Search Result
| Isoforms Recommended: |
ERα
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Results for "
ERα
" in MedChemExpress (MCE) Product Catalog:
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- HY-A0036
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TSE-424 acetate
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Estrogen Receptor/ERR
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Cancer
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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 .
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- HY-A0031
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TSE-424
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Estrogen Receptor/ERR
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Neurological Disease
Cancer
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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 .
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- HY-100689
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PPT
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Estrogen Receptor/ERR
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Cancer
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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%) .
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- HY-B0412
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Estriol
5 Publications Verification
Oestriol
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Estrogen Receptor/ERR
Endogenous Metabolite
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Cancer
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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 .
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- HY-150505
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Deubiquitinase
Apoptosis
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Cancer
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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 .
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- HY-153468
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TEQ103; Sera2
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Sodium Channel
TRP Channel
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Cancer
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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 .
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- HY-112100
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PROTAC-Linker Conjugates for PAC
Estrogen Receptor/ERR
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Cancer
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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) .
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- HY-162312
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Deubiquitinase
Apoptosis
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Cancer
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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 .
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- HY-111846
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PROTACs
Estrogen Receptor/ERR
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Cancer
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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)) .
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- HY-112611
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Estrogen Receptor/ERR
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Cancer
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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 .
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- HY-W036120
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2,2′,4,4′-Tetrahydroxybenzophenone
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Environmental Pollutants
Glycosidase
Estrogen Receptor/ERR
Pregnane X Receptor (PXR)
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Metabolic Disease
Endocrinology
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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 .
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- HY-126109
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Estrogen Receptor/ERR
Apoptosis
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Metabolic Disease
Endocrinology
Cancer
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(±)-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 .
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- HY-16023A
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EM-652; SCH 57068
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Estrogen Receptor/ERR
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Cancer
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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 .
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- HY-103457
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Estrogen Receptor/ERR
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Cancer
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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 .
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- HY-125703
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Estrogen Receptor/ERR
Apoptosis
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Infection
Inflammation/Immunology
Endocrinology
Cancer
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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 .
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- HY-108414
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- HY-149295
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PROTACs
Estrogen Receptor/ERR
Apoptosis
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Cancer
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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.
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- HY-112098
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PROTACs
Estrogen Receptor/ERR
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Cancer
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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.
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- HY-137144
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ZB716
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Estrogen Receptor/ERR
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Cancer
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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 .
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- HY-W088749
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PROTAC Linkers
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Cancer
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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) .
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- HY-W1006471
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- HY-145341
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Estrogen Receptor/ERR
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Cancer
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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 .
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- HY-177445
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Histone Acetyltransferase
Estrogen Receptor/ERR
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Cancer
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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) .
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- HY-176364
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- HY-A0031A
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TSE-424 hydrochloride
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Estrogen Receptor/ERR
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Cancer
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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 .
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- HY-129619
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SNIPERs
Estrogen Receptor/ERR
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Cancer
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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 .
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- HY-W1005067
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Molecular Glues
Hippo (MST)
Estrogen Receptor/ERR
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Others
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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 .
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- HY-A0036R
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TSE-424 acetate (Standard)
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Reference Standards
Estrogen Receptor/ERR
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Cancer
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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 .
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- HY-178961
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PROTACs
Estrogen Receptor/ERR
Apoptosis
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Cancer
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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 .
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- HY-174870
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PROTACs
Estrogen Receptor/ERR
Apoptosis
Fluorescent Dye
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Cancer
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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)) .
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- HY-174453
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PROTACs
Estrogen Receptor/ERR
Apoptosis
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Cancer
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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)) .
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- HY-145556
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Estrogen Receptor/ERR
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Cancer
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Bexirestrant is an orally active ER-α degrader. Bexirestrant can be used for the research of antiestrogen, antineoplastic .
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- HY-144733
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Estrogen Receptor/ERR
Apoptosis
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Cancer
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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 .
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- HY-175872
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Estrogen Receptor/ERR
Molecular Glues
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Others
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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 .
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- HY-W114419
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Estrogen Receptor/ERR
mTOR
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Cardiovascular Disease
Metabolic Disease
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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 .
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- HY-125263
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Estrogen Receptor/ERR
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Cancer
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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.
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- HY-175448
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PROTACs
Estrogen Receptor/ERR
IAP
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Cancer
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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)) .
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- HY-168205
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HSP
Apoptosis
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Cancer
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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 .
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- HY-16023
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EM-652 hydrochloride; SCH 57068 hydrochloride
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Estrogen Receptor/ERR
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Cancer
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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 .
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- HY-W998310
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(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 .
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- HY-176955
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Estrogen Receptor/ERR
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Cancer
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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 .
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- HY-175171
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Topoisomerase
VEGFR
c-Met/HGFR
EGFR
Estrogen Receptor/ERR
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Cancer
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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 .
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- HY-168869
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PROTACs
Estrogen Receptor/ERR
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Cancer
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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))
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- HY-131404
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TPBM
2 Publications Verification
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Estrogen Receptor/ERR
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Cancer
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TPBM is a potent estrogen receptor α (ERα) inhibitor with an IC50 value of 9 μM for 17β-estradiol (E2)-ERα. TPBM reduces E2·ERα 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 .
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- HY-126932
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Estrogen Receptor/ERR
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Cancer
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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 .
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- HY-132294A
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Estrogen Receptor/ERR
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Cancer
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(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 .
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- HY-179045
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Estrogen Receptor/ERR
Apoptosis
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Cancer
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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 .
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- HY-132194
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Estrogen Receptor/ERR
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Cancer
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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 .
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- HY-169941
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Estrogen Receptor/ERR
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Metabolic Disease
Cancer
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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 .
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- HY-156125
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Estrogen Receptor/ERR
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Others
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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 .
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- HY-155492
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Estrogen Receptor/ERR
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Cancer
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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 .
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- HY-144306
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Estrogen Receptor/ERR
Apoptosis
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Cancer
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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 .
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- HY-157765
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PROTACs
Estrogen Receptor/ERR
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Cancer
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PROTAC ERα Degrader-6 (compound A2) is a potent PROTAC degrader of ERα, with IC50 of 0.11 μM in MCE-7 cells. 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 .
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- HY-163680
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Estrogen Receptor/ERR
Cytochrome P450
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Cancer
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ERα degrader 9 is a dual targeting ligand for estrogen receptor α (ERα) and aromatase (ARO). ERα degrader 9 can be utilized for synthesis of PROTAC ERα Degrader-9 (HY-163679) .
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- HY-149081
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Estrogen Receptor/ERR
Cytochrome P450
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Cancer
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ERα degrader 6 (Compound 31q) is an ERα degrader (KI: 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 .
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- HY-146267
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Estrogen Receptor/ERR
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Cancer
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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 .
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- HY-172937
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Estrogen Receptor/ERR
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Cancer
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ERα degrader 13 (compound MR3) is potent ERα degrader with an IC50 of 0.55 μM. ERα degrader 13 induces an obvious tumor regression in the breast cancer xenograft mouse model .
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- HY-160562
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PROTACs
Estrogen Receptor/ERR
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Cancer
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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 .
