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Isoforms Recommended:	ERα

Results for "

ERα

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (1) Apoptosis (11) Cytochrome P450 (3) Deubiquitinase (2) E3 Ligase Ligand-Linker Conjugates (2) Endogenous Metabolite (1) Estrogen Receptor/ERR (60) Hippo (MST) (1) HSP (1) Isotope-Labeled Compounds (1) LDLR (1) Ligands for Target Protein for PROTAC (1) Molecular Glues (1) NF-κB (1) Prostaglandin Receptor (1) PROTAC-Linker Conjugates for PAC (1) PROTACs (10) SNIPERs (1) YAP (1)
By Research Areas:	Cancer (58) Endocrinology (9) Infection (1) Inflammation/Immunology (4) Metabolic Disease (3)
Click Chemistry:	Azide (2)

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-132194

ERα degrader-2	Estrogen Receptor/ERR	Cancer
ERα degrader-2 is a selective estrogen receptor degrader (SERD) with potent binding affinity with ERα (IC₅₀=17.1 nM), good degradation efficacy (EC₅₀=0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent agentgability, can be used for HER ⁺ breast cancer research .

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-170806

ERα degrader 12	Estrogen Receptor/ERR	Cancer
ERα degrader 12 (Compound RA3) is an estrogen receptor α (ERα) degrader with antitumor properties. ERα degrader 12 induces pronounced tumor growth inhibition in a breast cancer xenograft mouse model .

HY-168101

ERα degrader 11	Estrogen Receptor/ERR	Cancer
ERα degrader 11 (compound B16) is a selective ERα degrader that can be used as an estrogen receptor probe to investigate ER status in ER-positive breast cancer cells .

HY-168099

ERα degrader 10	Estrogen Receptor/ERR	Cancer
ERα degrader 10 is a selective and orally active estrogen receptor α (ERα) degrader. ERα degrader 10 exhibits potent ERα binding affinity (IC₅₀ of 24.0 nM) and degradation ability (EC₅₀ of 5.3 nM). ERα degrader 10 degrades ERα through the proteasome-mediated pathway. ERα degrader 10 can be used for the study of breast cancer .

HY-155492

ERα degrader 7	Estrogen Receptor/ERR	Cancer
ERα degrader 7 (compound B1) is a potent ERα degrader with an IC₅₀ of 14.6 nM and a DC₅₀ of 9.7 nM, respectively. ERα degrader 7 shows excellent antitumor activity, indicating its potential to evolve as a promising selective estrogen-receptor degrader (SERD) for breast cancer research .

HY-144306

ERα degrader 4	Estrogen Receptor/ERR Apoptosis	Cancer
ERα degrader 4 is an excellent and selective estrogen receptor α (ERα) degrader (IC₅₀ of 0.31, 0.41 and 0.48 μM in MDA-MB-231, MCF-7 and MCF-7/ADR cells, respectively). ERα degrader 4 has potent inhibitory activity against MCF-7 cell lines. ERα degrader 4 is a potential SERDs candidate for the research of breast cancer .

HY-P10393

ERα17p ERα (295-311)	Apoptosis	Cancer
ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .

HY-168644

Erα-IN-1	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. .

HY-146267

ERα degrader 5	Estrogen Receptor/ERR	Cancer
ERα degrader 5 (Compound 40) is a selective, orally bioavailable estrogen receptor (ER) degrader (SERD) with an EC₅₀ of 1.1 nM against ERα. ERα degrader 5 shows antitumor effect in vivo .

HY-161692

ERα degrader 8	Estrogen Receptor/ERR	Cancer
ERα degrader 8 (Compound 18j) is a selective Estrogen Receptor degrader. ERα degrader 8 is degrader to MCF-7 cells with IC₅₀ value of 0.15 μM .

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-163680

ERα degrader 9	Estrogen Receptor/ERR Cytochrome P450	Cancer
ERα degrader 9 is a dual targeting ligand for estrogen receptor α (ERα) and aromatase (ARO). ERα degrader 9 can be utilized for synthesis of PROTAC ERα Degrader-9 (HY-163679) .

HY-172937

ERα degrader 13	Estrogen Receptor/ERR	Cancer
ERα degrader 13 (compound MR3) is potent ERα degrader with an IC₅₀ of 0.55 μM. ERα degrader 13 induces an obvious tumor regression in the breast cancer xenograft mouse model .

