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

Estrogen Receptor/ERR Inhibitor

Estrogen Receptor/ERR Isoform Comparison

Estrogen Receptor/ERR Inhibitors (92):

Cat. No. Product Name Effect Purity
  • HY-164764
    ADX61623
    		Inhibitor 98.84%
    ADX61623 is a potent follicle stimulating hormone (FSH) receptor (FSHR) negative allosteric modulator (NAM). ADX61623 shows luteinizing hormone receptor (LH-R) activity and is not active on thyroid-stimulating hormone (TSH) receptors. ADX61623 can be used for the study of estrogen dependent disease.
  • HY-14590
    Kaempferol
    		Inhibitor 99.92%
    Kaempferol (Kempferol), a flavonoid found in many edible plants, inhibits estrogen receptor α expression in breast cancer cells and induces apoptosis in glioblastoma cells and lung cancer cells by activation of MEK-MAPK. Kaempferol can be uesd for the research of breast cancer.
  • HY-138642
    Vepdegestrant
    		Inhibitor 99.60%
    Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM.
  • HY-19822
    Elacestrant
    		Inhibitor 99.80%
    Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER+ breast cancer cell lines in vitro and in vivo.
  • HY-14589
    Chrysin
    		Inhibitor 99.85%
    Chrysin is one of the most well known estrogen blockers.
  • HY-136255
    Camizestrant
    		Inhibitor 98.04%
    Camizestrant (AZD-9833) is a potent and orally active estrogen receptor (ER) antagonist. Camizestrant is used for the study of ER+ HER2-advanced breast cancer.
  • HY-111226
    GSK5182
    		Inhibitor 99.85%
    GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM. GSK5182 does not interact with other nuclear receptors, including ERRα or ERα. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma (HCC).
  • HY-19822A
    Elacestrant dihydrochloride
    		Inhibitor 99.72%
    Elacestrant (RAD1901) dihydrochloride is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant dihydrochloride also can inhibit growth of ER+ breast cancer cell lines in vitro and in vivo.
  • HY-15449
    Kaempferide
    		Inhibitor 99.35%
    Kaempferide is an orally active flavonol isolated from Hippophae rhamnoides L. Kaempferide has anticancer, anti-inflammatory, antioxidant, antidiabetic, antiobesity, antihypertensive, and neuroprotective activities. Kaempferide induces apoptosis. Kaempferide promotes osteogenesis through antioxidants and can be used in osteoporosis research.
  • HY-N2335
    Coumestrol
    		Inhibitor 98.28%
    Coumestrol, a phytoestrogen present in soybean products, exhibits activities against cancers, neurological disorders, and autoimmune diseases. It suppresses proliferation of ES2 cells with an IC50 of 50 μM.
  • HY-B1100
    Estradiol cypionate
    		Inhibitor 99.62%
    Estradiol cypionate is the 17β-cypionate ester of Estradiol, which inhibits ET-1 synthesis by acting on estrogen receptors.
  • HY-12864
    Brilanestrant
    		Inhibitor 99.95%
    Brilanestrant (ARN-810; GDC-0810) is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM.
  • HY-128600
    ERD-308
    		Inhibitor 99.17%
    ERD-308 is a highly potent von Hippel-Lindau-based PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment. ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM in both cell lines (DC50 (concentration causing 50% of protein degradation) of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells, respectively).
  • HY-101447A
    SI-2 hydrochloride
    		Inhibitor 99.79%
    SI-2 (EPH 116 hydrochloride) is a highly promising SRC-3 inhibitor (PPI), with IC50 values of 3-20 nM for breast cancer cell death. SI-2 (EPH 116 hydrochloride) has a much improved toxicity and pharmacokinetic profile, with acceptable oral availability.
  • HY-18719B
    Endoxifen hydrochloride
    		Inhibitor 98.75%
    Endoxifen hydrochloride is a key active metabolite of Tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen hydrochloride has the potential for breast cancer study.
  • HY-112100
    PROTAC ERα Degrader-5
    		Inhibitor 98.96%
    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-139185
    PROTAC ERRα Degrader-3
    		Inhibitor 98.82%
    PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on von Hippel-Lindau ligand. PROTAC ERRα Degrader-3 is capable of specifically degrading ERRα protein by >80% at a concentration of 30 nM. PROTAC ERRα Degrader-3 is inactive against ERRβ and ERRγ proteins.
  • HY-12825
    BHPI
    		Inhibitor ≥98.0%
    BHPI is a potent inhibitor of nuclear estrogen–ERα-regulated gene expression; elicits sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis.
  • HY-18719
    Endoxifen (Z-isomer)
    		Inhibitor 99.20%
    Endoxifen Z-isomer is the most important Tamoxifen metabolite, inducing an anti-estrogenic effect in breast cancer cells expressing ERα. Endoxifen Z-isomer inhibits hERG. This effect is concentration-dependent, with an IC50 value of 1.6 μM.
  • HY-112611
    H3B-5942
    		Inhibitor 99.73%
    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 ERαWT or ERα mutations.