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- HY-179232
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Estrogen Receptor/ERR
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Cancer
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ERα antagonist 2 (Compound 5b) is an ER-α antagonist with an IC50 value of 1729 nM. ERα antagonist 2 exhibits significant inhibitory activity against breast cancer cell lines, and is still effective against ER-negative cells (MDA-MB-231), suggesting the existence of ER-independent pathways. ERα antagonist 2 can be used for the study of breast cancer .
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- HY-160563
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- HY-163679
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Estrogen Receptor/ERR
Cytochrome P450
PROTACs
Apoptosis
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Cancer
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PROTAC ERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader, which degrades estrogen receptor α (ERα) and aromatase (ARO). PROTAC ERα Degrader-9 binds to ERα with a Ki of 0.25 μM, inhibits ARO with an IC50 of 4.6 μM. PROTAC ERα Degrader-9 inhibits the proliferation of MCF-7 wildtype (IC50=0.54 μM) and ERα mutants MCF-7 EGFR (IC50=0.075 μM), MCF-7 D538G (IC50=0.31 μM), MCF-7 Y537S (IC50=2.3 μM), downregulates the expressions of ERS1 and MYC. PROTAC ERα Degrader-9 arrests the cell cycle at G2/M, induces apoptosis in MCF-7. PROTAC ERα Degrader-9 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-163680); Black: linker (HY-W007559); Blue: ligand for E3 ligase (HY-112078))
|
-
- HY-161692
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERα degrader 8 (Compound 18j) is a selective Estrogen Receptor degrader. ERα degrader 8 is degrader to MCF-7 cells with IC50 value of 0.15 μM .
|
-
- HY-145071
-
|
|
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-170336
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERα Degrader-10 (Compound 160a) is an orally active degrader for ERα with DC50 of 0.37-1.1 nM, in cells MCF7, T47D and CAMA-1. PROTAC ERα Degrader-10 exhibits antitumor efficacy in mouse model . (Pink: ligand for target protein (HY-170339); Black: linker (HY-30105); Blue: ligand for E3 ligase Cereblon (HY-168055))
|
-
- HY-111845
-
-
- HY-174475
-
-
- HY-174131
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
PVTX-321 (Compound 16a) is an orally active estrogen receptor α (ERα) degrader. PVTX-321 can potently degrade ERα (DC50=0.15 nM in MCF-7 cells) and also has inhibitory activity against mutant ERα (IC50=59 nM). PVTX-321 is promising for research of ER+/HER2- breast cancer .
|
-
- HY-P10393
-
|
ERα (295-311)
|
Apoptosis
|
Cancer
|
|
ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
|
-
- HY-144070A
-
|
|
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-144314
-
|
|
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-125263B
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
(R)-OP-1074 is an isomer of OP-1074 (HY-125263) and can serve as a control compound in experiments. 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.
|
-
- HY-144138
-
|
|
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-144137
-
|
|
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-178463
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
F0840-0093 is a highly selective estrogen receptor α (ERα) degrader. F0840-0093 exhibits potent antiproliferative activity against T47D cells with an IC50 value of 4.65 μM. F0840-0093 is promising for research of estrogen receptor-positive (ER+) breast cancer .
|
-
- HY-164924
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
ERD-12310A is a PROTAC targeting Estrogen Receptor α (ERα) with a ED50 value of 47 pM. ERD-12310A has oral activity. ERD-12310A is composed of PROTAC target protein ligand ER ligand-4 (HY-164925) (red part), E3 ligase ligand (S)-Deoxy-thalidomide (HY-168055) (blue part). ERD-12310A can be used in the research of ER + breast cancer .
|
-
- HY-123773
-
|
NSC 732011; HLX-801
|
Steroid Sulfatase
Estrogen Receptor/ERR
|
Cancer
|
|
SR-16157 (NSC 732011; HLX-801) is a dual-action steroid sulfatase (STS) inhibitor (IC50 = 0.1 uM) and selective ERα modulator. SR-16157 exhibits STS inhibitory and anti-estrogenic effects in breast cancer cells. SR-16157 may be used in breast cancer research .
|
-
- HY-B0723S
-
|
FC-1271a-d4
|
Isotope-Labeled Compounds
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 .
|
-
- HY-103451
-
|
|
Estrogen Receptor/ERR
|
Metabolic Disease
|
|
(R,R)-THC is an ERα agonist and an ERβ antagonist, with Kis of 9.0 nM and 3.6 nM for ERα and ERβ, respectively. (R,R)-THC has higher relative binding affinity for ERβ than ERα with the values of 25 and 3.6 .
|
-
- HY-A0031R
-
|
TSE-424 (Standard)
|
Reference Standards
Estrogen Receptor/ERR
|
Cancer
|
|
Bazedoxifene (Standard) is the analytical standard of Bazedoxifene. This product is intended for research and analytical applications. 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 .
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-
- HY-103451A
-
|
|
Estrogen Receptor/ERR
|
Metabolic Disease
|
|
rel-(R,R)-THC is the relative configuration of (R,R)-THC (HY-103451). (R,R)-THC is an ERα agonist and an ERβ antagonist, with Kis of 9.0 nM and 3.6 nM for ERα and ERβ, respectively. (R,R)-THC has higher relative binding affinity for ERβ than ERα with the values of 25 and 3.6 .
|
-
- HY-100689R
-
|
PPT (Standard)
|
Reference Standards
Estrogen Receptor/ERR
|
Cancer
|
|
Propyl pyrazole triol (Standard) is the analytical standard of Propyl pyrazole triol. This product is intended for research and analytical applications. 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%) .
|
-
- HY-168099
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERα degrader 10 is a selective and orally active estrogen receptor α (ERα) degrader. ERα degrader 10 exhibits potent ERα binding affinity (IC50 of 24.0 nM) and degradation ability (EC50 of 5.3 nM). ERα degrader 10 degrades ERα through the proteasome-mediated pathway. ERα degrader 10 can be used for the study of breast cancer .
|
-
- HY-170806
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERα degrader 12 (Compound RA3) is an estrogen receptor α (ERα) degrader with antitumor properties. ERα degrader 12 induces pronounced tumor growth inhibition in a breast cancer xenograft mouse model .
|
-
- HY-163467
-
-
- HY-146424
-
-
- HY-168101
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERα degrader 11 (compound B16) is a selective ERα degrader that can be used as an estrogen receptor probe to investigate ER status in ER-positive breast cancer cells .
|
-
- HY-179597
-
-
- HY-W749028
-
-
- HY-168644
-
-
- HY-179510
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
CDD-1274 is an ERα (Estrogen receptor α) variant inhibitor. CDD-1274 induces proteasomal degradation of ERα variants in breast cancer cell lines and causes Y537S ERα degradation. CDD-1274 potently blocks ligand-dependent and ligand-independent ER signaling in endocrine-resistant breast cancer cells. CDD-1274 can be used for the study of breast cancer .
|
-
- HY-P991578
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
SNG-8023 is an anti-ERα humanized monoclonal antibody. SNG-8023 can be used for cancer research, such as breast cancer .
