Estrogen Receptor/ERR Inhibitor

α-Zearalenol is a Mycotoxin with high affinity for the estrogen receptors (ER), α-Zearalenol is the derivative of zearalenone (ZEN), causes reproductive disorders in animals, due to its xenoestrogenic effects.

H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with K_is 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.

Regaloside C is an anti-inflammatory agent and antioxidant that scavenges ABTS and DPPH free radicals. Regaloside C targets multiple molecules including TNF-α, MMP-2, ERα, AKT1, TLR4 and HSP90-α. Regaloside C is applicable to research related to inflammatory diseases.

2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic.

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).

BHPI is a nuclear receptor ERα inhibitor. BHPI activates PLCγ and UPR. BHPI has antitumor activity against breast, endometrial, and ovarian cancers.

3-Formylsalicylic acid is a noncompetitive estrone sulfatase inhibitor with an IC₅₀ value of 0.15 mM, a K_i value of 0.12 mM. 3-Formylsalicylic acid shows a low acute toxicity.

AZ'6421 is an orally active ERα PROTAC degrader with a DC₅₀ of 0.4 nM. AZ'6421 recruits the VHL E3 ligase to form a ternary complex, inducing proteasome-mediated polyubiquitination and degradation of ERα. AZ'6421 inhibits the growth of ER⁺ cancer cells. AZ'6421 can be used in studies related to ER⁺ breast cancer.

Isocurcumenol, an estrogen receptor alpha (ERα) inhibitor isolated from Curcuma zedoaria Rhizomes, possesses anti-tumor acticity, with IC₅₀ values of 99.1μg/mL and 178.2 μg/mL in DLA and KB cells, respectively.

PELP1-IN-1 is a PELP1 inhibitor and an apoptosis inducer with no cytotoxic activity against non-cancer cell lines. PELP1-IN-1 targets wild-type, mutant and drug-resistant ER⁺ breast cancer, and promotes PELP1 degradation through the proteasome pathway. As an analog of SMIP34 (HY-169903), PELP1-IN-1 is applicable to the research of estrogen receptor α-positive breast cancer.

2-Hydroxyestrone-d₄ is the deuterium labeled 2-Hydroxyestrone. 2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic.

Bexirestrant is an orally active ER-α degrader. Bexirestrant can be used for the research of antiestrogen, antineoplastic.

2-Ethylhexyl diphenyl phosphate is an organophosphate flame retardants (OPFRs) and a PPARG agonist (EC₂₀: 2.04 µM). 2-Ethylhexyl diphenyl phosphate also inhibits ERRγ transcriptional activity (IC₅₀: 1.3 µM). 2-Ethylhexyl diphenyl phosphate upregulates 3β-HSD1, human chorionic gonadotropin (hCG) and progesterone secretion. 2-Ethylhexyl diphenyl phosphate can be used in studies of female reproduction and fetal development.

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 ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an PROTAC estrogen-related receptor alpha (ERRa) degrader.

2-Bromoestradiol is a estrogen 2-hydroxylase inhibitor. 2-Bromoestradiol decreases irreversible binding of radiolabeled estradiol metabolite(s) to microsomal proteins.

Chrysin (Standard) is the analytical standard of Chrysin. This product is intended for research and analytical applications. Chrysin is one of the most well known estrogen blockers.

4,7-Dihydroxycoumarin is an EGFR inhibitor, estrogen receptor inhibitor, and progesterone receptor inhibitor. 4,7-Dihydroxycoumarin against breast cancer cells with an IC₅₀ velue of 18.36 μg/mL. 4,7-Dihydroxycoumarin can be used for the research of breast 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.

(E/Z)-GSK5182 is a racemic compound of (E)-GSK5182 and (Z)-GSK5182 isomers. GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC₅₀ of 79 nM. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma.