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Results for "

Anti-estrogen

" in MedChemExpress (MCE) Product Catalog:

40

Inhibitors & Agonists

2

Peptides

9

Natural
Products

3

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P3833A
    Yp537 TFA

    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-125263
    OP-1074

    		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-10830A
    PBPE hydrochloride

    		Estrogen Receptor/ERR Cancer
    PBPE hydrochloride is a derivative of tamoxifen (HY-13757A) and a selective ligand for the anti-estrogen binding site (AEBS), the binding affinities (Ki) of PBPE hydrochloride and MBPE to AEBS are 8.79 and 17.57 nM, respectively .
    PBPE hydrochloride
  • HY-125263B
    (R)-OP-1074

    		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-P3833
    Yp537

    Anti-estrogen

    		 Estrogen Receptor/ERR Endocrinology
    Yp537 is an estrogen receptor (ER) inhibitor that blocks dimerization of the human estrogen receptor .
    Yp537
  • HY-118242
    RU 45144

    		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-106056
    Zindoxifene

    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-117649
    RU-39411

    		Estrogen Receptor/ERR Cancer
    RU-39411 is a steroidal anti-estrogen with mixed estrogenic/antiestrogen activity. RU-39411 has shown inhibitory effects on cell growth in the MCF-7 breast cancer model, with the effect being correlated with its binding affinity to the estrogen receptor. RU-39411 was able to downregulate the estrogen binding capacity of cells, but did not reduce estrogen receptor mRNA levels, indicating that the grafting of its side chain prevents the antagonistic effects usually associated with steroidal estrogens. The administration of RU-39411 can promote the synthesis of progesterone receptors, further supporting its activity as an estrogen .
    RU-39411
  • HY-118633
    Ethamoxytriphetol

    MER-25

    		 Estrogen Receptor/ERR Endocrinology
    Ethamoxytriphetol (MER-25) is a nonsteroidal antiestrogen .
    Ethamoxytriphetol
  • HY-B0515B
    Ibandronate Sodium

    		Apoptosis Metabolic Disease Cancer
    Ibandronate Sodium is an orally active, selective inhibitor of farnesyl pyrophosphate synthase (FPP synthase). Ibandronate Sodium can block the mevalonate pathway to inhibit the isoprenylation modification of small GTPases (such as RAS, RHO family proteins), induce tumor cell apoptosis and inhibit bone resorption. Ibandronate Sodium inhibits tumor cell proliferation (such as ER+ breast cancer cells), promotes the expression of the pro-apoptotic gene FAS, and can produce synergistic anti-tumor effects with anti-estrogen compounds. Ibandronate Sodium is used in the study of osteoporosis and bone metastatic tumors (such as breast cancer bone metastasis) .
    Ibandronate Sodium
  • HY-114631
    EM-800

    		Estrogen Receptor/ERR Cancer
    EM-800, an orally active anti-estrogen, serves as an antagonist to the transcriptional functions of estrogen receptors α (ERα) and β (ERβ). EM-800 possesses anticancer activity, capable of inhibiting the growth of breast cancer induced by 7,12-Dimethylbenz[a]anthracene (DMBA) (HY-W011845). Furthermore, in ovariectomized animals, EM-800 effectively slows down bone loss. Additionally, EM-800 shows potential in the research of breast and endometrial cancers, while exerting beneficial effects on bone and lipid metabolism .
    EM-800
  • HY-B0515
    Ibandronate Sodium Monohydrate

    BM-210955; RPR-102289A

    		 Apoptosis Metabolic Disease Cancer
    Ibandronate Sodium Monohydrate (BM-210955; RPR-102289A) is an orally active, selective inhibitor of farnesyl pyrophosphate synthase (FPP synthase). Ibandronate Sodium Monohydrate can block the mevalonate pathway to inhibit the isoprenylation modification of small GTPases (such as RAS, RHO family proteins), induce tumor cell apoptosis and inhibit bone resorption. Ibandronate Sodium Monohydrate inhibits tumor cell proliferation (such as ER + breast cancer cells), promotes the expression of the pro-apoptotic gene FAS, and can produce synergistic anti-tumor effects with anti-estrogen compounds. Ibandronate Sodium Monohydrate is used in the study of osteoporosis and bone metastatic tumors (such as breast cancer bone metastasis) .
    Ibandronate Sodium Monohydrate
  • HY-145556
    Bexirestrant

    		Estrogen Receptor/ERR Cancer
    Bexirestrant is an orally active ER-α degrader. Bexirestrant can be used for the research of antiestrogen, antineoplastic .
    Bexirestrant
  • HY-117153
    GW7604

    		Estrogen Receptor/ERR Cancer
    GW7604 is an antiestrogen. GW7604 is the metabolite of GW5638, which is a high affinity estrogen receptor (ER) antagonist .
    GW7604
  • HY-B0515R
    Ibandronate Sodium Monohydrate (Standard)

    BM-210955 (Standard); RPR-102289A (Standard)