|
-
- HY-181171
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
HIT-2 is an estrogen receptor alpha (ERα) inhibitor that can bind to the ERα ligand binding domain. HIT-2 forms stable interactions including hydrogen bonds, π-π stacking, and hydrophobic contacts to disrupt ERα-driven signaling. HIT-2 exhibits antineoplastic activity against breast cancer. HIT-2 can be used for the research of breast cancer .
|
-
- HY-124627
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
THIQ-40 is a tetrahydroisoquinoline-based, orally active, and selective estrogen receptor ERα degrader (SERD) (IC50=17 nM), with antitumor efficacy. THIQ-40 possesses functional ERα antagonistic activity, promotes ERα degradation and forms stable ERαLBD complexes. THIQ-40 shows the characteristic of rapid racemization in multi-species plasma. THIQ-40 can be widely applied to studies on the relevant mechanisms and drug development of ERα-positive breast cancer .
|
-
- HY-181345
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
OP-1690 is a complete estrogen receptor (ERα) antagonist (CERAN), with pIC50 values of 7.5 and 7.9 in alkaline phosphatase (AP) activity assay and TR-FRET assay, respectively. OP-1690 modulates receptor function by inducing ERα tetramerization, effectively induces ERα degradation, inhibits target gene transcription, but exhibits low antiproliferative potency. OP-1690 can be used for breast cancer research .
|
-
- HY-125675
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
VPC-16606 is a selective inhibitor targeting the activation function 2 (AF2) domain of estrogen receptor α (ERα). VPC-16606 blocks the interaction between ERα and coactivators, inhibits the activity of both wild-type and clinically drug-resistant mutant ERα, and exerts inhibitory effects on hormone-resistant breast cancer cells. VPC-16606 can be used in breast cancer research .
|
-
- HY-180959
-
-
- HY-179576
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Others
|
|
CV2a is a 14-3-3-directed molecular glue-based PROTAC that selectively targets the ERα protein complex with an EC50 of 0.10 μM. CV2a cooperatively recruits VHL to the 14-3-3/ERα complex and promotes robust polyubiquitination of the 14-3-3ζ/ERα complex .
|
-
- HY-181172
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
FRAGHIT-4 is an estrogen receptor alpha (ERα) inhibitor. FRAGHIT-4 exhibits antineoplastic activity against breast cancer via targeting ER signaling. FRAGHIT-4 can be used for the research of breast cancer .
|
-
- HY-43322
-
|
|
17β-HSD
|
Cancer
|
|
7-Coumaryl triflate is a type 17β-HSD1 inhibitor of 17β-hydroxysteroid dehydrogenase. Its IC50 is 360 nM and Ki is 173 nM. 7-Coumaryl triflate shows selectivity for 17β-HSD2 and has no detectable affinity for ERα or ERβ. 7-Coumaryl triflate can be used in related research on hormone-dependent breast cancer .
|
-
- HY-175445
-
|
|
PROTACs
Estrogen Receptor/ERR
IAP
NF-κB
TNF Receptor
Apoptosis
|
Cancer
|
|
GNE-5472 is a potent bifunctional ERα PRRTAC degrader, with its E3 ligand being a pan-IAP antagonist. GNE-5472 antagonizes cIAP1/2, activating the non-classical NF-κB pathway, resulting in a significant upregulation of TNFα expression. GNE-5472 inhibits the proliferation of breast cancer cells and induces cell apoptosis. GNE-5472 can be used for the study of breast cancer .
|
-
- HY-103456
-
PHTPP
Maximum Cited Publications
30 Publications Verification
|
Estrogen Receptor/ERR
|
Cancer
|
|
PHTPP is a selective estrogen receptor β (ERβ) antagonist with 36-fold selectivity over ERα .
|
-
- HY-183187
-
|
|
Estrogen Receptor/ERR
COX
|
Cancer
|
|
4H-Chromen-4-one-o-carborane is an estrogen receptor (ER) agonist, with an EC50 of 0.9 μM for ERα and an EC50 of 11.1 μM for ERβ. 4H-Chromen-4-one-o-carborane also acts as an inhibitor of COX-1 and COX-2, with an IC50 of 6.6 μM for COX-1 and an IC50 of 17.7 μM for COX-2 .
|
-
- HY-175785
-
|
|
Estrogen Receptor/ERR
Aryl Hydrocarbon Receptor
Apoptosis
MDM-2/p53
|
Cancer
|
|
X15695 is selective and orally active estrogen receptor (ERα) degrader. X15695 is an aryl hydrocarbon receptor (AHR) ligand. X15695 enables AHR to form a complex with the ERα, promoting its proteasomal degradation. X15695 inhibits the breast cancer cells proliferation, promotes cell cycle block and induces apoptosis. X15695 can be used for the study of breast cancer .
|
-
- HY-103453
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
(R)-DPN (compound 3) is a selective ERβ ligand with EC50s of 2.9, 0.8 nM for ERα and ERβ, respectively. (R)-DPN shows a very high affinity and potency preference for ERβ over ERα. (R)-DPN shows cytoxicity for HEC-1 and U2OS cells with EC50s of 286, 205 nM, respectively .
|
-
- HY-N2448
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Lindleyin, isolated from Rhei rhizoma, mediates hormonal effects through estrogen receptors. Lindleyin binds to ERα with estrogenic activity .
|
-
- HY-123664
-
|
LY133314
|
Estrogen Receptor/ERR
|
Cancer
|
|
Trioxifene mesylate (LY133314) 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 mesylate binds estradiol receptors, inhibits ERα-mediated gene expression, reduces circulating gonadotrophin levels. Trioxifene mesylate can be used for the research of advanced breast cancer and androgen-independent, metastatic prostatic adenocarcinoma .
|
-
- HY-119418
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Desketoraloxifene is an estrogen receptors alpha (ERα) activator at an AP-1 site. Desketoraloxifene can be used for the research of osteoporosis and breast cancer .
|
-
- HY-138089
-
|
|
Androgen Receptor
Estrogen Receptor/ERR
LDLR
|
Metabolic Disease
Cancer
|
|
17β-Hydroxy exemestane (17-H-EXE) is the primary active metabolite of Exemestane (HY-13632). 17β-Hydroxy exemestane is an aromatase inhibitor (IC50 = 69 nM) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). 17β-Hydroxy exemestane stimulates growth of AR- and ERα-positive MCF-7 (EC50= 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7 cells. 17β-Hydroxy exemestane inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae in ovariectomized rats .
|
-
- HY-183804
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ER Degrader-16 is an orally active ERα PROTAC degrader with a DC50 of 1.4 nM and an IC50 of 1.9 nM. PROTAC ER Degrader-16 inhibits ER-dependent breast cancer cell proliferation and exerts anti-tumor effects in mouse models. PROTAC ER Degrader-16 can be used for breast cancer research .
|
-
- HY-135529
-
|
LY133314 free base
|
Estrogen Receptor/ERR
|
Cancer
|
|
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-167701
-
|
|
Ligands for Target Protein for PROTAC
Apoptosis
Estrogen Receptor/ERR
|
Cancer
|
|
OBHSA is a selective estrogen receptor (ERα) degrader. OBHSA blocks the cell cycle by degrading cyclin D1, thereby overcoming Tamoxifen (HY-13757A) resistance. OBHSA also triggers excessive activation of the unfolded protein response (UPR) by inducing an increase in intracellular reactive oxygen species, ultimately leading to cell apoptosis. In addition, OBHSA can also be used as an ERα ligand to synthesize PROTAC degraders .
