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Estrogen Inhibitors

" in MedChemExpress (MCE) Product Catalog:

187

Inhibitors & Agonists

1

Biochemical Assay Reagents

6

Peptides

39

Natural
Products

29

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P3833A

    Anti-Estrogen TFA

    Estrogen Receptor/ERR Endocrinology
    Yp537 TFA is an estrogen receptor (ER) inhibitor that blocks dimerization of the human estrogen receptor .
    Yp537 TFA
  • HY-150601
    Estrogen receptor-IN-1
    1 Publications Verification

    Estrogen Receptor/ERR Metabolic Disease
    Estrogen receptor-IN-1 (compound 16) is a potent estrogen receptor (ER) inhibitor with IC50s of 13, 5µM for ERα and Erβ, respectively .
    Estrogen receptor-IN-1
  • HY-B2158

    Estrogen Receptor/ERR COX Cardiovascular Disease Endocrinology
    Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood .
    Chlorotrianisene
  • HY-N9329

    Monoamine Oxidase Estrogen Receptor/ERR Metabolic Disease
    Glicoricone, a phenolic compound, is isolated from a species of licorice. Glicoricone is an inhibitor of monoamine oxidase (MAO), with an IC50 of 140 μM. Glicoricone binds to estrogen receptor (ER) and shows estrogen antagonist activity .
    Glicoricone
  • HY-106056

    D 16726

    Estrogen Receptor/ERR Cancer
    Zindoxifene is a partial anti-estrogen. Zindoxifene works primarily by binding to estrogen receptors, thereby inhibiting the growth of estrogen-dependent tumor cells. Zindoxifene is able to exhibit the dual properties of estrogen agonists and antagonists and can be used in research and development to target estrogen-dependent tumors, such as prostate and breast cancer .
    Zindoxifene
  • HY-P3833

    Anti-Estrogen

    Estrogen Receptor/ERR Endocrinology
    Yp537 is an estrogen receptor (ER) inhibitor that blocks dimerization of the human estrogen receptor .
    Yp537
  • HY-153700

    Estrogen Receptor/ERR Endocrinology
    Estrogen receptor modulator 8 (compound 4) is an orally active inhibitor of Estrogen Receptor/ERR α (IC50=0.437 nM, MCF-7 cells). Estrogen receptor modulator 8 inhibits MCF-7 cells proliferation with an IC50 value of 0.1 nM .
    Estrogen receptor modulator 8
  • HY-118242

    Estrogen Receptor/ERR Calmodulin Others
    RU 45144 is an anti-estrogen compound that has the activity of antagonizing the binding of estrogen receptors to calmodulin. RU 45144 can inhibit the binding of estrogen receptors to calmodulin, and its effect is similar to that of tamoxifen. Its anti-estrogen effect may be related to specific side chains in the molecular structure, and the steroid skeleton may be involved in its anti-proliferative activity.
    RU 45144
  • HY-171477

    Estrogen Receptor/ERR Cancer
    Metahexestrol is an estrogen receptor (E2R) inhibitor with antitumor activity. It significantly inhibits the proliferation of estrogen receptor-positive MCF-7 human breast cancer cells (ED50 = 1.0 μM). Additionally, Metahexestrol also exhibits inhibitory effects in estrogen receptor-negative MDA-MB-231 cells, and its antiproliferative activity cannot be reversed by estrogen, suggesting that its mechanism of action may be partially independent of the E2R pathway. Metahexestrol can be used in research on estrogen-dependent breast cancer .
    Metahexestrol
  • HY-111484A

    SRN-927 Racemate

    Estrogen Receptor/ERR Cancer
    GDC-0927 Racemate (SRN-927 Racemate) is an estrogen receptor (ER) degrader that can effectively inhibit the activity of ER-α with an IC50 value of 0.2 nM and can be used in diseases related to estrogen receptors.
    GDC-0927 Racemate
  • HY-103450

    Estrogen Receptor/ERR Endocrinology Cancer
    G-36 is a cell-permeable nonsteroidal antagonist of the G protein-coupled estrogen receptor (GPER/GPR30), which selectively inhibits estrogen-mediated PI3K activation through GPER, rather than Erα. G-36 also inhibits estrogen-mediated calcium mobilization (IC50=112 nM). G-36 is promising for research in the field of cancer .
    G36
  • HY-B0723
    Ospemifene
    2 Publications Verification

