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human ER

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45

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4

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5

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16

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100583A

    Estrogen Receptor/ERR Drug Metabolite Cardiovascular Disease Neurological Disease Cancer
    (±)-Equol is the racemate of equol. (±)-equol exhibits EC50s of 200 and 74 nM for human ERα and ERβ, respectively. Equol is a metabolite of the soy isoflavones, daidzin and daidzein.
    (±)-Equol
  • 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 .
    Estetrol
  • HY-B0845
    Prochloraz
    1 Publications Verification

    BTS 40542

    Environmental Pollutants Estrogen Receptor/ERR Aryl Hydrocarbon Receptor Fungal Androgen Receptor Infection Endocrinology
    Prochloraz is an imidazole antifungal. Prochloraz is as an estrogen receptor (ER) and androgen receptor (AR) antagonist and an aromatase inhibitor with IC50 values of 25 μM, 4 μM and 0.3 μM, respectively. Prochloraz is able to activate the aryl hydrocarbon receptor (AhR) having an EC50 of 1 μM .
    Prochloraz
  • HY-14933
    Prinaberel
    3 Publications Verification

    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 .
    Prinaberel
  • HY-114297
    Zymosterol
    2 Publications Verification

    Endogenous Metabolite Others
    Zymosterol is a Cholesterol (HY-N0322) biosynthesis metabolite. Zymosterol, a precursor of Cholesterol, is found mostly in the plasma membrane. Zymosterol circulates within the cell .
    Zymosterol
  • HY-134809

    CADA

    HIV Infection Inflammation/Immunology
    Cyclotriazadisulfonamide (CADA) is a specific CD4-targeted HIV entry inhibitors. Cyclotriazadisulfonamide (CADA) inhibits the co-translational translocation of human CD4 (huCD4) into the ER lumen in a signal peptide (SP)-dependent way. Cyclotriazadisulfonamide is also a Sec61 translocon inhibitor .
    Cyclotriazadisulfonamide
  • HY-42484

    ERibulin intERmediate

    Microtubule/Tubulin Cancer
    ER-076349 (Eribulin intermediate) is an inhibitor of tubulin polymerization, induces G2-M cell cycle arrest, and disrupts mitotic spindles. ER-076349 inhibits cancer cell growth, and inhibits tumor growth in several human tumor xenografts. ER-076349 is an analog of Halichondrin B .
    ER-076349
  • HY-B0862

    Environmental Pollutants Herbicide Apoptosis Bcl-2 Family Caspase SOD Mitochondrial Metabolism Others
    Pendimethalin is an orally active herbicide that controls annual grasses and certain broadleaf weeds. Pendimethalin induces Apoptotic cell death through activating ER stress-mediated mitochondrial dysfunction in human umbilical vein endothelial cells .
    Pendimethalin
  • HY-100688
    ML390
    1 Publications Verification

    Dihydroorotate Dehydrogenase Cancer
    ML390 is a potent dihydroorotate dehydrogenase (DHODH) inhibitor. ML390 is an inducer of myeloid differentiation and causes myeloid differentiation in murine (ER-HoxA9) and human (U937 and THP1) acute myeloid leukemia (AML) models .
    ML390
  • HY-114263
    NXT629
    4 Publications Verification

    PPAR Cancer
    NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively . NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models .
    NXT629
  • HY-103457

    Estrogen Receptor/ERR Cancer
    Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells .
    Y134
  • HY-B1353

    4'-Hydroxypropiophenone

    Estrogen Receptor/ERR Endocrinology
    Paroxypropione (4'-Hydroxypropiophenone) is a manufactured, nonsteroidal estrogen and can be used for endocrine research .
    Paroxypropione
  • HY-131688

    PARP Caspase Inflammation/Immunology
    2-Chlorohexadecanoic acid, an inflammatory lipid mediator, interferes with protein palmitoylation,induces ER-stress markers, reduced the ER ATP content, and activates transcription and secretion of IL-6 as well as IL-8.2-Chlorohexadecanoic acid disrupts the mitochondrial membrane potential and induces procaspase-3 and PARP cleavage.2-Chlorohexadecanoic acid can across blood-brain barrier (BBB) and compromises ER- and mitochondrial functions in the human brain endothelial cell line hCMEC/D3 .
    2-Chlorohexadecanoic acid
  • HY-124414