|
-
- HY-150803
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
VHL Ligand 14 (Compound 11) is a VHL ligand for design of PROTAC estrogen receptor α (ERα) degraders, with a binding affinity IC50 of 196 nM .
|
-
- HY-177389
-
-
- HY-100583A
-
-
- HY-12870
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
AZD9496 is an effective, selective estrogen receptor (ERα) antagonist with an IC50 of 0.28 nM. AZD9496 is an orally active, selective estrogen receptor degrader (SERD).
|
-
- HY-12870A
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC50 of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD).
|
-
- HY-12825
-
-
- HY-43962
-
-
- HY-114770
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
(E,E)-GLL398 is a selective estrogen receptor degrader with potent binding activity to ERα (IC50 = 1.14 nM). (E,E)-GLL398 can effectively degrade ERα in MCF-7 breast cancer cells (IC50 = 0.21 μM). The introduced boronic acid group of (E,E)-GLL398 gives it superior oral bioavailability, with an AUC of 36.9 μg·h/mL in rats, which is significantly higher than that of GW7604 .
|
-
- HY-N0233
-
Bavachin
Maximum Cited Publications
12 Publications Verification
Corylifolin
|
Estrogen Receptor/ERR
|
Cancer
|
|
Bavachin, a flavonoid first isolated from seeds of P. corylifolia, acts as a phytoestrogen that activates the estrogen receptors ERα and ERβ with EC50s of 320 and 680 nM, respectively.
|
-
- HY-111061
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
GTX-758 is an orally active, nonsteroidal, selective agonist of ERα. GTX-758 plays an important role in castration resistant prostate cancer (CRPC) research .
|
-
- HY-150601
-
-
- HY-176225
-
|
|
PROTACs
Src
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
BY13 is a SRC-3 PROTAC degrader with a DC50 of 0.031 μM. BY13 selectively blocks the ER signaling pathway over that of androgen receptor (AR)) through down-regulating ERα level. BY13 potently overcomes endocrine resistance in breast cancer by inducing cell cycle arrest in G1 phase and apoptosis, with superior effect over Fulvestrant (HY-13636). BY13 significantly inhibits the growth of drug-resistant breast tumors without obvious toxicity in LCC2 xenograft mice model . Pink: SRC-3 ligand (SI-2) (HY-101447); Blue: CRBN ligase ligand (HY-41547); Black: linker (HY-176226)
|
-
- HY-170339
-
-
- HY-N15342
-
|
|
Estrogen Receptor/ERR
|
Metabolic Disease
Endocrinology
|
|
Tschimganidin is an ERα agonist with an IC50 of 1.4 μM. Found in plants of the Apiaceae family, Tschimganidin is a terpenoid compound with anti-obesity activity. It can be used for research in the field of endocrine and metabolic disorders .
|
-
- HY-103456R
-
|
|
Reference Standards
Estrogen Receptor/ERR
|
Cancer
|
|
PHTPP (Standard) is the analytical standard of PHTPP. This product is intended for research and analytical applications. PHTPP is a selective estrogen receptor β (ERβ) antagonist with 36-fold selectivity over ERα .
|
-
- HY-108414R
-
|
(+)-Equol (Standard)
|
Estrogen Receptor/ERR
Reference Standards
|
Cancer
|
|
(R)-Equol (Standard) is the analytical standard of (R)-Equol. This product is intended for research and analytical applications. (R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively.
|
-
- HY-111484A
-
|
SRN-927 Racemate
|
Estrogen Receptor/ERR
|
Cancer
|
|
GDC-0927 Racemate (SRN-927 Racemate) is an estrogen receptor (ER) degrader that can effectively inhibit the activity of ER-α with an IC50 value of 0.2 nM and can be used in diseases related to estrogen receptors.
|
-
- HY-150693
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
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-19822B
-
|
RAD1901 S enantiomer dihydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
|
Elacestrant S enantiomer dihydrochloride (RAD1901 S enantiomer dihydrochloride) is an low activity enantiomer of elacestrant dihydrochloride. Elacestrant (RAD1901) dihydrochloride is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.
|
-
- HY-103446
-
-
- HY-W615671
-
|
|
Estrogen Receptor/ERR
|
Others
|
|
4,4'-(Cyclohexylidenemethylene)diphenol (Compound 2) is a symmetric cyclic nonsteroidal estrogen. 4,4'-(Cyclohexylidenemethylene)diphenol has high binding affinity for estrogen receptors ERα and ERβ .
|
-
- HY-132247
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ErSO is a selective anticipatory unfolded protein response (a-UPR) activator. ErSO acts through ERα to elicit strong and sustained cytotoxic activation of the a-UPR. ErSO can be used for the research of cancer .
|
-
- HY-19822D
-
|
RAD1901 S enantiomer
|
Estrogen Receptor/ERR
|
Cancer
|
|
Elacestrant S enantiomer (RAD1901 S enantiomer) is an low activity enantiomer of elacestrant. Elacestrant (RAD1901) is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively .
|
-
- HY-19498
-
|
SIM-688
|
NF-κB
|
Inflammation/Immunology
|
|
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-19822S1
-
|
RAD1901-d4-1
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
|
|
Elacestrant-d4-1 is the deuterium labeled Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively .
|
-
- HY-N4121
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
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 .
|
-
- HY-15483
-
DY131
3 Publications Verification
GSK 9089
|
Estrogen Receptor/ERR
Smo
|
Endocrinology
Cancer
|
|
DY131 (GSK 9089) is a potent and selective ERRγ and ERRβ agonist. DY131displays inactive against ERRα, ERα and ERβ . DY131 also inhibits Smo signaling .
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-
- HY-155196
-
|
|
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 .
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-
- HY-176486
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ER degrader 11 (Compound 5) is an orally active, brain-penetrant and selective estrogen receptor (ER) degrader (ERα IC50=1.6 nM). ER degrader 11 is promising for research of breast cancer brain metastasis .
|
-
- HY-100583AR
-
-
- HY-B1662
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
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-N7748A
-
-
- HY-N0233R
-
|
Corylifolin (Standard)
|
Reference Standards
Estrogen Receptor/ERR
|
Cancer
|
|
Bavachin (Standard) is the analytical standard of Bavachin. This product is intended for research and analytical applications. Bavachin, a flavonoid first isolated from seeds of P. corylifolia, acts as a phytoestrogen that activates the estrogen receptors ERα and ERβ with EC50s of 320 and 680 nM, respectively.
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-
- HY-19822
-
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RAD1901
|
Estrogen Receptor/ERR
|
Cancer
|
|
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 .
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-
- HY-19822A
-
|
RAD1901 dihydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
|
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 .