    FC-1271a

    Estrogen Receptor/ERR Caspase Neurological Disease Endocrinology Cancer
    Ospemifene (FC-1271a) is an orally active and non-estrogenic selective estrogen receptor modulator (SERM) with Ki values of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene inhibits caspase-3 activity. Ospemifene inhibits neuronal degeneration, prevents bone loss, and increases vaginal weight and vaginal epithelial height. Ospemifene has anticancer activity against breast cancer .
    Ospemifene
  • HY-B2158S

    Isotope-Labeled Compounds Estrogen Receptor/ERR COX Cardiovascular Disease Endocrinology
    Chlorotrianisene-d9 is the deuterium labeled Chlorotrianisene. Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood .
    Chlorotrianisene-d9
  • HY-14247B

    CGS 16949A hemihydrate; (Rac)-FAD286 hydrochloride hemihydrate

    Cytochrome P450 Endocrinology Cancer
    Fadrozole hydrochloride hemihydrate is an orally active, potent, selective and nonsteroidal aromatase inhibitor, with an IC50 of 6.4 nM. Fadrozole hydrochloride hemihydrate inhibits the production of estrogen and progesterone, with IC50 values of 0.03 and 120 μM. Fadrozole hydrochloride hemihydrate shows prevention of spontaneous tumours. Fadrozole hydrochloride hemihydrate can be used for the research of estrogen-dependent disease and cancer .
    Fadrozole hydrochloride hemihydrate
  • HY-W106688

    Estrogen Receptor/ERR Endocrinology
    Triisopropyl phosphate inhibits TFF1 and EGR3 gene expression, exhibits anti-estrogenic activity that inhibits Estradiol (HY-B0141)-induced MCF-7 cell proliferation with an EC50 of 341 μM. Triisopropyl phosphate inhibits the estrogen response element (ERE)-stimulated luciferase activity in MVLN cells with an EC50 of 900 μM .
    Triisopropyl phosphate
  • HY-B2158R

    Reference Standards Estrogen Receptor/ERR COX Cardiovascular Disease Endocrinology
    Chlorotrianisene (Standard) is the analytical standard of Chlorotrianisene. This product is intended for research and analytical applications. Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood .
    Chlorotrianisene (Standard)
  • HY-169063

    Estrogen Receptor/ERR Cancer
    ZINC05925939 is an estrogen receptor beta (ESR2) inhibitor that can be used in breast cancer research .
    ZINC05925939
  • HY-131404
    TPBM
    1 Publications Verification

    Estrogen Receptor/ERR Cancer
    TPBM is a potent estrogen receptor α (ERα) inhibitor with an IC50 value of 9 μM for 17β-estradiol (E2)-ERα. TPBM reduces E2·ERα recruitment to an endogenous estrogen-responsive gene. TPBM inhibits E2-dependent growth of ERα-positive cancer cells (IC50=5 μM). TPBM is not toxic to cells and does not affect estrogen-independent cell growth .
    TPBM
  • HY-146424

    Estrogen Receptor/ERR Neurological Disease Cancer
    OBHS is an estrogen receptor α (ERα) inhibitor. OBHS can also be used as a blowing agent .
    OBHS
  • HY-135581

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
    Raloxifene 6-glucuronide
  • HY-135582

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
    Raloxifene 4'-glucuronide
  • HY-W010062

    Drug Derivative Cytochrome P450 Estrogen Receptor/ERR Metabolic Disease Cancer
    4-Chlorophenylacetic acid is a halogenated phenylacetic acid derivative. 4-Chlorophenylacetic acid is a potent aromatase inhibitor and antagonizes estrogen signaling. 4-Chlorophenylacetic acid can provide carbon and energy for Pseudomonas sp. strain CBS3. 4-Chlorophenylacetic acid is effective against estrogen-induced mammary tumorigenesis .
    4-Chlorophenylacetic acid
  • HY-B0141A

    Alfatradiol; Epiestradiol; Epiestrol

    5 alpha Reductase Endogenous Metabolite Bacterial Inflammation/Immunology
    Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.
    Alpha-Estradiol
  • HY-125263

    Estrogen Receptor/ERR Cancer
    OP-1074, a pure anti-estrogen drug, is a selective ER degrader (PA-SERD) with specific anti-estrogenic activity against ERα and ERβ, inhibiting 17β-estradiol (E2)-stimulated transcription with IC50 values of 1.6 and 3.2 nM, respectively.
    OP-1074
  • HY-B1100
    Estradiol cypionate
    5+ Cited Publications

    Estrogen Receptor/ERR Apoptosis Endocrinology Cancer
    Estradiol cypionate is the 17β-cypionate ester of Estradiol, which inhibits ET-1 synthesis by acting on estrogen receptors .
    Estradiol cypionate
  • HY-123247

