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Isoforms Recommended: ERα
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ERα

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製品番号 製品名 Target 研究分野 構造式
  • HY-A0036
    Bazedoxifene acetate
    15+ Cited Publications

    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 .
    Bazedoxifene acetate
  • HY-A0031
    Bazedoxifene
    15+ Cited Publications

    TSE-424

    Estrogen Receptor/ERR Neurological Disease 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 .
    Bazedoxifene
  • HY-100689
    Propyl pyrazole triol
    15+ Cited Publications

    PPT

    Estrogen Receptor/ERR Cancer
    Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%) .
    Propyl pyrazole triol
  • 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 .
    Estriol
  • HY-150505
    DC-U4106
    1 Publications Verification

    Deubiquitinase Apoptosis Cancer
    DC-U4106 is a USP8 targeting inhibitor with the Kdvalue 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 .
    DC-U4106
  • HY-153468

    TEQ103; Sera2

    Sodium Channel TRP Channel Cancer
    ErSO-TFPy (TEQ103) is an ERα+ tumor cell inhibitor with low nanomolar cytotoxic activity against ERα+ breast cancer cells. ErSO-TFPy activates the sodium channel TRPM4, causes an imbalance of intracellular calcium and sodium ions. ErSO-TFPy dysregulates calcium homeostasis in ERα+ tumor cells, triggers the anticipatory unfolded protein response, and induces rapid immune cell-independent necrotic cell death. ErSO-TFPy can be used for the research of estrogen receptor alpha positive breast cancer .
    ErSO-TFPy
  • HY-112100

    PROTAC-Linker Conjugates for PAC Estrogen Receptor/ERR Cancer
    MC-Val-Cit-PAB-PROTAC ERα Degrader-1 (compound LP2) consists an ADC linker and a PROTAC, whcih can be conjugated to an antibody to form PACs. MC-Val-Cit-PAB-PROTAC ERα Degrader-1 conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab) .
    MC-Val-Cit-PAB-PROTAC ERα Degrader-1
  • HY-162312

    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 .
    LLK203
  • HY-111846
    PROTAC ERα Degrader-2
    1 Publications Verification

    PROTACs Estrogen Receptor/ERR Cancer
    PROTAC ERα Degrader-2 (Compound 11) is a ERα PROTAC degrader. PROTAC ERα Degrader-2 significantly down-regulates the level of ERα in MCF-7 cells.(Pink: AR ligand (HY-43962), Blue: IAP Ligand (HY-177389), Black: Linker (HY-128833)) .
    PROTAC ERα Degrader-2
  • HY-112611

    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 Kis 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 .
    H3B-5942
  • HY-W036120

    2,2′,4,4′-Tetrahydroxybenzophenone

    Environmental Pollutants Glycosidase Estrogen Receptor/ERR Pregnane X Receptor (PXR) Metabolic Disease Endocrinology
    Benzophenone-2 (2,2',4,4'-Tetrahydroxybenzophenone) is an organic ultraviolet absorber that is widely used in personal care products and industrial products such as plastics and coatings. Benzophenone-2 is an endocrine disruptor that can interfere with estrogen receptors (ERα receptor) and pregnane X receptor (PXR receptor) activity, leading to reproductive toxicity, immune disorders, and metabolic abnormalities. Benzophenone-2 can inhibit the activity of α-glucosidase (IC50 = 49.72 μM), and can be used for research on diabetes .
    Benzophenone-2
  • HY-126109

    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 .
    (±)-8-Prenylnaringenin
  • 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-103457

    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 (Ki=0.09 nM) over ERβ (Ki=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells .
    Y134
  • HY-125703

    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 .
    Ferutinin
  • HY-108414

    (+)-Equol

    Estrogen Receptor/ERR Cancer
    (R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively.
    (R)-Equol
  • HY-149295

    PROTACs Estrogen Receptor/ERR Apoptosis Cancer
    PROTAC ERα Degrader-4 (Compound ZD12) is a highly potent and selectivePROTAC ERα degrader (Ki: 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.
    PROTAC ERα Degrader-4
  • 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.
    PROTAC ERα Degrader-1
  • HY-137144

    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 .
    Fulvestrant-3-boronic acid
  • HY-W088749

    PROTAC Linkers Cancer
    tert-Butyl-hexanedioic acid is a PROTAC linker. tert-Butyl-hexanedioic acid can be used to synthesize PROTAC molecules, such as PROTAC ERα Degrader-12 (HY-174453) .
    tert-Butyl-hexanedioic acid
  • HY-W1006471