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-
- HY-182498
-
|
|
Cytochrome P450
Estrogen Receptor/ERR
|
Cancer
|
|
(Z)-Norendoxifen is an aromatase inhibitor and estrogen receptor modulator. The IC50 value of (Z)-Norendoxifen against aromatase is 102 nM. The EC50 values of (Z)-Norendoxifen for ER-α and ER-β are 27.0 nM and 35.2 nM, respectively. (Z)-Norendoxifen can be used in breast cancer research .
|
-
- HY-110157
-
|
|
Estrogen Receptor/ERR
|
Neurological Disease
|
|
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 .
|
-
- HY-A0036D
-
|
TSE-424 acetate-D
|
Estrogen Receptor/ERR
|
Cancer
|
|
Bazedoxifene (acetate)-D (TSE-424 (acetate)-D) is the D-crystal form compound of Bazedoxifene acetate (HY-A0036). Bazedoxifene acetate is an orally active, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively .
|
-
- HY-128527
-
|
|
PROTAC-Linker Conjugates for PAC
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ER Degrader-3 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab) .
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-
- HY-164726
-
|
|
Estrogen Receptor/ERR
|
Others
|
|
Estrogen receptor modulator 11 (Compound 27) is a tetrahydroisoquinoline derivative. Estrogen receptor modulator 11 has a certain affinity for estrogen receptors (ER), with IC50 values of 285 nM and 421 nM for ERα and ERβ, respectively. Estrogen receptor modulator 11 lacks antagonist activity in the MCF-7 cellular assay .
|
-
- HY-128528
-
|
|
PROTAC-Linker Conjugates for PAC
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ER Degrader-2 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab) .
|
-
- HY-19822S2
-
|
RAD1901-d10
|
Estrogen Receptor/ERR
Isotope-Labeled Compounds
|
Cancer
|
|
Elacestrant-d10 is the deuterium labeled of Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also inhibits growth of ER + breast cancer cell lines in vitro and in vivo .
|
-
- HY-10426
-
|
|
Estrogen Receptor/ERR
Autophagy
|
Cancer
|
|
XCT-790 is a potent and selective inverse agonist for ERRα with an IC50 value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ .
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-
- HY-B1662R
-
|
|
Reference Standards
Estrogen Receptor/ERR
|
Endocrinology
|
|
Hexestrol (Standard) is the analytical standard of Hexestrol. This product is intended for research and analytical applications. 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-135590
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
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-175444
-
|
|
E3 Ligase Ligand-Linker Conjugates
IAP
|
Cancer
|
|
XIAP ligand-Linker Conjugate 1 is an E3 ligase ligand-linker conjugate that incorporates the XIAP BIR2 ligand XB2M54 (HY-175348) and linker. XIAP ligand-Linker Conjugate 1 can be used for synthesis of PROTAC ERα Degrader-1 (HY-112098) .
|
-
- HY-111226
-
-
- HY-N7627
-
-
- HY-B1662S3
-
|
|
Isotope-Labeled Compounds
MEK
Autophagy
Apoptosis
|
Cancer
|
|
Hexestrol-d4 is the deuterium labeled Hexestrol (HY-B1662). 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-B0723S2
-
|
FC-1271a-d5
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
|
|
Ospemifene-d5 (FC-1271a-d5) is deuterium labeled Ospemifene. Ospemifene is a non-estrogen selective estrogen receptor modulator (SERM), with Kis of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene can be used for the research of vaginal atrophy and breast cancer .
|
-
- HY-175348
-
-
- HY-P10843
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
R4K1 is a cell-permeable stapled peptide. R4K1 binds to the estrogen receptor (ER) α with high affinity and inhibits its interaction with coactivators. R4K1 can enter breast cancer cells to regulate gene transcription and inhibit cell proliferation. R4K1 can be used in the study of cancer .
|
-
- HY-163766
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Antiproliferative agent-51 (Compound 18h) exhibits inhibitory efficacy against estrogen receptor α (ERα) mediated transcription, with an IC50 of 1.6 nM. Antiproliferative agent-51 inhibits the proliferation of cancer cell ZR-75, with an IC50 of 0.031 μM. Antiproliferative agent-51 exhibits antitumor efficacy in mouse models .
|
-
- HY-149480
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer .
|
-
- HY-144070
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ErSO-DFP is an anticipatory unfolded protein response (a-UPR) activator. ErSO-DFP has enhanced selectivity for estrogen receptor alpha-positive (ERα+) cancer cells with a wider selectivity window than ErSO (HY-132247). ErSO-DFP displays antitumor activity against MCF-7 in mice. ErSO-DFP can cross the blood brain barrier .
|
-
- HY-135584
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
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-179433
-
|
|
PROTACs
Androgen Receptor
Estrogen Receptor/ERR
Src
|
Cancer
|
|
PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS). PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer .
|
-
- HY-159957
-
|
|
Histone Acetyltransferase
Estrogen Receptor/ERR
|
|
|
BAY-184 is a selective and orally active KAT6A and KAT6B inhibitor. BAY-184 inhibits KAT6A/KAT6B activity with an IC50 of 71 nM and 83 nM. respectively BAY-184 inhibits ERα transcriptional activity. BAY-184 inhibits proliferation of diverse breast cancer subtypes, and inhibits tumor growth .
|
-
- HY-19822S3
-
|
RAD1901-d6
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
|
|
Elacestrant-d6 (RAD1901-d6) is a deuterated labeled Elacestrant (HY-19822). Elacestrant is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
|
-
- HY-18719S
-
-
- HY-121372
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
Lactandrate is a D-high nitrogen steroid alkylating agent. It can interact with the ligand-binding domain (LBD) of estrogen receptor-alpha (ERα). Lactandrate has a growth inhibitory effect on breast cancer cells, with a GI50 value ranging from 5 to 65 μM. It shows anti-tumor activity in mouse breast tumors (MXT and CD8F1) as well as in human xenograft MX-1 .
|
-
- HY-174880
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
CRBN ligand-8-O-C6-NH2 is an E3 ligase ligand-linker conjugate that incorporates a CRBN ligand (HY-150831) and a linker. CRBN ligand-8-O-C6-NH2 can be used for synthesis of PROTAC ERα Degrader-11 (HY-174870) .
|
-
- HY-19822S
-
|
RAD1901-d4
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
|
|
Elacestrant-d4 (RAD1901-d4) is a deuterated labeled Elacestrant (HY-19822). Elacestrant (RAD1901) is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
|
-
- HY-B0141E
-
|
ent-β-Estradiol; ent-17β-Estradiol; ent-17β-Oestradiol
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Ent-Estradiol is the enantiomer of Estradiol (HY-B0141). Ent-Estradiol is a highly selective estrogen receptor ligand, but does not possess estrogenic activity. Ent-Estradiol displays IC50 values of 24.9 nM, 9.59 nM and 8.17 nM for human, rat and mouse ERβ, and 151 nM, 246 nM and 268 nM for human, rat and mouse ERα, respectively. Ent-Estradiol can be used for the study of menopausal physiological changes .
|
-
- HY-103450
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
|
G-36 is a cell-permeable nonsteroidal antagonist of the G protein-coupled estrogen receptor (GPER/GPR30), which selectively inhibits estrogen-mediated PI3K activation through GPER, rather than Erα. G-36 also inhibits estrogen-mediated calcium mobilization (IC50=112 nM). G-36 is promising for research in the field of cancer .