    Estrogen Receptor/ERR Drug Metabolite Cancer
    4'-Hydroxytamoxifen is a metabolite of Tamoxifen. 4'-Hydroxytamoxifen shows higher affinity for the ER than Tamoxifen. 4'-Hydroxytamoxifen induces a non-apoptotic cytotoxic effect in human endometrial adenocarcinoma cells .
    4'-Hydroxytamoxifen
  • HY-125209A

    Apoptosis PARP DNA/RNA Synthesis Cancer
    TH5427 hydrochloride is a NUDT5 inhibitor with a human target IC50 of 29 nM, ~690-fold selectivity over MTH1 in vitro, and selective functional inhibition over other NUDIX hydrolases including NUDT9 .TH5427 hydrochloride binds to the active site of NUDT5, blocking enzymatic activity related to ADP-ribose metabolism and PAR-derived ATP synthesis .TH5427 hydrochloride blocks progestin-dependent nuclear ATP synthesis, impairs progestin-induced chromatin remodeling, inhibits histone H1 displacement, disrupts progestin-dependent gene regulation, and abrogates progestin-dependent proliferation in breast cancer cells .TH5427 hydrochloride functions as a versatile probe to study nuclear ATP dynamics and ADP-ribose-related metabolism in cells .TH5427 hydrochloride engages NUDT5 at physiological temperatures, as demonstrated by Drug Affinity Responsive Target Stability (DARTS) assay .TH5427 hydrochloride stabilizes NUDT5 against thermal denaturation in cell lysates and intact cells, as shown by cellular thermal shift assay (CETSA) .TH5427 hydrochloride functionally inhibits NUDT5 activity, leading to downstream effects on oxidative DNA damage and DNA replication in triple-negative breast cancer (TNBC) cells .TH5427 hydrochloride suppresses proliferation of TNBC cells without inducing cell death or apoptosis, slows DNA replication in TNBC cells, promotes accumulation of oxidative DNA lesions, and triggers DNA damage response in TNBC cells .TH5427 hydrochloride suppresses growth of TNBC cells in vitro, inhibits growth of TNBC xenograft tumors in nude mice in vivo, and shows greater potency against TNBC cell lines compared to ER-positive and normal-like breast cell lines .TH5427 hydrochloride can be used for the research of breast cancer and triple-negative breast cancer .
    TH5427 hydrochloride
  • HY-124414A

    Estrogen Receptor/ERR Drug Metabolite Cancer
    4'-Hydroxytamoxifen TFA is a salt form of a metabolite of Tamoxifen. 4'-Hydroxytamoxifen TFA has a higher affinity for ER than Tamoxifen. 4'-Hydroxytamoxifen TFA induces non-apoptotic cytotoxicity in human endometrial adenocarcinoma cells .
    4'-Hydroxytamoxifen TFA
  • HY-116099

    Prostaglandin Receptor Inflammation/Immunology
    ER-819762 is an orally active, highly selective prostaglandin E2 (PGE2) EP4 receptor antagonist with an EC50 of 70 nM against human EP4 receptor. ER-819762 can be used for rheumatoid arthritis research .
    ER-819762
  • HY-138961
    ER-27319
    1 Publications Verification

    Syk Inflammation/Immunology
    ER-27319, an acridone derivative, is a potent and selective SYK inhibitor, and inhibits the tyrosine phosphorylation of SYK and its activity. ER-27319 inhibits the release of antigen-induced allergic mediators from human and rat mast cells with an IC50 of 10 μM and can be used for study in allergic diseases .
    ER-27319
  • HY-126932

    Estrogen Receptor/ERR Cancer
    TTC-352 is an orally bioavailable selective human estrogen receptor (ER) α partial agonist (ShERPA). TTC-352 inhibits the growth of three ER+ breast cancer cells. TTC-352 induces tumor regression accompanied by exit of ERα from the nucleus to extranuclear sites .
    TTC-352
  • HY-W011241

    (8R,9S)-Cinchonine hydrochloride; LA40221 hydrochloride

    Apoptosis Parasite Cancer
    Cinchonine hydrochloride ((8R,9S)-Cinchonine hydrochloride) is a natural alkaloid present in Cinchona bark, with antimalarial activity. Cinchonine hydrochloride activates endoplasmic reticulum (ER) stress-induced apoptosis in human liver cancer cells .
    Cinchonine hydrochloride
  • HY-W288480

    Apoptosis Cancer
    Trihexyl phosphate is an organophosphate flame retardant. Trihexyl phosphate causes mitochondrial impairment and induces cell apoptosis in CHO cells. Trihexyl phosphate promotes the proliferation of human breast cancer cells (MCF-7) in a dose-dependent manner and exerts estrogenicity via ERα-independent pathways .
    Trihexyl phosphate
  • HY-123024

    BL-S-640; SK&F 60771

    Apoptosis Bacterial Antibiotic Infection Cancer
    Cefatrizine (BL-S-640) is an orally active and broad-spectrum cephalosporin antibiotic. Cefatrizine is also a eEF2K inhibitor, with anti-proliferative activity in human breast cancer cells, which could induce ER stress, leading to cell death. Cefatrizine can be used in studies of cancer and bacterial infection .
    Cefatrizine
  • HY-123163

    RWJ-66826; RTI-6617-003

    Progesterone Receptor Glucocorticoid Receptor Androgen Receptor Estrogen Receptor/ERR Endocrinology Cancer
    JNJ-1250132 (RWJ-66826) is an orally active and potent steroidal progesterone receptor (PR) antagonist, with an IC50 of 1.3 nM. JNJ-1250132 inhibits binding of the receptor to DNA in vitro. JNJ-1250132 is a potent competitive inhibitor of binding to the human glucocorticoid receptor (GR) (IC50=0.50 nM) and the rat androgen receptor (AR) (IC50=5.6 nM), and was a weak inhibitor of binding to human Estrogen receptor (ER) (IC50 >3000 nM) .
    JNJ-1250132
  • HY-175171

    Topoisomerase VEGFR c-Met/HGFR EGFR Estrogen Receptor/ERR Cancer
    Anticancer agent 276 (Compound 5) is a multi-target anticancer agent. Anticancer agent 276 has a potent anticancer activity against human tumor cells with IC50s of 6.90 and 4.48 μM for HEPG2 and MCF7 cells, respectively. Anticancer agent 276 shows strong and stable interactions across multiple targets, including Topoisomerase II, VEGFR2, c-Met, EGFR and ERα .
    Anticancer agent 276
  • HY-108489
    ER-27319 maleate
    1 Publications Verification

    Syk Inflammation/Immunology
    ER-27319 (maleate), an acridone derivative, is a potent and selective SKY inhibitor, and inhibits the tyrosine phosphorylation of SYK and its activity. ER-27319 (maleate) inhibits the release of antigen-induced allergic mediators from human and rat mast cells with an IC50 of 10 μM and can be used for study in allergic diseases [1] [2] .
    ER-27319 maleate
  • HY-P11298

    Caspase Apoptosis JNK p38 MAPK Interleukin Related IFNAR Inflammation/Immunology Cancer
    d-T101 peptide, a human hormone-peptide, is a T1/ST2 receptor ligand. d-T101 peptide binds to the T1/ST2 receptor and activates caspases 8, 9 and 3 mediated apoptosis, together with activation of JNKinase and p38 MAPKinase. d-T101 peptide also changes Golgi structural with function loss and downregulation of the endoplasmic reticulum (ER) stress repair mechanism. d-T101 peptide has immunostimulatory and anticancer activity, selectively induces apoptosis in proliferating cancer cells and increases IL-2 and IFN-γ expression as well as the recruitment of NK cells and M1 macrophages to the tumor site .
    d-T101 peptide
  • HY-P3833

