2. Signaling Pathways
  3. Vitamin D Related/Nuclear Receptor
  4. Estrogen Receptor/ERR
  5. ERβ Isoform

ERβ

ERβ (estrogen receptor beta, ESR2) is a ligand-activated nuclear receptor that regulates transcriptional programs controlling cellular differentiation, proliferation, and tissue homeostasis through estrogen-responsive gene networks[1]. Mechanistically, ERβ functions as a transcription factor and can modulate estrogen signaling by interacting with target promoters and forming heterodimers with related estrogen receptor isoforms[2]. Through these activities, ERβ influences gene expression patterns associated with cell-cycle regulation and cellular growth control, making it an important regulator of physiological and pathological processes[1][2]. In disease contexts, reduced ERβ expression has been reported in multiple tumor types, and accumulating evidence supports a tumor-suppressive role for ERβ in cancer biology[1]. Experimental studies further demonstrate that ERβ activation can suppress proliferation and alter migration-associated transcriptional programs, supporting its utility in mechanistic cancer models[3]. Compared with the closely related isoform ERα, ERβ displays distinct transcriptional properties and can inhibit ERα-driven transcriptional activity under specific conditions, thereby reducing cellular sensitivity to estradiol signaling[2]. Structural analyses additionally indicate that ERβ adopts ligand-binding domain conformations that differ from ERα, providing a molecular basis for subtype-specific functional responses and pharmacological selectivity[4]. For experimental applications, several ERβ-selective agonists have been developed and are widely used to investigate ERβ-dependent signaling pathways, isoform-specific biology, and therapeutic mechanisms while minimizing ERα-mediated proliferative effects[5].

Cat. No. Product Name Effect Purity
  • HY-12452
    DPN
    		Agonist 99.66%
    DPN (Diarylpropionitrile) is a non-steroidal estrogen receptor β (ERβ) selective ligand, with an EC50 of 0.85 nM. DPN has neuroprotective effects in a number of neurological diseases.
  • HY-N0250
    Saikosaponin D
    		Activator 99.81%
    Saikosaponin D is a triterpene saponin isolated from Bupleurum, with anti-inflammatory, anti-bacterial, anti-tumor, and anti-allergic activities; Saikosaponin D inhibits selectin, STAT3 and NF-kB and activates estrogen receptor-β.
  • HY-103454
    MPP dihydrochloride
    		Modulator 99.54%
    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-103454B
    MPP hydrochloride
    		Modulator 99.25%
    MPP hydrochloride is a potent and selective ER (estrogen receptor) modulator. MPP hydrochloride induces significant apoptosis in the endometrial cancer and oLE cell lines. MPP hydrochloride reverses the the positive effects of beta-estradiol. MPP hydrochloride has mixed agonist/antagonist action on murine uterine ERalpha in vivo.
  • HY-14933
    Prinaberel
    		Agonist 98.05%
    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-135529
    Trioxifene
    		Modulator
    Trioxifene (LY133314 free base) is an orally active and selective estrogen receptor (ER) modulator with human ERα IC50 of 203.49 nM and Ki 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-186074
    ERβ agonist-2
    		Inhibitor
    ERβ agonist-2 (Page 72) is a selective ERβ agonist with an EC50 of 800 nM or lower. ERβ agonist-2 selectively inhibits T cell activation and/or proliferation, thereby reducing circulating T cell levels in subjects, without exerting significant effects on circulating neutrophil, monocyte or B cell levels. ERβ agonist-2 is applicable to studies of chronic heart failure after myocardial infarction, as well as graft-versus-host disease, multiple sclerosis and experimental autoimmune encephalomyelitis.
  • HY-180850
    ERB-2
    		Degrader
    ERB-2 is a selective ERβ PROTAC degrader. ERB-2 removes the inhibitory effect of ERβ on ROS, leading to the accumulation of ROS, mitochondrial damage, and ultimately triggering cell apoptosis (apoptosis). ERB-2 significantly inhibits tumor growth in the nude mouse model of NCI-H1975OR tumors. ERB-2 can be used for the study of non-small cell lung cancer.
  • HY-18295
    Erteberel
    		Agonist 99.88%
    Erteberel (LY500307) is a potent and selective estrogen receptor beta (ERβ) agonist with Ki and EC50 of 1.54 nM and 3.61 nM, respectively. Erteberel has anti-tumor activities.
  • HY-B1662
    Hexestrol
    		Agonist 99.79%
    Hexestrol is a nonsteroidal synthetic estrogen, with a Ki of 0.06 and 0.06 nM for estrogen receptor alpha (ERα) and ERβ. Hexestrol can be used for the research of the diseases caused by estrogen deficiencym, and it also can increase the weight of cattle.
  • HY-101271
    WAY-200070
    		Agonist 99.57%
    WAY-200070 is a selective estrogen receptor β (ERβ) agonist with an IC50 of 2.3 nM.
  • HY-149295
    PROTAC ERα Degrader-4
    		Degrader 99.06%
    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.
  • HY-125703
    Ferutinin
    		Modulator 99.23%
    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 Ca2+-ionophore that increases calcium permeability of lipid bilayer membranes, mitochondria. Ferutinin possesses estrogenic, antitumor, antibacterial and antiinflammatory activities.
  • HY-126109
    (±)-8-Prenylnaringenin
    		Modulator 99.97%
    (±)-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-N6043
    Hydroxytyrosol acetate
    		Activator 98.10%
    Hydroxytyrosol acetate is an orally active, blood-brain barrier-permeable multi-active compound with multiple effects including antibacterial, antioxidant, anti-platelet aggregation, and neuroprotective activities. Hydroxytyrosol acetate not only inhibits the growth of Vibrio by increasing bacterial membrane permeability, but also interacts with DNA and mediates supercoiled DNA relaxation. Meanwhile, Hydroxytyrosol acetate effectively reduces thrombosis and inhibits lipid oxidation by inhibiting COX activity and promoting vascular nitric oxide production. In terms of neuroprotection, Hydroxytyrosol acetate significantly alleviates neuronal apoptosis and inflammatory responses by up-regulating the expression level of ERβ, thereby improving cognitive function in Alzheimer's disease models. Hydroxytyrosol acetate has been widely used in scientific research related to Vibrio infection, arterial thrombosis, Alzheimer's disease and other related fields.
  • HY-161740
    PHTPP-1304
    		Degrader 99.96%
    PHTPP-1304 is a PHTPP-based autophagy targeting chimera (AUTOTAC). PHTPP-1304 induces the degradation of estrogen receptor ERβ through the autophagy pathway, rather than ubiquitination (DC50 ≈ 2 nM, in HEK293T cells; < 100 nM in ACHN renal carcinoma and MCF-7 breast cancer cells). PHTPP-1304 can induce the self-oligomerization of p62. PHTPP-1304 can be used to study various cancers mediated by ERβ.
  • HY-103457
    Y134
    		Antagonist 99.67%
    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.
  • HY-150693
    Estrogen receptor β antagonist 2
    		Antagonist 98.39%
    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-16023A
    Acolbifene
    		Antagonist 99.42%
    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-110157
    AC-186
    		Agonist 99.61%
    AC-186 is a selective non-steroidal estrogen receptor β (ERβ) agonist with EC50s of 6 nM and 5000 nM for ERβ and ERα, respectively. AC-186 shows gender selective neuroprotective effects in a male rat model of Parkinson's disease.
Cat. No. Product Name / Synonyms Species Source