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Results for "

ERα antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (2) Apoptosis (4) Endogenous Metabolite (3) Estrogen Receptor/ERR (31) Glucocorticoid Receptor (1) IAP (3) Isotope-Labeled Compounds (1) Ligands for E3 Ligase (1) Melatonin Receptor (1) mTOR (1) NF-κB (1) NO Synthase (2) NOD-like Receptor (NLR) (1) PROTACs (2) Reference Standards (2) TNF Receptor (1)
By Research Areas:	Cancer (29) Cardiovascular Disease (3) Endocrinology (3) Infection (1) Inflammation/Immunology (2) Metabolic Disease (5) Neurological Disease (1)
Click Chemistry:	Tetrazine (1)

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Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	상품명	Target	연구분야	Chemical Structure

HY-103456

PHTPP Maximum Cited Publications 30 Publications Verification	Estrogen Receptor/ERR	Cancer
PHTPP is a selective estrogen receptor β (ERβ) antagonist with 36-fold selectivity over ERα .

HY-12870

AZD9496 25+ Cited Publications	Estrogen Receptor/ERR	Cancer
AZD9496 is an effective, selective estrogen receptor (ERα) antagonist with an IC₅₀ of 0.28 nM. AZD9496 is an orally active, selective estrogen receptor degrader (SERD).

HY-B0412

Estriol 5 Publications Verification Oestriol	Estrogen Receptor/ERR Endogenous Metabolite	Cancer
Estriol (Oestriol), an orally active estrogen, is a *ERα* and ERβ agonist. Estriol is a potent GPR30 antagonist in estrogen receptor-negative breast cancer cells. Estriol can ameliorate disease severity through immunomodulatory mechanisms that decrease tissue inflammation. Estriol has powerful proconvulsant effects .

HY-103450

G36	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 .

HY-15731

Estetrol	Estrogen Receptor/ERR Endogenous Metabolite NO Synthase	Cardiovascular Disease Cancer
Estetrol, an orally active estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol binds ERα as well as ERβ (with a fourfold lower affinity). Estetrol increases eNOS expression/activity and NO synthesis in endothelial cells. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast. Estetrol can be used in contraception and menopausal hormone research .

HY-112611

H3B-5942	Estrogen Receptor/ERR	Cancer
H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant *ERα* by targeting Cys530, with K_is of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERα ^WT or ERα mutations .

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 .

HY-103457

Y134	Estrogen Receptor/ERR	Cancer
Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at *ERα* and ERβ. Y134 shows 121.1-fold selectivity for ERα (K_i=0.09 nM) over ERβ (K_i=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells .

HY-125703

Ferutinin	Estrogen Receptor/ERR Apoptosis	Infection Inflammation/Immunology Endocrinology Cancer
Ferutinin, a natural terpenoid compound, is an estrogen receptor ERα agonist and estrogen ERβ-receptor agonist/antagonist with IC₅₀s of 33.1 nM and 180.5 nM, respectively. Ferutinin acts as an electrogenic Ca ²⁺-ionophore that increases calcium permeability of lipid bilayer membranes, mitochondria. Ferutinin possesses estrogenic, antitumor, antibacterial and antiinflammatory activities .

HY-145341

GNE-149	Estrogen Receptor/ERR	Cancer
GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC₅₀=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer .

HY-150693

*Estrogen receptor β antagonist* 2**	Estrogen Receptor/ERR	Cancer
Estrogen receptor β antagonist 2 is a potent and selective estrogen receptor β (ERβ) antagonist with IC₅₀s of 109.10, 0.63 µM for Erα and Erβ, respectively .

HY-12870A

AZD9496 maleate 25+ Cited Publications	Estrogen Receptor/ERR	Cancer
AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC₅₀ of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD).

HY-144733

ERα antagonist 1	Estrogen Receptor/ERR Apoptosis	Cancer
ERα antagonist 1 (Compound 19d) is a potent, selective, covalent estrogen receptor α (ERα) antagonist. ERα antagonist 1 induces apoptosis and cell cycle G0/G1 phase arrest in MCF-7 cells .