|
-
- HY-125091
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
LY2066948 is a selective and orally active estrogen receptor modulator (SERM). LY2066948 has high affinity for estrogen receptors ERα and ERβ (Ki: 0.51 and 1.36 nM respectively) and shows potent antiestrogenic activity. LY2066948 blocks uterine weight gain induced by Ethynyl estradiol (HY-B0216) in immature rats. LY2066948 can be used for research of uterine fibroids and myomas .
|
-
- HY-107835
-
|
FCR 2769
|
Environmental Pollutants
Apoptosis
Bcl-2 Family
Parasite
Insecticide
|
Infection
Cancer
|
|
Flumethrin (FCR 2769) is a pyrethroid insecticide and acaricide . Flumethrin targets voltage-gated sodium channels and estrogen receptor α (ERα). Flumethrin induces cytotoxicity, apoptosis, genotoxicity and DNA damage in breast cancer cells by regulating the expression of BCL2, BAX, TP53 and P21 genes. Flumethrin is applicable to relevant studies on ectoparasite infections (tick and flea burdens) in dogs and cats, as well as breast cancer .
|
-
- HY-103454
-
|
|
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-127133
-
|
MPP
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Methylpiperidino pyrazole (MPP) is a potent and selective ER (estrogen receptor) modulator. Methylpiperidino pyrazole induces significant apoptosis in the endometrial cancer and oLE cell lines. Methylpiperidino pyrazole reverses the the positive effects of beta-estradiol. Methylpiperidino pyrazole has mixed agonist/antagonist action on murine uterine ERalpha in vivo .
|
-
- HY-103454R
-
|
|
Reference Standards
Estrogen Receptor/ERR
Apoptosis
|
Endocrinology
Cancer
|
|
MPP dihydrochloride (Standard) is the analytical standard of MPP dihydrochloride (HY-103454). This product is intended for research and analytical applications. 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-15731
-
|
|
Estrogen Receptor/ERR
Endogenous Metabolite
NO Synthase
|
Cardiovascular Disease
Cancer
|
|
Estetrol, an orally active estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol binds ERα as well as ERβ (with a fourfold lower affinity). Estetrol increases eNOS expression/activity and NO synthesis in endothelial cells. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast. Estetrol can be used in contraception and menopausal hormone research .
|
-
- HY-170382
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
ER covalent antagonist-1 (Compound 39D) is the antagonist for estrogen receptor α (ERα). ER covalent antagonist-1 inhibits the proliferation of ERα-positive cell MCF-7 with an IC50 of 0.98 μM, arrests the cell cycle at G0/G1 phase, and induces apoptosis. ER covalent antagonist-1 exhibits antitumor efficacy in mouse model .
|
-
- HY-N0401A
-
|
|
Bacterial
Estrogen Receptor/ERR
FATP
|
Infection
Metabolic Disease
Cancer
|
|
(Z)-Ligustilide is extracted from Ligusticum chuanxiong Hort, has antimicrobial and antifungal activity, exhibits an average antifungal score of 5.6 . (Z)-Ligustilide is orally active, it inhibits the expression of FATP5 and DGAT, inhibits fatty acid uptake and esterification in mice and has potential as therapeutics for nonalcoholic fatty liver disease (NAFLD) . (Z)-Ligustilide is also able to reactivate ERα, has epigenetic regulation, and is used in the study of tamoxifen-resistant breast cancer .
|
-
- HY-14933
-
|
ERB-041
|
Estrogen Receptor/ERR
Wnt
Apoptosis
|
Cancer
|
|
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-A0031S
-
|
TSE-424-d4
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
|
|
Bazedoxifene-d4 is deuterium labeled Bazedoxifene. 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[1][2].
|
-
- HY-180409
-
|
|
Androgen Receptor
|
Cancer
|
|
YM580 is a potent, orally active and selective Androgen Receptor (AR) antagonist (IC50 = 0.11 μM, hAR Ki = 4.6 nM, rAR Ki = 6.2 nM). YM580 exhibits good selectivity over PR, GR, and ERα (Kis > 3300 nM). YM580 decreases ventral prostate weight in mature intact rats dose-dependently without affecting serum testosterone levels. YM580 can be used for the research of prostate cancer .
|
-
- HY-B0723
-
|
FC-1271a
|
Estrogen Receptor/ERR
Caspase
|
Neurological Disease
Endocrinology
Cancer
|
|
Ospemifene (FC-1271a) is an orally active and non-estrogenic selective estrogen receptor modulator (SERM) with Ki values of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene inhibits caspase-3 activity. Ospemifene inhibits neuronal degeneration, prevents bone loss, and increases vaginal weight and vaginal epithelial height. Ospemifene has anticancer activity against breast cancer .
|
-
- HY-A0031S2
-
|
TSE-424-d4 acetate
|
Estrogen Receptor/ERR
|
Cancer
|
|
Bazedoxifene-d4 (acetate) is the deuterium labeled Bazedoxifene[1]. 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[2][3].
|
-
- HY-10426R
-
|
|
Reference Standards
Estrogen Receptor/ERR
Autophagy
|
Cancer
|
|
XCT790 (Standard) is the analytical standard of XCT790 (HY-10426). This product is intended for research and analytical applications. XCT-790 is a potent and selective inverse agonist for ERRα with an IC50 value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ .
|
-
- HY-121441
-
|
|
Estrogen Receptor/ERR
|
Inflammation/Immunology
|
|
Fispemifene, an orally active selective estrogen receptor modulator with anti-inflammatory and antiestrogenic action, attenuates glandular inflammation in an animal model of chronic nonbacterial prostatitis .
|
-
- HY-107835R
-
|
FCR 2769 (Standard)
|
Reference Standards
Insecticide
Parasite
Apoptosis
Bcl-2 Family
|
Infection
Cancer
|
|
Flumethrin (Standard) (FCR 2769 (Standard)) is the analytical standard of Flumethrin (HY-107835). This product is intended for research and analytical applications. Flumethrin (FCR 2769) is a pyrethroid insecticide and acaricide. Flumethrin targets voltage-gated sodium channels and estrogen receptor α (ERα). Flumethrin induces cytotoxicity, apoptosis, genotoxicity and DNA damage in breast cancer cells by regulating the expression of BCL2, BAX, TP53 and P21 genes. Flumethrin is applicable to relevant studies on ectoparasite infections (tick and flea burdens) in dogs and cats, as well as breast cancer.
|
-
- HY-B1984
-
|
4,4'-DDD; p,p'-Dichlorodiphenyl dichloroethane
|
Environmental Pollutants
Drug Metabolite
Apoptosis
Insecticide
Necroptosis
|
Infection
Neurological Disease
Cancer
|
|
p,p'-DDD (4,4’-DDD) is an organochlorine insecticide, a major metabolite of p,p'-DDT. p,p'-DDD is an agonist at estrogen receptor α(ERα) and ERβ. p,p'-DDD increases DNA damage, apoptosis and necrosis in peripheral blood. p,p'-DDD stimulates cell proliferation in SKBR3 cells. p,p'-DDD activates the AP-1 transcription factor. p,p'-DDD decreases sleep times of barbiturates and steroids in rats .
