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Results for "

human ERα

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) Autophagy (1) Biochemical Assay Reagents (1) c-Met/HGFR (1) COX (1) Drug Metabolite (2) EGFR (1) Endogenous Metabolite (2) Estrogen Receptor/ERR (18) Isotope-Labeled Compounds (1) Microtubule/Tubulin (1) NO Synthase (2) PROTACs (1) Reference Standards (1) Serotonin Transporter (1) Topoisomerase (1) TRP Channel (1) VEGFR (1) Wnt (1)
By Research Areas:	Cancer (16) Cardiovascular Disease (4) Endocrinology (1) Metabolic Disease (1) Neurological Disease (3)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100583A

(±)-Equol	Estrogen Receptor/ERR Drug Metabolite	Cardiovascular Disease Neurological Disease Cancer
(±)-Equol is the racemate of equol. (±)-equol exhibits EC₅₀s of 200 and 74 nM for human ERα and ERβ, respectively. Equol is a metabolite of the soy isoflavones, daidzin and daidzein.

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-14933

Prinaberel 3 Publications Verification ERB-041	Estrogen Receptor/ERR Wnt Apoptosis	Cancer
Prinaberel (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC₅₀s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. Prinaberel induces ovarian cancer apoptosis .

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-114411

ERRγ inverse agonist 1	Estrogen Receptor/ERR	Cancer
ERRγ inverse agonist 1 (Compound 12) is a selective ERRγ inverse agonist with an IC₅₀ value of 0.040 μM against ERRγ. ERRγ inverse agonist 1 inhibits the activity of ERRγ at the functional level. ERRγ inverse agonist 1 can be used in the research of anaplastic thyroid cancer .

HY-W008581

Estradiol 3-methyl ether 3-O-Methyl estradiol; 17β-Estradiol 3-methyl ether; 3-Methoxyestradiol	Biochemical Assay Reagents TRP Channel Microtubule/Tubulin Autophagy	Metabolic Disease Cancer
Estradiol 3-methyl ether (EDME) is a highly selective TRPML1 ion channel antagonist and microtubule (microtubule) depolymerizing agent, with IC₅₀ values of 0.22 μM and 3.8 μM against TRPML1 and TRPML2, respectively; it shows no activity against TRPML3. Estradiol 3-methyl ether induces the disruption of cytoplasmic microtubule networks in mammalian cells, with an EC₅₀ of 9 μM. Independent of estrogen receptors, Estradiol 3-methyl ether blocks autophagy (autophagy), TFEB nuclear translocation, and inhibits the migration and invasion of triple-negative breast cancer cells by suppressing TRPML1. Estradiol 3-methyl ether is applicable for relevant research on triple-negative breast cancer .

HY-126932

TTC-352	Estrogen Receptor/ERR	Cancer
TTC-352 is an orally bioavailable selective human estrogen receptor (ER) α partial agonist (ShERPA). TTC-352 inhibits the growth of three ER+ breast cancer cells. TTC-352 induces tumor regression accompanied by exit of *ERα* from the nucleus to extranuclear sites .

HY-175171

Anticancer agent 276	Topoisomerase VEGFR c-Met/HGFR EGFR Estrogen Receptor/ERR	Cancer
Anticancer agent 276 (Compound 5) is a multi-target anticancer agent. Anticancer agent 276 has a potent anticancer activity against human tumor cells with IC₅₀s of 6.90 and 4.48 μM for HEPG2 and MCF7 cells, respectively. Anticancer agent 276 shows strong and stable interactions across multiple targets, including Topoisomerase II, VEGFR2, c-Met, EGFR and ERα .

HY-100583AR

(±)-Equol (Standard)	Reference Standards Estrogen Receptor/ERR Drug Metabolite	Cardiovascular Disease Neurological Disease Cancer
(±)-Equol (Standard) is the analytical standard of (±)-Equol. This product is intended for research and analytical applications. (±)-Equol is the racemate of equol. (±)-equol exhibits EC50s of 200 and 74 nM for human ERα and ERβ, respectively. Equol is a metabolite of the soy isoflavones, daidzin and daidzein.

HY-123664

Trioxifene mesylate LY133314	Estrogen Receptor/ERR	Cancer
Trioxifene mesylate (LY133314) is an orally active and selective estrogen receptor (ER) modulator with human *ERα* IC₅₀ of 203.49 nM and K_i of 20.84 nM. Trioxifene mesylate binds estradiol receptors, inhibits ERα-mediated gene expression, reduces circulating gonadotrophin levels. Trioxifene mesylate can be used for the research of advanced breast cancer and androgen-independent, metastatic prostatic adenocarcinoma .