HY-W114419

Bisphenol C	Estrogen Receptor/ERR mTOR	Cardiovascular Disease Metabolic Disease
Bisphenol C is an estrogen receptor-α (ERα) agonist and an ERβ antagonist, with IC₅₀ values of 2.65 nM for ERα and 1.94 nM for ERβ. Bisphenol C is a material of manufacturing polyester polymers like polycarbonate, is widely used in daily items like water bottles, food packaging, textile and so on .

HY-175448

GNE-1567	PROTACs Estrogen Receptor/ERR IAP	Cancer
GNE-1567 is a potent ERα PROTAC degrader and a selective XIAP antagonist with a K_d value of 0.03 μM. GNE-1567 is indicated for breast cancer research. (Pink: ligand for target protein (HY-18719); Black: linker; Blue: ligand for E3 ligase (HY-175449)) .

HY-179232

ERα antagonist 2	Estrogen Receptor/ERR	Cancer
ERα antagonist 2 (Compound 5b) is an *ER-α* antagonist with an IC₅₀ value of 1729 nM. ERα antagonist 2 exhibits significant inhibitory activity against breast cancer cell lines, and is still effective against ER-negative cells (MDA-MB-231), suggesting the existence of ER-independent pathways. ERα antagonist 2 can be used for the study of breast cancer .

HY-169941

ERα/ERβ antagonist-1	Estrogen Receptor/ERR	Metabolic Disease Cancer
ERα/ERβ antagonist-1 (Compound 10) is partial antagonists of *ERα* and ERβ. ERα/ERβ antagonist-1 reduces *ERα* and ERβ activity in a dose-dependent manner in HepG2 liver cells .

HY-175348

XB2M54	Ligands for E3 Ligase IAP NOD-like Receptor (NLR)	Others Inflammation/Immunology Cancer
XB2M54 is a selective XIAP antagonist. XB2M54 inhibits NOD2-mediated inflammatory signaling. XB2M54 is an E3 ligase ligand. XB2M54 can be used for synthesis of PROTAC ERα Degrader-1 (HY-112098) .

HY-125627

CP-394531	Glucocorticoid Receptor Androgen Receptor	Neurological Disease Metabolic Disease
CP-394531 is an efficient and highly selective non-steroidal glucocorticoid receptor (GR) antagonist, with a K_i value of 0.1 nM. CP-394531 has a weak binding to androgen receptor (AR) (K_i = 130 nM), and has almost no effect on progesterone receptor (PR) and estrogen receptors (ERα, ERβ). CP-394531 completely blocks the half-maximal agonistic effect induced by Dexamethasone (HY-14648G), with a K_if of 4.1 nM. CP-394531 can be used to study various diseases such as diabetes, obesity, depression, neurodegenerative diseases, glaucoma and Cushing's disease .

HY-176955

ER degrader 12	Estrogen Receptor/ERR	Cancer
ER degrader 12 (Example 1) is an estrogen receptor (ER) degrader with IC₅₀ values for ERα and ERβ of 2.3 and 80.2 nM respectively (TR-FRET experiment). ER degrader 12 inhibits the proliferation of MCF-7 cells, with an IC₅₀ of 1.53 nM. ER degrader 12 can be used for research on breast cancer .

HY-103451

(R,R)-THC	Estrogen Receptor/ERR	Metabolic Disease
(R,R)-THC is an ERα agonist and an ERβ antagonist, with K_is of 9.0 nM and 3.6 nM for ERα and ERβ, respectively. (R,R)-THC has higher relative binding affinity for ERβ than ERα with the values of 25 and 3.6 .

HY-103451A

rel-(R,R)-THC	Estrogen Receptor/ERR	Metabolic Disease
rel-(R,R)-THC is the relative configuration of (R,R)-THC (HY-103451). (R,R)-THC is an *ERα* agonist and an ERβ antagonist, with K_is of 9.0 nM and 3.6 nM for *ERα* and ERβ, respectively. (R,R)-THC has higher relative binding affinity for ERβ than *ERα* with the values of 25 and 3.6 .

HY-103456R

PHTPP (Standard)	Reference Standards Estrogen Receptor/ERR	Cancer
PHTPP (Standard) is the analytical standard of PHTPP. This product is intended for research and analytical applications. PHTPP is a selective estrogen receptor β (ERβ) antagonist with 36-fold selectivity over ERα .