|
-
- HY-175260
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ZN-c5 is a selective and orally active estrogen receptor degrader. ZN-c5 exhibits high potency in the cellular assay (MCF-7, IC50 = 0.3 nM) and binds with high affinity to ERα and ERβ (IC50 = 0.4 nM and 0.8 nM, respectively). ZN-c5 inhibits tumor growth in MCF-7 mouse xenograft model and WHIM20 xenograft model. ZN-c5 can be used for the study of breast cancer .
|
-
- HY-146440
-
|
|
Histone Demethylase
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
LSD1/ER-IN-1 (compound 11g) is a potent ER and LSD1 inhibitor, with an IC50 of 1.55 μM (LSD1). LSD1/ER-IN-1 has high affinity selectivity for ERα protein, with α/β ratio of 7.11. LSD1/ER-IN-1 shows good antiproliferative activity against MCF-7 breast cancer cells, with an IC50 of 8.79 μM .
|
-
- HY-114631
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
EM-800, an orally active anti-estrogen, serves as an antagonist to the transcriptional functions of estrogen receptors α (ERα) and β (ERβ). EM-800 possesses anticancer activity, capable of inhibiting the growth of breast cancer induced by 7,12-Dimethylbenz[a]anthracene (DMBA) (HY-W011845). Furthermore, in ovariectomized animals, EM-800 effectively slows down bone loss. Additionally, EM-800 shows potential in the research of breast and endometrial cancers, while exerting beneficial effects on bone and lipid metabolism .
|
-
- HY-110193
-
SPP-86
2 Publications Verification
|
RET
|
Cancer
|
|
SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells . SPP-86 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-122815
-
|
Fusicoccin A
|
Apoptosis
|
Cancer
|
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Fusicoccin (Fusicoccin A), a fungal pytotoxin, is a stabilizer of specific 14-3-3 protein-protein interactions. Fusicoccin sabilizes H +-ATPase/14-3-3 cmplex in pants, maintaining the enzyme in activated state. Fusicoccin also stabilizes 14-3-3 protein interactions with binding partners containing a C-terminal 14-3-3 recognition motif (a mode 3 motif), such as ERα, GPIbα, TASK3, CTFR, and p53. Fusicoccin induces apoptosis in cancer cells and has anticancer activity .
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- HY-103450R
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Reference Standards
Estrogen Receptor/ERR
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Endocrinology
Cancer
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G36 (Standard) is the analytical standard of G36 (HY-103450). This product is intended for research and analytical applications. G-36 is a cell-permeable nonsteroidal antagonist of the G protein-coupled estrogen receptor (GPER/GPR30), which selectively inhibits estrogen-mediated PI3K activation through GPER, rather than Erα. G-36 also inhibits estrogen-mediated calcium mobilization (IC50=112 nM). G-36 is promising for research in the field of cancer .
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- HY-15731S1
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Isotope-Labeled Compounds
NO Synthase
Endogenous Metabolite
Estrogen Receptor/ERR
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Cardiovascular Disease
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Estetrol-d4 (Major) is the deuterium labeled Estetrol (HY-15731). Estetrol, an orally active estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol binds ERα as well as ERβ (with a fourfold lower affinity). Estetrol increases eNOS expression/activity and NO synthesis in endothelial cells. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast. Estetrol can be used in contraception and menopausal hormone research .
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- HY-125627
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Glucocorticoid Receptor
Androgen Receptor
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Neurological Disease
Metabolic Disease
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CP-394531 is an efficient and highly selective non-steroidal glucocorticoid receptor (GR) antagonist, with a Ki value of 0.1 nM. CP-394531 has a weak binding to androgen receptor (AR) (Ki = 130 nM), and has almost no effect on progesterone receptor (PR) and estrogen receptors (ERα, ERβ). CP-394531 completely blocks the half-maximal agonistic effect induced by Dexamethasone (HY-14648G), with a Kif of 4.1 nM. CP-394531 can be used to study various diseases such as diabetes, obesity, depression, neurodegenerative diseases, glaucoma and Cushing's disease .
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- HY-155197
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Microtubule/Tubulin
Estrogen Receptor/ERR
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Cancer
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ER degrader 7 (Compound 35t) is an ERα and ERβ degrader. ER degrader 7 inhibits tubulin polymerization. ER degrader 7 inhibits cell viability with IC50s of 0.06, 2.56, 15.84, 1.59, 1.67, 1.37 μM for MCF-7, T47D, MCF-10A, LCC2, T47D D538G, and T47D Y537S cells respectively. ER degrader 7 also inhibits breast cancer tumor growth .
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- HY-B1984R
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4,4'-DDD (Standard); p,p'-Dichlorodiphenyl dichloroethane (Standard)
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Reference Standards
Drug Metabolite
Apoptosis
Necroptosis
Insecticide
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Infection
Neurological Disease
Cancer
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p,p'-DDD (Standard) is the analytical standard of p,p'-DDD (HY-B1984) . This product is intended for research and analytical applications. p,p'-DDD (4,4’-DDD) is an organochlorine insecticide, a major metabolite of p,p'-DDT. p,p'-DDD is an agonist at estrogen receptor α(ERα) and ERβ. p,p'-DDD increases DNA damage, apoptosis and necrosis in peripheral blood. p,p'-DDD stimulates cell proliferation in SKBR3 cells. p,p'-DDD activates the AP-1 transcription factor. p,p'-DDD decreases sleep times of barbiturates and steroids in rats.
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- HY-U00425
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Ligands for Target Protein for PROTAC
Estrogen Receptor/ERR
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Metabolic Disease
Cancer
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PROTAC ERRα ligand 1 is a PROTAC target protein ligand. PROTAC ERRα ligand 1 is an orally active ERRα inverse agonist with IC50 values of 0.6 μM for ERRα. PROTAC ERRα ligand 1 shows no significant activity against a panel of other nuclear receptors, including ERα c, ERRγ, ERβ, PPARα, PPARγ, PPARδ, and RXRα. PROTAC ERRα ligand 1 can provide enhanced insulin sensitivity in vivo. PROTAC ERRα ligand 1 can be used for metabolic diseases research, such as type 2 diabetes and obesity .
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- HY-B1984S
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4,4'-DDD-d8; p,p'-Dichlorodiphenyl dichloroethane-d8
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Drug Metabolite
Apoptosis
Necroptosis
Insecticide
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Infection
Neurological Disease
Cancer
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p,p'-DDD-d8 is the deuterium labeled p,p'-DDD[1]. p,p'-DDD (4,4’-DDD) is an organochlorine insecticide, a major metabolite of p,p'-DDT. p,p'-DDD is an agonist at estrogen receptor α(ERα) and ERβ. p,p'-DDD increases DNA damage, apoptosis and necrosis in peripheral blood. p,p'-DDD stimulates cell proliferation in SKBR3 cells. p,p'-DDD activates the AP-1 transcription factor. p,p'-DDD decreases sleep times of barbiturates and steroids in rats .