    		 Apoptosis Cancer
    Ibandronate Sodium Monohydrate (BM-210955; RPR-102289A) (Standard) is the analytical standard of Ibandronate Sodium Monohydrate (HY-B0515). This product is intended for research and analytical applications. Ibandronate Sodium Monohydrate (BM-210955; RPR-102289A) is an orally active, selective inhibitor of farnesyl pyrophosphate synthase (FPP synthase). Ibandronate Sodium Monohydrate can block the mevalonate pathway to inhibit the isoprenylation modification of small GTPases (such as RAS, RHO family proteins), induce tumor cell apoptosis and inhibit bone resorption. Ibandronate Sodium Monohydrate inhibits tumor cell proliferation (such as ER + breast cancer cells), promotes the expression of the pro-apoptotic gene FAS, and can produce synergistic anti-tumor effects with anti-estrogen compounds. Ibandronate Sodium Monohydrate is used in the study of osteoporosis and bone metastatic tumors (such as breast cancer bone metastasis) .
    Ibandronate Sodium Monohydrate (Standard)
  • HY-W926789
    (E)-GW7604

    		Estrogen Receptor/ERR Metabolic Disease Cancer
    (E)-GW7604 is the (E)-isomer of GW7604, an antiestrogen and a metabolite of GW5638 (HY-112746), which is a high-affinity estrogen receptor (ER) antagonist .
    (E)-GW7604
  • HY-W150752
    Triphenylethylene

    		Estrogen Receptor/ERR Calcium Channel Endocrinology
    Triphenylethylene is an aromatic hydrocarbon that possesses weak estrogenic activity. Triphenylethylene antiestrogens relax duodenal intestinal muscle via a mechanism that involves inhibition of L-type Ca 2+ channels but not activation of K + channels .
    Triphenylethylene
  • HY-18719A
    Endoxifen Z-isomer hydrochloride
    3 Publications Verification

    		 Estrogen Receptor/ERR Potassium Channel Cancer
    Endoxifen Z-isomer hydrochloride is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα).
    Endoxifen Z-isomer hydrochloride
  • HY-N3981
    Guajadial

    		Others Cancer
    Guajadial, a caryophyllene-based meroterpenoid, has anti-estrogenic and anticancer effect. Guajadial reverses multidrug resistance in cancer. Guajadial can be isolated from Psidium guajava leaves .
    Guajadial
  • HY-W087008
    7-Hydroxyflavanone

    		Cytochrome P450 Endocrinology Cancer
    7-Hydroxyflavanone is a potent inhibitor of aromatase (CYP19) activity with the IC50 of 65 μM. 7-Hydroxyflavanone exerts various biological effects, including anticarcinogenic, antioxidant and (anti-)estrogenic effects, and modula
    7-Hydroxyflavanone
  • HY-N1581
    Quassin

    Nigakilactone D

    		 Parasite Infection Endocrinology
    Quassin (Nigakilactone D) is a bioactive triterpenoid from stem bark extract of Quassia amara. Quassin inhibits P. falciparum with an IC50 of 0.15 μM. Quassin possesses reversible antifertility, anti-estrogenic and anti-plasmodial activity .
    Quassin
  • HY-N3316
    Martynoside

    		Others
    Martynoside protects ex vivo bone marrow cells from 5-fluorouracil (5-FU)-induced cell death and inflammation response by down-regulating the TNF signaling pathway .Martynoside is a potent antiestrogen in MCF-7 cells, increasing IGFBP3 levels
    Martynoside
  • HY-122411A
    (E/Z)-Panomifene hydrochloride

    (E/Z)-EGIS 5650 hydrochloride; (E/Z)-GYKI-13504 hydrochloride

    		 Estrogen Receptor/ERR Cancer
    (E/Z)-Panomifene (hydrochloride) is an orally active tamoxifen (TMX) (HY-13757A) analog. (E/Z)-Panomifene (hydrochloride) is a selective anti-estrogenic compound. (E/Z)-Panomifene (hydrochloride) has anti-tumor activity and can be used in breast cancer research .
    (E/Z)-Panomifene hydrochloride
  • HY-117038
    Anordiol

    		Estrogen Receptor/ERR Endocrinology
    Anordiol is an antiestrogenic compound with weak estrogenic activity. It can reduce the parameters of uterine growth (including uterine wet weight, soluble protein content, and DNA content) induced by estradiol in rats and can also regulate the estrous cycle in rats. Anordiol holds potential application value in the research of antiestrogen-related diseases .
    Anordiol
  • HY-13636
    Fulvestrant
    Maximum Cited Publications
    98 Publications Verification

    ICI 182780; ZD 9238; ZM 182780

    		 Estrogen Receptor/ERR Autophagy Apoptosis Cancer
    Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .
    Fulvestrant
  • HY-129099
    N-Desmethyltamoxifen