HY-144137

*Estrogen receptor antagonist* 1**	Estrogen Receptor/ERR	Cancer
Estrogen receptor antagonist 1 is a selective estrogen receptor antagonist. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. Estrogen receptor antagonist 1 has the potential for the research of breast cancer diseases (extracted from patent WO2021249533A1, compound 4) .

HY-170382

*ER covalent antagonist-1*	Estrogen Receptor/ERR Apoptosis	Cancer
ER covalent antagonist-1 (Compound 39D) is the antagonist for estrogen receptor α (ERα). ER covalent antagonist-1 inhibits the proliferation of ERα-positive cell MCF-7 with an IC₅₀ of 0.98 μM, arrests the cell cycle at G0/G1 phase, and induces apoptosis. ER covalent antagonist-1 exhibits antitumor efficacy in mouse model .

HY-144138

*Estrogen receptor antagonist* 2**	Estrogen Receptor/ERR	Cancer
Estrogen receptor antagonist 2 is a selective estrogen receptor downregulator. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. Estrogen receptor antagonist 2 has the potential for the research of breast cancer diseases (extracted from patent WO2021228210A1, compound 3) .

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 .

HY-15731S1

Estetrol-d4 (Major)	Isotope-Labeled Compounds NO Synthase Endogenous Metabolite Estrogen Receptor/ERR	Cardiovascular Disease
Estetrol-d₄ (Major) is the deuterium labeled Estetrol (HY-15731). Estetrol, an orally active estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol binds ERα as well as ERβ (with a fourfold lower affinity). Estetrol increases eNOS expression/activity and NO synthesis in endothelial cells. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast. Estetrol can be used in contraception and menopausal hormone research .

HY-169382

Melatonin-Tamoxifen Conjugate	Melatonin Receptor	Cancer
Melatonin-Tamoxifen Conjugate (compound 16c) is an anticancer drug conjugate composed of Melatonin (HY-B0075) and Tamoxifen (HY-13757A), which is a potent antagonist of *ERα* (IC₅₀=863 nM). Melatonin-Tamoxifen Conjugate binds to MLT receptor (K_i=3.1 nM) and promotes β-arrestin (EC₅₀=914 nM) and ERK activation (EC₅₀=98 nM) in cells expressing hMT1 receptor. Melatonin-Tamoxifen Conjugate against several common cell lines MCF-7, MDA-MB-231, and HT-1080 with IC₅₀s of 6.8 μM, 6.4 μM, and 1.7 μM, respectively.

HY-181345

OP-1690	Estrogen Receptor/ERR	Cancer
OP-1690 is a complete estrogen receptor (ERα) antagonist (CERAN), with pIC₅₀ values of 7.5 and 7.9 in alkaline phosphatase (AP) activity assay and TR-FRET assay, respectively. OP-1690 modulates receptor function by inducing ERα tetramerization, effectively induces ERα degradation, inhibits target gene transcription, but exhibits low antiproliferative potency. OP-1690 can be used for breast cancer research .

HY-175445

GNE-5472	PROTACs Estrogen Receptor/ERR IAP NF-κB TNF Receptor Apoptosis	Cancer
GNE-5472 is a potent bifunctional ERα PRRTAC degrader, with its E3 ligand being a pan-IAP antagonist. GNE-5472 antagonizes cIAP1/2, activating the non-classical NF-κB pathway, resulting in a significant upregulation of TNFα expression. GNE-5472 inhibits the proliferation of breast cancer cells and induces cell apoptosis. GNE-5472 can be used for the study of breast cancer .

HY-124627

THIQ 40	Estrogen Receptor/ERR	Cancer
THIQ-40 is a tetrahydroisoquinoline-based, orally active, and selective estrogen receptor *ERα* degrader (SERD) (IC₅₀=17 nM), with antitumor efficacy. THIQ-40 possesses functional ERα antagonistic activity, promotes ERα degradation and forms stable ERαLBD complexes. THIQ-40 shows the characteristic of rapid racemization in multi-species plasma. THIQ-40 can be widely applied to studies on the relevant mechanisms and drug development of ERα-positive breast cancer .

