
|
|
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) is a progestogen hormonal contraceptive. |
|
|
S1377 |
Drospirenone
|
Drospirenone (ZK 3059) is a synthetic progestin that is an analog to spironolactone. |
-
Nat Cancer, 2020, 1(2):235-248
-
J Thromb Haemost, 2015, 13(10):1918-24
|
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S1665 |
Estrone
|
Estrone is an estrogenic hormone. |
-
Mol Cell, 2019, 75(6):1103-1116.e9
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S5219 |
Allylestrenol
|
Allylestrenol is an orally active progestagen of the 19-nortestosterone series resembling progesterone. |
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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. |
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E0707New |
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. |
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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. |
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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. |
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S1625 |
Ethinyl Estradiol
|
Ethinyl Estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills. |
- Hum Mol Genet, 2020, ddaa244
- Regul Toxicol Pharmacol, 2020, S0273-2300(20)30246-4
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S1705 |
Progesterone (NSC 9704)
|
Progesterone (NSC 9704, NSC 64377, Pregn-4-ene-3,20-dione) 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. |
- Stem Cells Transl Med, 2022, 11(5):552-565
- Thorac Cancer, 2020, 10.1111/1759-7714.13528
- Mol Cell, 2019, 75(6):1103-1116.e9
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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. |
- Cell Chem Biol, 2022, S2451-9456(22)00006-X
- Sci Adv, 2021, 7(43):eabh1022
- Cancer Lett, 2021, 513:36-49
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S1727 |
Levonorgestrel
|
Levonorgestrel (D-Norgestrel) is a female hormone that prevents ovulation. |
- J Control Release, 2021, S0168-3659(21)00550-2
- Nat Cancer, 2020, 1(2):235-248
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S1858 |
Dienestrol
|
Dienestrol(Restrol) is a synthetic, non-steroidal estrogen. It is an estrogen receptor agonist. |
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S1859 |
Diethylstilbestrol
|
Diethylstilbestrol (Stilbestrol) is a synthetic nonsteroidal estrogen, used to prevent miscarriage and other pregnancy complications. |
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Hum Cell, 2021, 34(6):1911-1918
- Hum Cell, 2021, 10.1007/s13577-021-00579-z
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S2125 |
Mestranol
|
Mestranol is the 3-methyl ether of ethinyl estradiol, which is a potent estrogen receptor agonist and used as oral contraceptives. |
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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
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S2473 |
Hexestrol
|
Hexestrol (Bibenzyl) binds to ERα and ERβ with EC50 of 0.07 nM and 0.175 nM, respectively. |
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S2567 |
Medroxyprogesterone acetate (NSC-26386)
|
Medroxyprogesterone acetate (MPA, NSC-26386, Medroxyprogesterone 17-acetate, Farlutin) is a synthetic progestin and act as a potent progesterone receptor agonist, used to treat abnormal menstruation or irregular vaginal bleeding. |
- Front Oncol, 2021, 11:665832
- Research Square, 2020, 10.21203/rs.3.rs-30247/v1
- EBioMedicine, 2019, 44:563-573
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S2604 |
Dehydroepiandrosterone (DHEA)
|
Dehydroepiandrosterone (DHEA, Prasterone, Dehydroisoandrosterone) is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist. |
- Stem Cell Rev Rep, 2021, 10.1007/s12015-021-10239-2
- J Chromatogr B Analyt Technol Biomed Life Sci, 2021, 1186:123002
- SSRN, 2021, 10.2139/ssrn.3886996
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S2611 |
Ethisterone
|
Ethisterone is a progestogen hormone being considered to treat prostate cancer. |
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S3149 |
Estradiol valerate
|
Estradiol is a synthetic ester used to treat menopausal symptoms and hormone deficiencies. |
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S3160 |
Ethynodiol diacetate
|
Ethynodiol diacetate (8080 CB) is one of the first synthetic progestogens used in contraceptive pills. |
|
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S3167 |
Altrenogest
|
Altrenogest (A35957, RU2267) is a progestogen structurally related to veterinary steroid trenbolone. |
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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. |
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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). |
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S3635 |
Medroxyprogesterone
|
Medroxyprogesterone (MP) is a synthetic pregnane steroid and a derivative of progesterone. It is a potent progesterone receptor agonist. |
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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. |
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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. |
|
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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. |
- Mol Med Rep, 2021, 24(4)686
- Mol Med Rep, 2021, 24(4)686
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S4046 |
Estradiol Cypionate
|
Estradiol cypionate is the 17 β-cyclopentylpropinate ester of estradiol, which inhibits ET-1 synthesis via estrogen receptor. |
- Autophagy, 2016, 12(9):1593-613
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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. |
|
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S4110 |
Estradiol Benzoate
|
Estradiol benzoate is an estradiol analog which binds to the human, murine and chicken ERα with IC50 of 22-28 nM. |
- Front Pharmacol, 2022, 13:841941
- Nutr Metab (Lond), 2021, 18(1):63
|
|
S4154 |
Cholesterol
|
Cholesterol is the principal sterol of all higher animals required to build and maintain membranes. |
- Nat Commun, 2022, 13(1):791
- EMBO Mol Med, 2022, 14(2):e14903
- EMBO Rep, 2021, e52537
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|
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. |
|
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S4638 |
Desogestrel
|
Desogestrel (Cerazette, Desogen, Desogestrelum, Org-2969) is a synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents. |
|
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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. |
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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. |
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S4883 |
Lynestrenol
|
Lynestrenol (Ethinylestrenol) is a synthetic progestational hormone, an agonist of the progesterone receptor and has weak androgenic and estrogenic activity. |
|
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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. |
|
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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. |
|
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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. |
|
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S5676 |
Zearalenone
|
Zearalenone (F2 toxin, RAL) is a non-steroidal estrogenic mycotoxin that acts by binding the estrogen receptor (ER). |
- Cell Res, 2022, 10.1038/s41422-022-00668-0
|
|
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. |
|
|
S6601 |
(±)-Equol
|
(±)-Equol, an isoflavandiol estrogen, is a metabolite of the soy isoflavones, daidzin and daidzein. |
|
|
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. |
|
|
S7828 |
Licochalcone A
|
Licochalcone A is an estrogenic flavanoid extracted from licorice root, showing antimalarial, anticancer, antibacterial and antiviral activities. Phase 3.