HY-149081

ERα degrader 6	Estrogen Receptor/ERR Cytochrome P450	Cancer
ERα degrader 6 (Compound 31q) is an ERα degrader (K_I: 75 nM). ERα degrader 6 also inhibits ARO with an IC₅₀ of 37.7 nM. ERα degrader 6 inhibits tumor growth in MCF-7 tumor xenograft model. ERα degrader 6 can be used for breast cancer research .

HY-111845

Estrone-N-O-C1-amido ERα ligand 1	Estrogen Receptor/ERR Ligands for Target Protein for PROTAC	Cancer
Estrone-N-O-C1-amido (ERα ligand 1) is an Estrone-based estrogen ligand, which targets estrogen receptor α (ERα). Estrone-N-O-C1-amido (ERα ligand 1) binds to cIAP1 ligand Bestatin via a linker to form SNIPER .

HY-156125

*14-3-3σ/ERα* stabilizer-1**	Estrogen Receptor/ERR	Others
14-3-3σ/ERα stabilizer-1 (Compound 181) is a covalent *14-3-3σ*/ERα stabilizer. 14-3-3σ/ERα stabilizer-1 can be used for research of molecular glues .

HY-149295

*PROTAC ERα* Degrader-4**	PROTACs Estrogen Receptor/ERR Apoptosis	Cancer
PROTAC ERα Degrader-4 (Compound ZD12) is a highly potent and selectivePROTAC ERα degrader (K_i: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER ⁺ breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.

HY-163467

CHEMBL4224880	Estrogen Receptor/ERR	Cancer
CHEMBL4224880 is an estrogen receptor-α (ER-α) binder .

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 .

HY-112100

*PROTAC ERα* Degrader-5**	PROTAC-Linker Conjugates for PAC Estrogen Receptor/ERR	Cancer
PROTAC ERα Degrader-5 (compound LP2) consists an ADC linker and a PROTAC, whcih can be conjugated to an antibody to form PACs. PROTAC ERα Degrader-5 conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab) .

HY-160563

*PROTAC ERα* Degrader-8**	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ERα Degrader-8 (compound ii-56) is a potent PROTAC degrader of Erα, with DC₅₀ of 0.000006 μM in MCF7 cells .

HY-111846

*PROTAC ERα* Degrader-2** 1 Publications Verification	SNIPERs PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ERα Degrader-2 comprises a IAP ligand binding group, a linker and an estrogen receptor α (ERα) binding group. PROTAC ERα Degrader-2 is an ERα degrader. Maximal ERα degradation at 30 μM concentration in human mammary tumor MCF7 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs) .

HY-170336

*PROTAC ERα* Degrader-10**	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ERα Degrader-10 (Compound 160a) is an orally active degrader for ERα with DC₅₀ of 0.37-1.1 nM, in cells MCF7, T47D and CAMA-1. PROTAC ERα Degrader-10 exhibits antitumor efficacy in mouse model . (Pink: ligand for target protein (HY-170339); Black: linker (HY-30105); Blue: ligand for E3 ligase Cereblon (HY-168055))

HY-157765

*PROTAC ERα* Degrader-6**	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ERα Degrader-6 (compound A2) is a potent PROTAC degrader of ERα, with IC₅₀ of 0.11 μM in MCE-7 cells. PROTAC ERα Degrader-6 has anti-tumor effect. PROTAC ERα Degrader-6 is a fluorescent probes with Em of 582 nm that enable real-time visualization of ERα protein degradation .

HY-163679

*PROTAC ERα* Degrader-9**	Estrogen Receptor/ERR Cytochrome P450 PROTACs Apoptosis	Cancer
PROTAC ERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader, which degrades estrogen receptor α (ERα) and aromatase (ARO). PROTAC ERα Degrader-9 binds to ERα with a K_i of 0.25 μM, inhibits ARO with an IC₅₀ of 4.6 μM. PROTAC ERα Degrader-9 inhibits the proliferation of MCF-7 wildtype (IC₅₀=0.54 μM) and ERα mutants MCF-7 ^EGFR (IC₅₀=0.075 μM), MCF-7 ^D538G (IC₅₀=0.31 μM), MCF-7 ^Y537S (IC₅₀=2.3 μM), downregulates the expressions of ERS1 and MYC. PROTAC ERα Degrader-9 arrests the cell cycle at G2/M, induces apoptosis in MCF-7. PROTAC ERα Degrader-9 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-163680); Black: linker (HY-W007559); Blue: ligand for E3 ligase (HY-112078))