    		PKC Estrogen Receptor/ERR Drug Metabolite Endogenous Metabolite Cancer
    N-Desmethyltamoxifen is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation .
    N-Desmethyltamoxifen
  • HY-129099A
    N-Desmethyltamoxifen hydrochloride

    		PKC Estrogen Receptor/ERR Drug Metabolite Endogenous Metabolite Cancer
    N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation .
    N-Desmethyltamoxifen hydrochloride
  • HY-148789
    Palazestrant

    OP-1250

    		 Estrogen Receptor/ERR Inflammation/Immunology Cancer
    Palazestrant is an antiestrogen and antineoplastic agent. Palazestrant can completely inhibit the activity of 17b-estradiol (E2) with IC50 value of 6.4 nM, and inhibit the proliferation of MCF7 and CAMA-1 cells with IC50 value of 1.4-1.6 nM. Palazestrant can inhibit ER +/HER2 + cancer .
    Palazestrant
  • HY-18719
    Endoxifen (Z-isomer)
    3 Publications Verification

    		 Estrogen Receptor/ERR Potassium Channel Cancer
    Endoxifen Z-isomer is an oral active Tamoxifen (HY-13757A) metabolite, inducing an anti-estrogenic effect in breast cancer cells expressing ERα. Endoxifen Z-isomer inhibits hERG. This effect is concentration-dependent, with an IC50 value of 1.6 μM .
    Endoxifen (Z-isomer)
  • HY-13636S
    Fulvestrant-d3

    ICI 182780-d3; ZD 9238-d3; ZM 182780-d3

    		 Isotope-Labeled Compounds Estrogen Receptor/ERR Autophagy Apoptosis Cancer
    Fulvestrant-d3 is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .
    Fulvestrant-d3
  • HY-N1581R
    Quassin (Standard)

    		Parasite Infection Endocrinology
    Quassin (Standard) is the analytical standard of Quassin. This product is intended for research and analytical applications. Quassin (Nigakilactone D) is a bioactive triterpenoid from stem bark extract of Quassia amara. Quassin inhibits P. falciparum with an IC50 of 0.15 μM. Quassin possesses reversible antifertility, anti-estrogenic and anti-plasmodial activity .
    Quassin (Standard)
  • HY-W106688
    Triisopropyl phosphate

    		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-135671
    AhR modulator-1

    		Aryl Hydrocarbon Receptor VEGFR Estrogen Receptor/ERR Endocrinology Cancer
    AhR modulator-1 (compound 6-MCDF) is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. AhR modulator-1 inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. AhR modulator-1 also possess anti-estrogenic properties in rat uterus .
    AhR modulator-1
  • HY-16023B
    (Rac)-Acolbifene

    EM-343; (Rac)-EM-652

    		 Estrogen Receptor/ERR Cancer
    (Rac)-Acolbifene (EM-343; (Rac)-EM-652) is the racemic form of EM652 (estrogen receptor?antagonist), has anti-estrogenic and estrogenic activities. (Rac)-Acolbifene (EM-343; (Rac)-EM-652) contains a piperidine ring, shows good pharmacological profile,relative binding affinity (RBA)=380 .
    (Rac)-Acolbifene
  • HY-129099AR
    N-Desmethyltamoxifen hydrochloride (Standard)

    		PKC Estrogen Receptor/ERR Drug Metabolite Endogenous Metabolite Cancer
    N-Desmethyltamoxifen (hydrochloride) (Standard) is the analytical standard of N-Desmethyltamoxifen (hydrochloride). This product is intended for research and analytical applications. N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation[1][2][3].
    N-Desmethyltamoxifen hydrochloride (Standard)
  • HY-16023A
    Acolbifene
    2 Publications Verification

    EM-652; SCH 57068

    		 Estrogen Receptor/ERR Cancer
    Acolbifene (EM-652), the active metabolite of EM800, is an orally active pure antiestrogen and selective estrogen receptor antagonist. Acolbifene (EM-652) inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM). Acolbifene (EM-652) possesses potent and pure anticarcinogenic properties .
    Acolbifene
  • 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-W774926
    Permethrin-d6

    NRDC-143-d6

    		 Isotope-Labeled Compounds Na+/K+ ATPase Parasite Sodium Channel Mitochondrial Metabolism Infection Neurological Disease
    Permethrin-d6 (NRDC-143-d6) is deuterium labeled Permethrin. 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-d6
  • HY-B1234
    Octinoxate

    Octyl methoxycinnamate

    		 Androgen Receptor Estrogen Receptor/ERR Thyroid Hormone Receptor Cytochrome P450 Metabolic Disease Endocrinology
    Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo .
    Octinoxate
  • HY-B1234S
    Octinoxate-13C,d3

    		Cytochrome P450 Thyroid Hormone Receptor Androgen Receptor Estrogen Receptor/ERR Isotope-Labeled Compounds Metabolic Disease Endocrinology
    Octinoxate-13C,d3 is the deuterium labeled Octinoxate (HY-W245806). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo .
    Octinoxate-13C,d3

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