    Cytochrome P450 Endocrinology
    LY113174 is an orally active aromatase inhibitor (IC50 = 24 nM). LY113174 blocks testosterone induced increase in uterine weight in rat, and inhibits ovarian estrogen biosynthesis .
    LY113174
  • HY-173279

    Cytochrome P450 Endocrinology
    CYP19A1-IN-1 (Compound 9) is a CYP19A1 inhibitor with an IC50 of 271 nM. CYP19A1-IN-1 inhibits the activity of converting androgens to estrogens by binding to CYP19A1. CYP19A1-IN-1 can be used in the research of sex hormone-related diseases such as estrogen-dependent breast cancer .
    CYP19A1-IN-1
  • HY-N3943

    Tyrosinase Neurological Disease
    Glabrene, an isoflavene derived from licorice root, shows estrogen-like activity. Glabrene is a tyrosinase inhibitor with an IC50 of 3.5 μM .
    Glabrene
  • HY-126109

    Estrogen Receptor/ERR Apoptosis Metabolic Disease Endocrinology Cancer
    (±)-8-Prenylnaringenin, a natural prenylated flavonoid, is a potent phytoestrogen. (±)-8-Prenylnaringenin is an orally active selective estrogen receptor modulator (SERM) (Estrogen Receptor/ERR) that inhibits ERα and ERβ with IC50s of 57 nM and 68 nM, respectively. (±)-8-Prenylnaringenin has anticancer effects, and can be used for osteoporosis research .
    (±)-8-Prenylnaringenin
  • HY-124403

    Estrogen Receptor/ERR Cancer
    D 15413 is an orally active antagonist for nonsteroidal estrogen. D 15413 inhibits growth of estrogen receptor positive MCF-7 cell with an inhibition rate of 70% at 10 -7 M. D 15413 exhibits antitumor efficacy against DMBA (HY-W011845) or MNU (HY-34758)-induced breast cancer .
    D 15413
  • HY-135581S1

    Isotope-Labeled Compounds Estrogen Receptor/ERR Endocrinology
    Raloxifene 6-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
    Raloxifene 6-glucuronide-d4 lithium
  • HY-135582S1

    Isotope-Labeled Compounds Estrogen Receptor/ERR Endocrinology
    Raloxifene 4'-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 4'-glucuronide. Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
    Raloxifene 4'-glucuronide-d4 lithium
  • HY-129433

    17β-HSD Endocrinology
    17β-HSD1-IN-2 (PBRM) is a non-estrogenic and steroidal covalent irreversible inhibitor of 17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) (Ki=368 nM). 17β-HSD1-IN-2 can be used for the research of estrogen-dependent disorders .
    17β-HSD1-IN-2
  • HY-137391

    Estrogen Receptor/ERR Metabolic Disease
    2-Bromoestradiol is a estrogen 2-hydroxylase inhibitor. 2-Bromoestradiol decreases irreversible binding of radiolabeled estradiol metabolite(s) to microsomal proteins .
    2-Bromoestradiol
  • HY-135582S

    Estrogen Receptor/ERR Isotope-Labeled Compounds Endocrinology
    Raloxifene 4'-glucuronide-d4 is deuterated labeled Raloxifene 4'-glucuronide (HY-135582). Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
    Raloxifene 4'-glucuronide-d4
  • HY-13757A
    Tamoxifen
    Maximum Cited Publications
    139 Publications Verification

    ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen

    Estrogen Receptor/ERR HSP Autophagy Apoptosis Endocrinology Cancer
    Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which 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. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER transgenic mouse .
    Tamoxifen
  • HY-B0887
    Permethrin
    1 Publications Verification

    NRDC-143

    Parasite Mitochondrial Metabolism Sodium Channel Na+/K+ ATPase Infection Neurological Disease
    Permethrin (NRDC-143) is an insecticide, acaricide and a high selectively inhibitor of the Mitochondrial complex I, found in sediment and water samples. Permethrin shows estrogenic in vivo and anti-estrogenic activity in vitro. Permethrin also acts as a neurotoxin affecting neuron membranes by prolonging Sodium channel activation. Permethrin decreases resistance to bacterial infections in medaka (Oryzias latipes) .
    Permethrin
  • HY-19822S3

    RAD1901-d6

    Isotope-Labeled Compounds Estrogen Receptor/ERR Cancer
    Elacestrant-d6 (RAD1901-d6) is a deuterated labeled Elacestrant (HY-19822). Elacestrant is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
    Elacestrant-d6
  • HY-121149B