HY-160562

*PROTAC ERα* Degrader-7**	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ERα Degrader-7 (compound i-320) is a potent estrogen receptor alpha(ERα) PROTAC degrader with a DC₅₀ value of 0.000006 µM. PROTAC ERα Degrader-7 comprises a cereblon-binding moiety LBM linked to a ligand ERBM that binds ERα and comprises a benzofused partially saturated 6-membered carbocyclic or heterocyclic ring .

HY-112098

*PROTAC ERα* Degrader-1** 1 Publications Verification	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.

HY-111484A

GDC-0927 Racemate 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.

HY-19498

WAY-204688 SIM-688	NF-κB	Inflammation/Immunology
WAY-204688 is an estrogen receptor (ER-α) selective, orally active inhibitor of NF-κB transcriptional activity with an IC₅₀ of 122 ± 30 nM for NF-κB-luciferase (NF-κB-luc) in HAECT-1 cells.

HY-155196

ER degrader 6	Estrogen Receptor/ERR	Cancer
ER degrader 6 (compound 35s) is a potent Estrogen Receptor (ER)α degrader. ER degrader 6 disrupts the microtubule network by restraining tubulin polymerization. ER degrader 6 suppresses tumor growth without noticeable poisonousness .

HY-N7748A

Epi-cryptoacetalide	Estrogen Receptor/ERR Prostaglandin Receptor	Inflammation/Immunology Endocrinology
Epi-cryptoacetalide is a natural diterpenoid. Epi-cryptoacetalide reveals high affinity to *ER-α* and PGE2 receptor (EP2 subtype) with K_i values of 0.3 μM and 1.92 μM, respectively. Epi-cryptoacetalide has anti-endometriosis activities .

HY-145071

*PROTAC ERα* Y537S degrader-1**	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ERα Y537S degrader-1 comprises a ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Y537S degrader-1 extracts from patent WO2021143822, example 12. PROTAC ERα Y537S degrader-1 is an estrogen receptor-alpha (ERα) Y537S degrader .

HY-W1006471

Estrogen receptor-agonist-1	Estrogen Receptor/ERR	Endocrinology
Estrogen receptor-agonist-1 (compound 4e) is a estrogen receptor (ER) agonist that binds to ERα with high affinity .

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.

HY-164924

ERD-12310A	PROTACs	Cancer
ERD-12310A is a PROTAC targeting Estrogen Receptor α (ERα) with a ED₅₀ value of 47 pM. ERD-12310A has oral activity. ERD-12310A is composed of PROTAC target protein ligand ER ligand-4 (HY-164925) (red part), E3 ligase ligand (S)-Deoxy-thalidomide (HY-168055) (blue part) .

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.

HY-135590

Raloxifene 4-Monomethyl Ether	Estrogen Receptor/ERR	Endocrinology
Raloxifene 4-Monomethyl Ether (Compound 37) is a Raloxifene derivative that inhibits estrogen receptor α. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC₅₀ of 1 μM and a pIC₅₀ of 6 .

HY-135584

Raloxifene 6-Monomethyl Ether	Estrogen Receptor/ERR	Endocrinology
Raloxifene 6-Monomethyl Ether (Compound 7) is a Raloxifene derivative that inhibits estrogen receptor α. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC₅₀ of 250 nM and a pIC₅₀ of 6.6 .

HY-144314

PSDalpha	Estrogen Receptor/ERR	Cancer
PSDalpha is an ERα degrader conjugating photosensitizer (PS), triphenylamine benzothiadiazole (TB) and 17β-estradiol via an acetylene bond. PSDalpha shows excellent anti-proliferation performance on MCF-7 cells. The maximum absorption wavelength of PSDalpha in the visible region is located at 465 nm .

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-W114419

Bisphenol C	Estrogen Receptor/ERR	Others
Bisphenol C is an ERα agonist and ERβ antagonist that inhibits 17β-estradiol .