    Anti-estrogen

    Estrogen Receptor/ERR Endocrinology
    Yp537 is an estrogen receptor (ER) inhibitor that blocks dimerization of the human estrogen receptor .
    Yp537
  • HY-100583AR

    Reference Standards Estrogen Receptor/ERR Drug Metabolite Cardiovascular Disease Neurological Disease Cancer
    (±)-Equol (Standard) is the analytical standard of (±)-Equol. This product is intended for research and analytical applications. (±)-Equol is the racemate of equol. (±)-equol exhibits EC50s of 200 and 74 nM for human ERα and ERβ, respectively. Equol is a metabolite of the soy isoflavones, daidzin and daidzein.
    (±)-Equol (Standard)
  • 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 .
    Trioxifene mesylate
  • HY-E70615

    Endogenous Metabolite Cancer
    Protein Disulfide Isomerase, Human, an oxidoreductase, is a mainly endoplasmic reticulum (ER) resident protein. Protein Disulfide Isomerase, Human plays an important role in maintaining cellular homeostasis through thiol oxidation/reduction cycling, chaperone action, and isomerization of client proteins .
    Protein Disulfide Isomerase, Human
  • HY-167868

    TRP Channel Apoptosis Neurological Disease Cancer
    DWP-05195 is a TRPV1 antagonist that can inhibit the pain signal transduction. DWP-05195 induces ER stress-dependent apoptosis through the ROS-p38-CHOP pathway in human ovarian cancer cells .
    DWP-05195
  • HY-15731S1

    Isotope-Labeled Compounds NO Synthase Endogenous Metabolite Estrogen Receptor/ERR Cardiovascular Disease
    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 .
    Estetrol-d4 (Major)
  • HY-121149B

    (E/Z)-3-Hydroxytamoxifen

    Estrogen Receptor/ERR Apoptosis Cancer
    (E/Z)-Droloxifene is a mixture of (E)-droloxifene (a selective estrogen receptor modulator) and (Z)-droloxifene. (E)-Droloxifene binds to the estrogen receptor (ER) with an IC50 value of 24 nM in rabbit uterine homogenates. (E)-Droloxifene increases uterine weight in immature rats, and reduces estradiol-induced increases in uterine weight in juvenile rats. (E)-Droloxifene also inhibits 17β-estradiol-stimulated growth of MCF-7, ZR-75-1, and T47D human breast cancer cells. (Z)-Droloxifene binds weakly to ER and has no estrogenic or antiestrogenic activity .
    (E/Z)-Droloxifene
  • HY-124414R

    Reference Standards Estrogen Receptor/ERR Drug Metabolite Cancer
    4'-Hydroxytamoxifen (Standard) is the analytical standard of 4'-Hydroxytamoxifen. This product is intended for research and analytical applications. 4'-Hydroxytamoxifen is a metabolite of Tamoxifen. 4'-Hydroxytamoxifen shows higher affinity for the ER than Tamoxifen. 4'-Hydroxytamoxifen induces a non-apoptotic cytotoxic effect in human endometrial adenocarcinoma cells .
    4'-Hydroxytamoxifen (Standard)
  • HY-124414AR

    Reference Standards Estrogen Receptor/ERR Drug Metabolite Cancer
    4'-Hydroxytamoxifen (TFA) (Standard) is the analytical standard of 4'-Hydroxytamoxifen (TFA). This product is intended for research and analytical applications. 4'-Hydroxytamoxifen TFA is a salt form of a metabolite of Tamoxifen. 4'-Hydroxytamoxifen TFA has a higher affinity for ER than Tamoxifen. 4'-Hydroxytamoxifen TFA induces non-apoptotic cytotoxicity in human endometrial adenocarcinoma cells[1].
    4'-Hydroxytamoxifen TFA (Standard)
  • HY-P5344