    Estrogen Receptor/ERR Endocrinology
    Estrogen receptor-agonist-1 (compound 4e) is a estrogen receptor (ER) agonist that binds to ERα with high affinity .
    Estrogen receptor-agonist-1
  • HY-145341

    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 .
    GNE-149
  • HY-177445

    Histone Acetyltransferase Estrogen Receptor/ERR Cancer
    KAT6-IN-4 (Compound Example 2) is a selective lysine acetyltransferase 6 (KAT6) inhibitor. KAT6-IN-4 suppresses transcription of oncogenes like ERα. KAT6-IN-4 demonstrates potent antitumor efficacy in ER +/HER2 - breast cancer xenografts. KAT6-IN-4 is promising for research of KAT6-driven malignancies (e.g., breast cancer, NSCLC) .
    KAT6-IN-4
  • HY-176364

    Estrogen Receptor/ERR Target Protein Ligand-Linker Conjugates Cancer
    AZD9496-O-C3-O-C3-O-C-acid is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for ERα (HY-12870) and a PROTAC linker, which recruits E3 ligases. AZD9496-O-C3-O-C3-O-C-acid can be used for synthesis of PROTAC AZ'6421 (HY-135312) .
    AZD9496-O-C3-O-C3-O-C-acid
  • HY-A0031A

    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 .
    Bazedoxifene hydrochloride
  • HY-129619

    SNIPERs Estrogen Receptor/ERR Cancer
    SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein (IC50=0.097 μM). SNIPER(ER)-87 preferentially recruits XIAP to ERα in the cells, and XIAP is the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-induced ERα degradation .
    SNIPER(ER)-87
  • HY-W1005067

    Molecular Glues Hippo (MST) Estrogen Receptor/ERR Others
    EN171 is a covalent ligand that covalently targets both C38 and C96 on 14-3-3 to enhance 14-3-3 interactions with ERα, YAP and TAZ, leading to impaired estrogen receptor and Hippo pathway transcriptional activity. EN171 can not only be used as a molecular glue to enhance native protein interactions but can also be used as a covalent 14-3-3 recruiter in heterobifunctional molecules to sequester nuclear neo-substrates such as BRD4 and BLC6 into the cytosol .
    EN171
  • HY-A0036R

    TSE-424 acetate (Standard)

    Reference Standards Estrogen Receptor/ERR Cancer
    Bazedoxifene (acetate) (Standard) is the analytical standard of Bazedoxifene (acetate). This product is intended for research and analytical applications. 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 .
    Bazedoxifene acetate (Standard)
  • HY-178961

    PROTACs Estrogen Receptor/ERR Apoptosis Cancer
    PROTAC ERα Degrader-13 is an orally active PROTAC molecule that efficiently and selectively degrades ERα (DC50 = 3.78 nM). PROTAC ERα Degrader-13 has the characteristics of strong anti proliferation (IC50 = 0.6 nM), induction of apoptosis, and overcoming drug resistance in MCF-7 cells. PROTAC ERα Degrader-13 has good safety and no significant organ toxicity. PROTAC ERα Degrader-13 can be used for cancer research .
    PROTAC ERα Degrader-13
  • HY-174870

    PROTACs Estrogen Receptor/ERR Apoptosis Fluorescent Dye Cancer
    PROTAC ERα Degrader-11 is a selective and intrinsically fluorescent (Ex: 366 nm, Em: 440 nm) ERα PROTAC degrader. PROTAC ERα Degrader-11 shows good antiproliferative activity, selective ERα degradation and imaging capabilities in MCF-7 breast cancer cell lines. PROTAC ERα Degrader-11 induces G2/M phase arrest and induces apoptosis in MCF-7 cells. PROTAC ERα Degrader-11 is well-tolerated up to a dose of 500 mg/ kg with no acute toxicity in athymic nude mice. PROTAC ERα Degrader-11 can be used for the study of breast cancer.(Pink: ERα ligand (HY-167701), Blue: CRBN Ligand (HY-150831), Black: Linker, E3 ligase ligand-linker conjugate (HY-174880)) .
    PROTAC ERα Degrader-11
  • HY-174453

    PROTACs Estrogen Receptor/ERR Apoptosis Cancer
    PROTAC ERα Degrader-12 is a potent and selective Erα PROTAC degrader. PROTAC ERα Degrader-12 has antiproliferative effects in multiple breast cancer cell lines with wild-type or mutant ERα. PROTAC ERα Degrader-12 can halt the cell cycle and induce cell apoptosis. PROTAC ERα Degrader-12 exhibits excellent antitumor and ERα degradation activity. PROTAC ERα Degrader-12 can be used for research on breast cancer. (Pink: ER ligand-11 (HY-174475); Blue: VHL ligand (HY-112078); Black: Linker (HY-W088749); VHL ligand + Linker ( HY-W998310)) .
    PROTAC ERα Degrader-12
  • HY-145556