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- HY-183188
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- HY-147165
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VT02956
1 Publications Verification
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Ser/Thr Kinase
Large Tumor Suppressor (LATS)
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Cancer
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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.
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- HY-169382
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Melatonin Receptor
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Cancer
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Melatonin-Tamoxifen Conjugate (compound 16c) is an anticancer drug conjugate composed of Melatonin (HY-B0075) and Tamoxifen (HY-13757A), which is a potent antagonist of ERα (IC50=863 nM). Melatonin-Tamoxifen Conjugate binds to MLT receptor (Ki=3.1 nM) and promotes β-arrestin (EC50=914 nM) and ERK activation (EC50=98 nM) in cells expressing hMT1 receptor. Melatonin-Tamoxifen Conjugate against several common cell lines MCF-7, MDA-MB-231, and HT-1080 with IC50s of 6.8 μM, 6.4 μM, and 1.7 μM, respectively.
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- HY-139999
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-139999A
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-181136
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Estrogen Receptor/ERR
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Metabolic Disease
Cancer
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Antiestrogenic agent-1, an organophosphorus 13α-estrone derivative, is an antiestrogenic agent. Antiestrogenic agent-1 can disrupt estrogen signaling by inhibiting estrogen-mediated transcriptional activity. Antiestrogenic agent-1 can inhibit cancer cells proliferation, migration, invasion and induce G1-phase arrest. Antiestrogenic agent-1 mitigates estrogen-induced uterine growth in immature rats and inhibits tumor growth in a murine triple-negative breast cancer mice model. Antiestrogenic agent-1 can be used for the researches of cancer and endocrinology,such as breast cancer, oropharyngeal squamous cell carcinoma .
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- HY-114411
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Estrogen Receptor/ERR
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Cancer
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ERRγ inverse agonist 1 (Compound 12) is a selective ERRγ inverse agonist with an IC50 value of 0.040 μM against ERRγ. ERRγ inverse agonist 1 inhibits the activity of ERRγ at the functional level. ERRγ inverse agonist 1 can be used in the research of anaplastic thyroid cancer .
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- HY-163561
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Histone Methyltransferase
Estrogen Receptor/ERR
IFNAR
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Cancer
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CARM1-IN-6 is a potent CARM1 inhibitor that inhibits CARM1 enzymatic activity with an IC50 of 12.3 μM and a Kd of 0.6785 μM. CARM1-IN-6 suppresses oncogenic estrogen/ERα-target gene expression, activates type I interferon (IFN) and IFN-induced genes (ISGs), induces cell cycle arrest, and inhibits breast cancer cell proliferation both in vitro and in vivo. CARM1-IN-6 can be used for the research of breast cancer .
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- HY-W008581
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3-O-Methyl estradiol; 17β-Estradiol 3-methyl ether; 3-Methoxyestradiol
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Biochemical Assay Reagents
TRP Channel
Microtubule/Tubulin
Autophagy
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Metabolic Disease
Cancer
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Estradiol 3-methyl ether (EDME) is a highly selective TRPML1 ion channel antagonist and microtubule (microtubule) depolymerizing agent, with IC50 values of 0.22 μM and 3.8 μM against TRPML1 and TRPML2, respectively; it shows no activity against TRPML3. Estradiol 3-methyl ether induces the disruption of cytoplasmic microtubule networks in mammalian cells, with an EC50 of 9 μM. Independent of estrogen receptors, Estradiol 3-methyl ether blocks autophagy (autophagy), TFEB nuclear translocation, and inhibits the migration and invasion of triple-negative breast cancer cells by suppressing TRPML1. Estradiol 3-methyl ether is applicable for relevant research on triple-negative breast cancer .
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- HY-P10393
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ERα (295-311)
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Apoptosis
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Cancer
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ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
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- HY-P10843
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Estrogen Receptor/ERR
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Cancer
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R4K1 is a cell-permeable stapled peptide. R4K1 binds to the estrogen receptor (ER) α with high affinity and inhibits its interaction with coactivators. R4K1 can enter breast cancer cells to regulate gene transcription and inhibit cell proliferation. R4K1 can be used in the study of cancer .
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| 製品番号 |
製品名 |
Target |
研究分野 |
Image |
| 製品番号 |
製品名 |
Category |
Target |
構造式 |
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- HY-18719S
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Endoxifen-d5 (Z-isomer) is the deuterium labeled Endoxifen (Z-isomer) (HY-18719). Endoxifen (Z-isomer) is an oral active Tamoxifen (HY-13757A) 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 .
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- HY-19822S
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Elacestrant-d4 (RAD1901-d4) is a deuterated labeled Elacestrant (HY-19822). Elacestrant (RAD1901) is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
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- HY-B1984S
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p,p'-DDD-d8 is the deuterium labeled p,p'-DDD[1]. p,p'-DDD (4,4’-DDD) is an organochlorine insecticide, a major metabolite of p,p'-DDT. p,p'-DDD is an agonist at estrogen receptor α(ERα) and ERβ. p,p'-DDD increases DNA damage, apoptosis and necrosis in peripheral blood. p,p'-DDD stimulates cell proliferation in SKBR3 cells. p,p'-DDD activates the AP-1 transcription factor. p,p'-DDD decreases sleep times of barbiturates and steroids in rats .
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- HY-B0723S
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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 .
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- HY-19822S1
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Elacestrant-d4-1 is the deuterium labeled Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively .
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- HY-19822S2
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Elacestrant-d10 is the deuterium labeled of Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also inhibits growth of ER + breast cancer cell lines in vitro and in vivo .
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- HY-B0723S2
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Ospemifene-d5 (FC-1271a-d5) is deuterium labeled Ospemifene. Ospemifene is a non-estrogen selective estrogen receptor modulator (SERM), with Kis of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene can be used for the research of vaginal atrophy and breast cancer .
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- HY-19822S3
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Elacestrant-d6 (RAD1901-d6) is a deuterated labeled Elacestrant (HY-19822). Elacestrant is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
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- HY-A0031S
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Bazedoxifene-d4 is deuterium labeled Bazedoxifene. 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[1][2].
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- HY-A0031S2
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Bazedoxifene-d4 (acetate) is the deuterium labeled Bazedoxifene[1]. 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[2][3].
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- HY-15731S1
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Estetrol-d4 (Major) is the deuterium labeled Estetrol (HY-15731). Estetrol, an orally active estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol binds ERα as well as ERβ (with a fourfold lower affinity). Estetrol increases eNOS expression/activity and NO synthesis in endothelial cells. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast. Estetrol can be used in contraception and menopausal hormone research .
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- HY-B1662S3
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Hexestrol-d4 is the deuterium labeled Hexestrol (HY-B1662). 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 .
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- HY-179232
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Tetrazine
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ERα antagonist 2 (Compound 5b) is an ER-α antagonist with an IC50 value of 1729 nM. ERα antagonist 2 exhibits significant inhibitory activity against breast cancer cell lines, and is still effective against ER-negative cells (MDA-MB-231), suggesting the existence of ER-independent pathways. ERα antagonist 2 can be used for the study of breast cancer .
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- HY-139999
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Azide
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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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-139999A
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Azide
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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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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