HY-164726

Estrogen receptor modulator 11	Estrogen Receptor/ERR	Others
Estrogen receptor modulator 11 (Compound 27) is a tetrahydroisoquinoline derivative. Estrogen receptor modulator 11 has a certain affinity for estrogen receptors (ER), with IC₅₀ values of 285 nM and 421 nM for *ERα* and ERβ, respectively. Estrogen receptor modulator 11 lacks antagonist activity in the MCF-7 cellular assay .

HY-180409

YM580	Androgen Receptor	Cancer
YM580 is a potent, orally active and selective Androgen Receptor (AR) antagonist (IC₅₀ = 0.11 μM, hAR Ki = 4.6 nM, rAR Ki = 6.2 nM). YM580 exhibits good selectivity over PR, GR, and *ERα* (K_is > 3300 nM). YM580 decreases ventral prostate weight in mature intact rats dose-dependently without affecting serum testosterone levels. YM580 can be used for the research of prostate cancer .

HY-103450R

G36 (Standard)	Reference Standards Estrogen Receptor/ERR	Endocrinology Cancer
G36 (Standard) is the analytical standard of G36 (HY-103450). This product is intended for research and analytical applications. 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 .

Cat. No.	상품명	Category	Target	Chemical Structure

HY-B0412

Estriol 5 Publications Verification Oestriol	Monophenols Immune System Disorder Classification of Application Fields Disease markers Phenols Endocrine diseases Endogenous metabolite Disease Research Fields Steroids Cancer Source Classification	Estrogen Receptor/ERR Endogenous Metabolite
Estriol (Oestriol), an orally active estrogen, is a *ERα* and ERβ agonist. Estriol is a potent GPR30 antagonist in estrogen receptor-negative breast cancer cells. Estriol can ameliorate disease severity through immunomodulatory mechanisms that decrease tissue inflammation. Estriol has powerful proconvulsant effects .

HY-15731

Estetrol	Cardiovascular Disease Monophenols Classification of Application Fields Phenols Endogenous metabolite Disease Research Fields Steroids Source Classification	Estrogen Receptor/ERR Endogenous Metabolite NO Synthase
Estetrol, an orally active estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol binds ERα as well as ERβ (with a fourfold lower affinity). Estetrol increases eNOS expression/activity and NO synthesis in endothelial cells. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast. Estetrol can be used in contraception and menopausal hormone research .

HY-125703

Ferutinin	Viguiera dentata (Cav.) Spreng. Infection Classification of Application Fields Terpenoids Sesquiterpenes Umbelliferae Plants Disease Research Fields Endocrinology Source Classification Cancer	Estrogen Receptor/ERR Apoptosis
Ferutinin, a natural terpenoid compound, is an estrogen receptor ERα agonist and estrogen ERβ-receptor agonist/antagonist with IC₅₀s of 33.1 nM and 180.5 nM, respectively. Ferutinin acts as an electrogenic Ca ²⁺-ionophore that increases calcium permeability of lipid bilayer membranes, mitochondria. Ferutinin possesses estrogenic, antitumor, antibacterial and antiinflammatory activities .

Cat. No.	상품명	Chemical Structure

HY-15731S1

Estetrol-d4 (Major)
Estetrol-d₄ (Major) is the deuterium labeled Estetrol (HY-15731). Estetrol, an orally active estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol binds ERα as well as ERβ (with a fourfold lower affinity). Estetrol increases eNOS expression/activity and NO synthesis in endothelial cells. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast. Estetrol can be used in contraception and menopausal hormone research .

Estetrol-d4 (Major)

Estetrol-d₄ (Major) is the deuterium labeled Estetrol (HY-15731). Estetrol, an orally active estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol binds ERα as well as ERβ (with a fourfold lower affinity). Estetrol increases eNOS expression/activity and NO synthesis in endothelial cells. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast. Estetrol can be used in contraception and menopausal hormone research .

Cat. No.	상품명		Classification

HY-179232

ERα antagonist 2		Tetrazine
ERα antagonist 2 (Compound 5b) is an *ER-α* antagonist with an IC₅₀ value of 1729 nM. ERα antagonist 2 exhibits significant inhibitory activity against breast cancer cell lines, and is still effective against ER-negative cells (MDA-MB-231), suggesting the existence of ER-independent pathways. ERα antagonist 2 can be used for the study of breast cancer .

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ERα antagonist

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Isotope-Labeled Compounds

Click Chemistry

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