    Estrogen Receptor/ERR Cancer
    Bexirestrant is an orally active ER-α degrader. Bexirestrant can be used for the research of antiestrogen, antineoplastic .
    Bexirestrant
  • HY-144733

    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 .
    ERα antagonist 1
  • HY-175872

    Estrogen Receptor/ERR Molecular Glues Others
    14-3-3σ/ERα stabilizer-2 (Compound 41) is a covalent 14-3-3σ/ERα stabilizer with a Kd of 10.1 nM. 14-3-3σ/ERα stabilizer-2 significantly decreases the dissociation rate of ERα, stabilizing the binary ERα/14-3-3σ interaction. 14-3-3σ/ERα stabilizer-2 can be used for molecular glues research .
    14-3-3σ/ERα stabilizer-2
  • HY-W114419

    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 .
    Bisphenol C
  • HY-125263

    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-175448

    PROTACs Estrogen Receptor/ERR IAP Cancer
    GNE-1567 is a potent ERα PROTAC degrader and a selective XIAP antagonist with a Kd 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)) .
    GNE-1567
  • HY-168205

    HSP Apoptosis Cancer
    HSP90-IN-33 (compound 24e) is a potent Hsp90 inhibitor with Kd values of ≥200, 7.3 µM for Hsp90α, Hsp90β, respectively. HSP90-IN-33 induces apoptosis and cell cycle arrest at G0/G1 phase. HSP90-IN-33 decreases the protein expression of ERα, CDK4 and Akt .
    HSP90-IN-33
  • HY-16023
    Acolbifene hydrochloride
    2 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 .
    Acolbifene hydrochloride
  • HY-W998310

    E3 Ligase Ligand-Linker Conjugates Cancer
    (S,R,S)-AHPC-Me-CO-C4-COOH is a conjugate of the E3 ligase VHL ligand and a linker, which can be used to synthesize PROTAC ERα Degrader-12 (HY-174453). PROTAC ERα Degrader-12 is a potent and highly selective ERα PROTAC degrader .
    (S,R,S)-AHPC-Me-CO-C4-COOH
  • HY-176955

    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 .
    ER degrader 12
  • HY-175171

    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 .
    Anticancer agent 276
  • HY-168869

    PROTACs Estrogen Receptor/ERR Cancer
    Tamoxifen-PEG-Clozapine is an estrogen receptor α (ERα) PROTAC degrader. Tamoxifen-PEG-Clozapine degrades ERα via a ubiquitin-proteasome system that uses the ubiquitin protein ligase E3 component N-recognin 5. Tamoxifen-PEG-Clozapine can be used for the research of cancer . (Pink: ERα inhibitor (HY-W271653); Black: linker (HY-168870); Blue: CRBN Ligand (HY-G0021))
    Tamoxifen-PEG-Clozapine
  • HY-131404
    TPBM
    2 Publications Verification

    Estrogen Receptor/ERR Cancer
    TPBM is a potent estrogen receptor α (ERα) inhibitor with an IC50 value of 9 μM for 17β-estradiol (E2)-ERα. TPBM reduces EERα recruitment to an endogenous estrogen-responsive gene. TPBM inhibits E2-dependent growth of ERα-positive cancer cells (IC50=5 μM). TPBM is not toxic to cells and does not affect estrogen-independent cell growth .
    TPBM
  • HY-126932

    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 .
    TTC-352
  • HY-132294A

    Estrogen Receptor/ERR Cancer
    (1S,3R)-GNE-502 (compound 179) is a potent ERα degrader with an EC50 value of 13 nM against ERα in MCF7 HCS. (1S,3R)-GNE-502 can be used to research cancer related with estrogen receptor .
    (1S,3R)-GNE-502
  • HY-179045

    Estrogen Receptor/ERR Apoptosis Cancer
    ERα degrader 14 (Compound B7) is a potent ERα degrader. ERα degrader 14 exhibits significantly potent and selective anti-proliferative activity on two ERα-positive breast cancer cell lines (MCF-7 and T47D). ERα degrader 14 induces cell cycle arrest, inhibits cell migration, and induces cell apoptosis. ERα degrader 14 effectively inhibits tumor growth in mouse models. ERα degrader 14 can be used for the study of breast cancer .
    ERα degrader 14
  • HY-132194

    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 .
    ERα degrader-2
  • HY-169941

    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 .
    ERα/ERβ antagonist-1
  • HY-156125

    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 .
    14-3-3σ/ERα stabilizer-1

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