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-103454

MPP dihydrochloride 5+ Cited Publications	Estrogen Receptor/ERR Apoptosis	Endocrinology Cancer
MPP dihydrochloride is a potent and selective ER (estrogen receptor) modulator. MPP dihydrochloride induces significant apoptosis in the endometrial cancer and oLE cell lines. MPP dihydrochloride reverses the positive effects of beta-estradiol. MPP dihydrochloride has mixed agonist/antagonist action on murine uterine ERalpha in vivo .

HY-127133

Methylpiperidino pyrazole MPP	Estrogen Receptor/ERR	Endocrinology
Methylpiperidino pyrazole (MPP) is a potent and selective ER (estrogen receptor) modulator. Methylpiperidino pyrazole induces significant apoptosis in the endometrial cancer and oLE cell lines. Methylpiperidino pyrazole reverses the the positive effects of beta-estradiol. Methylpiperidino pyrazole has mixed agonist/antagonist action on murine uterine ERalpha in vivo .

HY-137144

Fulvestrant-3-boronic acid ZB716	Estrogen Receptor/ERR	Cancer
Fulvestrant-3-boronic acid is an orally active ERα inhibitor, which binds to ERα competitively (IC₅₀ = 4.1 nM) and effectively degrades ERα in breast cancer cells .

HY-121441

Fispemifene	Estrogen Receptor/ERR	Inflammation/Immunology
Fispemifene, an orally active selective estrogen receptor modulator with anti-inflammatory and antiestrogenic action, attenuates glandular inflammation in an animal model of chronic nonbacterial prostatitis .

HY-150505

DC-U4106	Deubiquitinase Apoptosis	Cancer
DC-U4106 is a USP8 targeting inhibitor with the K_dvalue of 4.7 μM and the IC₅₀ value of 1.2 μM. DC-U4106 can target the ubiquitin pathway and facilitate the degradation of Erα. DC-U4106 inhibits tumor growth with minimal toxicity and has the potential for the research of breast cancer .

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-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 .

Cat. No.	Product Name	Target	Research Area

HY-P10393

ERα17p ERα (295-311)	Apoptosis	Cancer
ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-125703

Ferutinin	Viguiera dentata (Cav.) Spreng. Infection Structural Classification Classification of Application Fields Terpenoids Sesquiterpenes Source classification Umbelliferae Plants Disease Research Fields Endocrinology 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 .

HY-B0412

Estriol 4 Publications Verification Oestriol	Structural Classification Monophenols Immune System Disorder Classification of Application Fields Source classification Disease markers Phenols Endocrine diseases Endogenous metabolite Disease Research Fields Steroids Cancer	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-N7748A

Epi-cryptoacetalide	Terpenoids Labiatae Samanea saman (Jacq.) Merr. Diterpenoids Plants	Estrogen Receptor/ERR Prostaglandin Receptor
Epi-cryptoacetalide is a natural diterpenoid. Epi-cryptoacetalide reveals high affinity to *ER-α* and PGE2 receptor (EP2 subtype) with K_i values of 0.3 μM and 1.92 μM, respectively. Epi-cryptoacetalide has anti-endometriosis activities .

Cat. No.	Product Name	Chemical Structure

HY-B0723S

Ospemifene-d4
Ospemifene-d₄ is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active estrogen receptor modulator for the prevention of osteoporosis with IC₅₀ values of 827 nM and 1633 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene has bone-sparing, antitumor, and cholesterol-lowering effects .

Cat. No.	Product Name		Classification

HY-139999

LCL-PEG3-N3		Azide
LCL-PEG3-N3 is a decoy oligonucleotide ligand for E3 ligase which can be used for developing chimeric molecules LCL-ER(dec), degrading the estrogen receptor . LCL-PEG3-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HY-139999A

LCL-PEG3-N3 hydrochloride		Azide
LCL-PEG3-N3 (hydrochloride) is a decoy oligonucleotide ligand for E3 ligase which can be used for developing chimeric molecules LCL-ER(dec), degrading the estrogen receptor . LCL-PEG3-N3 (hydrochloride) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

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ERα

Inhibitors & Agonists

Peptides

NaturalProducts

Isotope-Labeled Compounds

Click Chemistry

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