|
- Biomed Res Int, 2022, 2022:5687832
- Environ Toxicol, 2021, 10.1002/tox.23422
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S9629New |
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. |
|
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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. |
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S1227 |
Raloxifene HCl
|
Raloxifene (LY156758, Keoxifene) HCl 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. |
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
- Hum Cell, 2021, 10.1007/s13577-021-00639-4
|
|
S1238 |
Tamoxifen (ICI 46474)
|
Tamoxifen (ICI 46474, (Z)-Tamoxifen, trans-Tamoxifen) is a selective estrogen receptor modulator (SERM). Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis. |
- Blood Cancer J, 2022, 12(3):36
- Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
- Cancers (Basel), 2021, 13(9)2116
|
|
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. |
- Endocrinology, 2021, 162(10)bqab142
- bioRxiv, 2020, 2020/9/20.4.7.30734
- J Virol, 2019, 93(8)
|
|
S1914 |
Pregnenolone
|
Pregnenolone is an endogenous steroid hormone, used in the treatment of fatigue, Alzheimer’s disease, trauma and injuries. |
- J Sep Sci, 2019, 42(10):1833-1841
- Phytother Res, 2018, 32(6):996-1003
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|
S1972 |
Tamoxifen (ICI 46474) Citrate
|
Tamoxifen Citrate (ICI 46474) 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. |
- Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
- Cancers (Basel), 2021, 13(9)2116
- Cell Death Dis, 2021, 12(6):619
|
|
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. |
- Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
- Cell Chem Biol, 2021, S2451-9456(21)00400-1
- Transl Oncol, 2021, 14(11):101192
|
|
S2167 |
Bazedoxifene (TSE-424) acetate
|
Bazedoxifene Acetate (WAY-140424, TSE-424) is a third generation selective estrogen receptor modulator (SERM). |
- Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
- Transl Oncol, 2021, 14(11):101192
- Mol Cancer Ther, 2020, 7 pii: molcanther
|
|
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. |
- Acta Biomater, 2021, S1742-7061(21)00586-9
|
|
S2314 |
Kaempferol (NSC 407289)
|
Kaempferol (NSC 407289, Robigenin), 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. |
- Molecules, 2021, 26(5)1210
- Eur J Pharmacol, 2021, 907:174251
- Nat Metab, 2021, 10.1038/s42255-021-00479-4
|
|
S2561 |
Clomifene citrate
|
Clomifene citrate (NSC 35770, Clomiphene citrate) is a selective estrogen receptor modulator, used in the treatment of ovulation induction. |
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Hum Cell, 2021, 34(6):1911-1918
- Hum Cell, 2021, 10.1007/s13577-021-00579-z
|
|
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. |
- J Clin Endocrinol Metab, 2019, 104(12):6256-6264
- Cell Prolif, 2017, 50(5)
|
|
S4285 |
Ospemifene
|
Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM), used for the treatment of dyspareunia.
|
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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. |
|
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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. |
|
|
S5393 |
Cyclofenil
|
Cyclofenil is a selective estrogen receptor modulator showing a higher affinity for ERβ than Erα. |
|
|
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. |
|
|
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. |
- Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
- Drug Test Anal, 2020, 10.1002/dta.2917
|
|
S6927New |
Dihydroresveratrol
|
Dihydroresveratrol is a natural product possessing significant biological activities. Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. |
|
|
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. |
- Nucleic Acids Res, 2022, 50(5):2836-2853
- Sci Adv, 2021, 7(43):eabh1022
- Nat Commun, 2021, 12(1):6020
|
|
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. |
|
|
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. |
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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. |
- Mol Cancer Res, 2021, 19(6):1026-1039
|
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