HY-121372

Lactandrate	Estrogen Receptor/ERR	Cancer
Lactandrate is a D-high nitrogen steroid alkylating agent. It can interact with the ligand-binding domain (LBD) of estrogen receptor-alpha (ERα). Lactandrate has a growth inhibitory effect on breast cancer cells, with a GI₅₀ value ranging from 5 to 65 μM. It shows anti-tumor activity in mouse breast tumors (MXT and CD8F1) as well as in human xenograft MX-1 .

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-B0141E

ent-Estradiol ent-β-Estradiol; ent-17β-Estradiol; ent-17β-Oestradiol	Estrogen Receptor/ERR	Endocrinology
Ent-Estradiol is the enantiomer of Estradiol (HY-B0141). Ent-Estradiol is a highly selective estrogen receptor ligand, but does not possess estrogenic activity. Ent-Estradiol displays IC₅₀ values of 24.9 nM, 9.59 nM and 8.17 nM for human, rat and mouse ERβ, and 151 nM, 246 nM and 268 nM for human, rat and mouse ERα, respectively. Ent-Estradiol can be used for the study of menopausal physiological changes .

HY-135529

Trioxifene LY133314 free base	Estrogen Receptor/ERR	Cancer
Trioxifene (LY133314 free base) is an orally active and selective estrogen receptor (ER) modulator with human *ERα* IC₅₀ of 203.49 nM and K_i of 20.84 nM. Trioxifene binds estradiol receptors, inhibits ERα-mediated gene expression, reduces circulating gonadotrophin levels. Trioxifene can be used for the research of advanced breast cancer and androgen-independent, metastatic prostatic adenocarcinoma .

HY-183187

4H-Chromen-4-one-o-carborane	Estrogen Receptor/ERR COX	Cancer
4H-Chromen-4-one-o-carborane is an estrogen receptor (ER) agonist, with an EC₅₀ of 0.9 μM for ERα and an EC₅₀ of 11.1 μM for ERβ. 4H-Chromen-4-one-o-carborane also acts as an inhibitor of COX-1 and COX-2, with an IC₅₀ of 6.6 μM for COX-1 and an IC₅₀ of 17.7 μM for COX-2 .

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-184011

SERT-IN-4	Serotonin Transporter Estrogen Receptor/ERR	Neurological Disease
SERT-IN-4 is a brain-penetrant and orally active SERT inhibitor and ERβ agonist with human SERT IC₅₀ of 16.92 nM and human ERβ EC₅₀ of 3.66 nM. SERT-IN-4 inhibits SERT-mediated substrate transport, increases hippocampal serotonin levels, modulates p-CREB and BDNF expression.SERT-IN-4 reduces immobility in CUMS mice, improves social interaction and reduces inactivity in CSDS mice.SERT-IN-4 can be used for the research of major depressive disorder .

HY-125675

VPC-16606	Estrogen Receptor/ERR	Cancer
VPC-16606 is a selective inhibitor targeting the activation function 2 (AF2) domain of estrogen receptor α (ERα). VPC-16606 blocks the interaction between ERα and coactivators, inhibits the activity of both wild-type and clinically drug-resistant mutant ERα, and exerts inhibitory effects on hormone-resistant breast cancer cells. VPC-16606 can be used in breast cancer research .

HY-183804

PROTAC ER Degrader-16	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ER Degrader-16 is an orally active ERα PROTAC degrader with a DC₅₀ of 1.4 nM and an IC₅₀ of 1.9 nM. PROTAC ER Degrader-16 inhibits ER-dependent breast cancer cell proliferation and exerts anti-tumor effects in mouse models. PROTAC ER Degrader-16 can be used for breast cancer research .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-100583A

(±)-Equol	Cardiovascular Disease Monophenols Neurological Disease Classification of Application Fields Leguminosae Glycine max (L.) merr Phenols Polyphenols Plants Disease Research Fields Source Classification	Estrogen Receptor/ERR Drug Metabolite
(±)-Equol is the racemate of equol. (±)-equol exhibits EC₅₀s of 200 and 74 nM for human ERα and ERβ, respectively. Equol is a metabolite of the soy isoflavones, daidzin and daidzein.

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-100583AR

(±)-Equol (Standard)	Structural Classification Monophenols Leguminosae Glycine max (L.) merr Phenols Polyphenols Plants Source Classification	Reference Standards Estrogen Receptor/ERR Drug Metabolite
(±)-Equol (Standard) is the analytical standard of (±)-Equol. This product is intended for research and analytical applications. (±)-Equol is the racemate of equol. (±)-equol exhibits EC50s of 200 and 74 nM for human ERα and ERβ, respectively. Equol is a metabolite of the soy isoflavones, daidzin and daidzein.

Cat. No.	Product Name	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 .

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