    Fluorigenic PEXEL peptide

    Parasite Others
    Dabcyl-LNKRLLHETQ-Edans (Fluorigenic PEXEL peptide) is a biological active peptide. (This FRET substrate peptide for Plasmepsin V (PMV) is derived from the conserved Plasmodium Export Element (PEXEL) motif of Histidine-Rich Protein II (HRPII). PMV is an ER aspartic protease that recognizes and cleaves the RXL sequence within the PEXEL motif of proteins exported by human malaria parasite Plasmodium falciparum, allowing them to translocate into host erythrocytes.)
    Dabcyl-LNKRLLHETQ-Edans
  • 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 .
    Lactandrate
  • HY-B0845R

    BTS 40542 (Standard)

    Reference Standards Fungal Estrogen Receptor/ERR Androgen Receptor Aryl Hydrocarbon Receptor Infection Endocrinology
    Prochloraz (Standard) is the analytical standard of Prochloraz. This product is intended for research and analytical applications. Prochloraz is an imidazole antifungal. Prochloraz is as an estrogen receptor (ER) and androgen receptor (AR) antagonist and an aromatase inhibitor with IC50 values of 25 μM, 4 μM and 0.3 μM, respectively. Prochloraz is able to activate the aryl hydrocarbon receptor (AhR) having an EC50 of 1 μM .
    Prochloraz (Standard)
  • HY-180323

    RAR/RXR Inflammation/Immunology
    ER-38925 is a retinoid agonist with selevtivity to retinoic acid receptor subtype α (RAR-α). ER-38925 prolongs the lifespan of the recipient mice dose-dependently. ER-38925 potently inhibits alloantigenstimulated donor T lymphocyte prolifertion in vitro. ER-38925 can prevent the development of antiallogeneic cytotoxic T lymphocyte response in mice. ER-38925 inhibits serum anti-DNA autoantibody production in mouse model of human chronic GVHD .
    ER-38925
  • HY-P3833A

    Anti-estrogen TFA

    Estrogen Receptor/ERR Endocrinology
    Yp537 TFA is an estrogen receptor (ER) inhibitor that blocks dimerization of the human estrogen receptor .
    Yp537 TFA
  • 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 .
    Trioxifene
  • 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 .
    ent-Estradiol
  • HY-182674

    Sec61 HIV Flavivirus Neurotensin Receptor Infection Cancer
    VGD020 is a highly potent and selective Sec61 translocon inhibitor . VGD020 suppresses the expression of cell surface CD4 by inhibiting signal peptide-dependent co-translational ER translocation, interferes with the initiation of ER translocation of dengue virus polyprotein, and reduces the expression of Sortilin in breast cancer cells. VGD020 exhibits broad anti-flavivirus and anti-HIV activities. VGD020 can be used in research related to dengue virus infection, Zika virus infection, yellow fever virus infection, human immunodeficiency virus infection, and breast cancer .
    VGD020
  • HY-100688R

    Reference Standards Dihydroorotate Dehydrogenase Cancer
    ML390 (Standard) is the analytical standard of ML390 (HY-100688). This product is intended for research and analytical applications. ML390 is a potent dihydroorotate dehydrogenase (DHODH) inhibitor. ML390 is an inducer of myeloid differentiation and causes myeloid differentiation in murine (ER-HoxA9) and human (U937 and THP1) acute myeloid leukemia (AML) models .
    ML390 (Standard)
  • HY-179476

    Androgen Receptor Endogenous Metabolite Inflammation/Immunology Cancer
    3-Oxochol-5-en-24-oic acid is a rare bile acid produced by the intestinal microbiota. 3-Oxochol-5-en-24-oic acid is a potent antagonist of the human androgen receptor (hAR), with an IC50 of 119.4 nM. 3-Oxochol-5-en-24-oic acid has no significant agonistic or antagonistic effects on estrogen receptors (ER) or glucocorticoid receptors (GR). 3-Oxochol-5-en-24-oic acid effectively inhibits the growth of prostate cancer cells. In animal models, it enhances the efficacy of anti-PD-1 therapy by regulating the differentiation of CD8 + T cells. 3-Oxochol-5-en-24-oic acid can be used for research on regulating host immunity and anti-tumor studies .
    3-Oxochol-5-en-24-oic acid

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