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Isoforms Recommended:	ERα

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ERα

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By Targets:	Apoptosis (8) Biochemical Assay Reagents (1) Cytochrome P450 (1) Deubiquitinase (2) Endogenous Metabolite (1) Estrogen Receptor/ERR (39) Ligands for E3 Ligase (2) Ligands for Target Protein for PROTAC (1) Prostaglandin Receptor (1) PROTAC-Linker Conjugates for PAC (1) PROTACs (7) SNIPERs (1) YAP (1)
By Research Areas:	Cancer (41) Endocrinology (4) Infection (1) Inflammation/Immunology (2) Metabolic Disease (1)
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-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-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-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-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 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-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	Estrogen Receptor/ERR	Cancer
Bexirestrant is an orally active *ER-α* degrader. Bexirestrant can be used for the research of antiestrogen, antineoplastic .

HY-112098

*PROTAC ERα* Degrader-1**	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-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-111846

*PROTAC ERα* Degrader-2**	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-157765

*PROTAC ERα* Degrader-6**	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ERα Degrader-6 (compound A3) is a potent PROTAC degrader of ERα, with DC₅₀ of 0.12 μM. 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-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-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 .

*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-111484A

GDC-0927 Racemate SRN-927 Racemate	Estrogen Receptor/ERR	Cancer
GDC-0927 Racemate (SRN-927 Racemate) is a degrader of estrogen receptor, potently inhibits *ER-α* activity, with an IC₅₀ of 0.2 nM, and is used in the research of ER-related diseases.

HY-19498

WAY-204688 SIM-688
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-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-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-125263

OP-1074	Estrogen Receptor/ERR	Cancer
OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC₅₀ of 1.6 and 3.2 nM, respectively .

HY-135590

Raloxifene 4-Monomethyl Ether	Estrogen Receptor/ERR
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-125263B

(R)-OP-1074	Others	Cancer
(R)-OP-1074 is the isomer of OP-1074 (HY-125263), and can be used as an experimental control. OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC₅₀ of 1.6 and 3.2?nM, respectively .

HY-135584

Raloxifene 6-Monomethyl Ether	Estrogen Receptor/ERR
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-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-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-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-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-127133

Methylpiperidino pyrazole MPP	Biochemical Assay Reagents
MPP is a highly selective estrogen receptor alpha (ERα) antagonist. MPP reduces the ratio of p-ERα/ERα . https://www.ncbi.nlm.nih.gov/pubmed/29799481 Labouesse MA, et al. Effects of selective estrogen receptor alpha and beta modulators on prepulse inhibition in male mice. Psychopharmacology (Berl). 2015 Aug;232(16):2981-94. https://www.ncbi.nlm.nih.gov/pubmed/25893642

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-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-144070A

(Rac)-ErSO-DFP	Estrogen Receptor/ERR	Cancer
(Rac)-ErSO-DFP is a derivative of ErSO-DFP and a selective small molecule Erα biomodulator. (Rac)-ErSO-DFP againsts ERα+ breast cancer (including resistant tumors) by hyperactiving the Erα-dependent a-UPR (extracted from patent WO2022087234A1) .

HY-16023A

Acolbifene 1 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-B0723S

Ospemifene D4 FC-1271a d₄	Estrogen Receptor/ERR	Cancer
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[1][2].

HY-16023

Acolbifene hydrochloride 1 Publications Verification EM-652 hydrochloride; SCH 57068 hydrochloride	Estrogen Receptor/ERR	Cancer
Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC₅₀=2 nM) and ERβ (IC₅₀=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties .

HY-162312

LLK203	Deubiquitinase Apoptosis	Cancer
LLK203 is a potent USP2/USP8 dual-target inhibitor with IC₅₀s of 0.89 μM and 0.52 μM, respectively. LLK203 leads a degradation of ERα and induces apoptosis of breast cancer MCF-7 cells. LLK203 demonstrates antitumor activities against the 4T1 tumor mice model .

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-B0412

Estriol 3 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-126109

(±)-8-Prenylnaringenin	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 .

HY-147165

VT02956	YAP	Cancer
VT02956 is a LATS inhibitor (IC₅₀: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids . VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-A0031

Bazedoxifene Maximum Cited Publications 10 Publications Verification TSE-424	Estrogen Receptor/ERR	Cancer
Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC₅₀s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .

HY-A0036

Bazedoxifene acetate Maximum Cited Publications 10 Publications Verification TSE-424 acetate	Estrogen Receptor/ERR	Cancer
Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal selective estrogen receptor modulator (SERM), with IC₅₀s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .

HY-A0031A

Bazedoxifene hydrochloride TSE-424 hydrochloride	Estrogen Receptor/ERR	Cancer
Bazedoxifene hydrochloride (TSE-424 hydrochloride) is an oral active, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC₅₀s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride acts as an inhibitor of IL-6/GP130 protein-protein interactions. Bazedoxifene hydrochloride can be used for the research of pancreatic cancer .

HY-139999

LCL-PEG3-N3	Ligands for E3 Ligase	Cancer
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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

HY-139999A

LCL-PEG3-N3 hydrochloride	Ligands for E3 Ligase	Cancer
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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-125703

Ferutinin	Infection Classification of Application Fields Terpenoids Sesquiterpenes Source classification Thymus quinquecostatus Cêlak. Plants Umbelliferae 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 3 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[1][2].

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ERα

Inhibitors & Agonists

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Isotope-Labeled Compounds

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