    (E/Z)-3-Hydroxytamoxifen

    Estrogen Receptor/ERR Apoptosis Cancer
    (E/Z)-Droloxifene is a mixture of (E)-droloxifene (a selective estrogen receptor modulator) and (Z)-droloxifene. (E)-Droloxifene binds to the estrogen receptor (ER) with an IC50 value of 24 nM in rabbit uterine homogenates. (E)-Droloxifene increases uterine weight in immature rats, and reduces estradiol-induced increases in uterine weight in juvenile rats. (E)-Droloxifene also inhibits 17β-estradiol-stimulated growth of MCF-7, ZR-75-1, and T47D human breast cancer cells. (Z)-Droloxifene binds weakly to ER and has no estrogenic or antiestrogenic activity .
    (E/Z)-Droloxifene
  • HY-18719B
    Endoxifen hydrochloride
    1 Publications Verification

    Cytochrome P450 Estrogen Receptor/ERR Drug Metabolite Parasite Cancer
    Endoxifen hydrochloride is a key active metabolite of Tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen hydrochloride has the potential for breast cancer study .
    Endoxifen hydrochloride
  • HY-18719E
    Endoxifen
    1 Publications Verification

    Cytochrome P450 Estrogen Receptor/ERR Drug Metabolite Parasite Cancer
    Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen has the potential for breast cancer study .
    Endoxifen
  • HY-163712

    Estrogen Receptor/ERR Endocrinology
    17-Epiestriol is an estrogen metabolite and a selective estrogen receptor (ER) β agonist. 17-epiestriol inhibits the mRNA and protein expression of the vascular cell adhesion molecule VCAM-1 induced by tumor necrosis factor α (TNFα). 17-epiestriol also inhibits TNFα-induced VCAM-1 expression and prevents NF-κB migration to the nucleus. 17-Epiestriol also induces the mRNA and protein expression of endothelial nitric oxide synthase .
    17-Epiestriol
  • HY-14248
    Letrozole
    15+ Cited Publications

    CGS 20267

    Cytochrome P450 Autophagy Cancer
    Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer .
    Letrozole
  • HY-W010062R

    Reference Standards Cytochrome P450 Estrogen Receptor/ERR Drug Derivative Metabolic Disease Cancer
    4-Chlorophenylacetic acid (Standard) is the analytical standard of 4-Chlorophenylacetic acid. This product is intended for research and analytical applications. 4-Chlorophenylacetic acid is a halogenated phenylacetic acid derivative. 4-Chlorophenylacetic acid is a potent aromatase inhibitor and antagonizes estrogen signaling. 4-Chlorophenylacetic acid can provide carbon and energy for Pseudomonas sp. strain CBS3. 4-Chlorophenylacetic acid is effective against estrogen-induced mammary tumorigenesis .
    4-Chlorophenylacetic acid (Standard)
  • HY-19822S

    RAD1901-d4

    Isotope-Labeled Compounds Estrogen Receptor/ERR Cancer
    Elacestrant-d4 (RAD1901-d4) is a deuterated labeled Elacestrant (HY-19822). Elacestrant (RAD1901) is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
    Elacestrant-d4
  • HY-117726

    Estrogen Receptor/ERR NF-κB Inflammation/Immunology
    WAY-169916 is a pathway-selective ligand of ER (estrogen receptor) that acts by inhibiting NF-kB transcriptional activity. WAY-169916 has potent anti-inflammatory effect .
    WAY-169916
  • HY-13757
    Tamoxifen Citrate
    Maximum Cited Publications
    139 Publications Verification

    ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate

    Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis . Tamoxifen Citrate also can induce gene knockout of CreER transgenic mouse .
    Tamoxifen Citrate
  • HY-125263B

    Estrogen Receptor/ERR Cancer
    (R)-OP-1074 is an isomer of OP-1074 (HY-125263) and can serve as a control compound in experiments. OP-1074, a pure anti-estrogen drug, is a selective ER degrader (PA-SERD) with specific anti-estrogenic activity against ERα and ERβ, inhibiting 17β-estradiol (E2)-stimulated transcription with IC50 values of 1.6 and 3.2 nM, respectively.
    (R)-OP-1074
  • HY-137449

    G1T48

    Estrogen Receptor/ERR CDK Cancer
    Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a CDK4/6 inhibitor .
    Rintodestrant
  • HY-168644

    Estrogen Receptor/ERR Endocrinology
    Erα-IN-1 (compound 3c) is an inhibitor of estrogen receptor α (ERα), blocking ERa activity in MCF7/ERE-LUC cells. .
    Erα-IN-1

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