Search Result
Results for "
Estrogen Inhibitors
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
29
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P3833A
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- HY-150601
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- HY-B2158
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Estrogen Receptor/ERR
COX
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Cardiovascular Disease
Endocrinology
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Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood .
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- HY-N9329
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Monoamine Oxidase
Estrogen Receptor/ERR
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Metabolic Disease
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Glicoricone, a phenolic compound, is isolated from a species of licorice. Glicoricone is an inhibitor of monoamine oxidase (MAO), with an IC50 of 140 μM. Glicoricone binds to estrogen receptor (ER) and shows estrogen antagonist activity .
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- HY-106056
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D 16726
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Estrogen Receptor/ERR
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Cancer
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Zindoxifene is a partial anti-estrogen. Zindoxifene works primarily by binding to estrogen receptors, thereby inhibiting the growth of estrogen-dependent tumor cells. Zindoxifene is able to exhibit the dual properties of estrogen agonists and antagonists and can be used in research and development to target estrogen-dependent tumors, such as prostate and breast cancer .
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- HY-P3833
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- HY-153700
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Estrogen Receptor/ERR
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Endocrinology
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Estrogen receptor modulator 8 (compound 4) is an orally active inhibitor of Estrogen Receptor/ERR α (IC50=0.437 nM, MCF-7 cells). Estrogen receptor modulator 8 inhibits MCF-7 cells proliferation with an IC50 value of 0.1 nM .
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- HY-118242
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Estrogen Receptor/ERR
Calmodulin
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Others
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RU 45144 is an anti-estrogen compound that has the activity of antagonizing the binding of estrogen receptors to calmodulin. RU 45144 can inhibit the binding of estrogen receptors to calmodulin, and its effect is similar to that of tamoxifen. Its anti-estrogen effect may be related to specific side chains in the molecular structure, and the steroid skeleton may be involved in its anti-proliferative activity.
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- HY-171477
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Estrogen Receptor/ERR
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Cancer
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Metahexestrol is an estrogen receptor (E2R) inhibitor with antitumor activity. It significantly inhibits the proliferation of estrogen receptor-positive MCF-7 human breast cancer cells (ED50 = 1.0 μM). Additionally, Metahexestrol also exhibits inhibitory effects in estrogen receptor-negative MDA-MB-231 cells, and its antiproliferative activity cannot be reversed by estrogen, suggesting that its mechanism of action may be partially independent of the E2R pathway. Metahexestrol can be used in research on estrogen-dependent breast cancer .
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- HY-111484A
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SRN-927 Racemate
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Estrogen Receptor/ERR
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Cancer
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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.
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- HY-103450
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Estrogen Receptor/ERR
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Endocrinology
Cancer
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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-B0723
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FC-1271a
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Estrogen Receptor/ERR
Caspase
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Neurological Disease
Endocrinology
Cancer
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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 .
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- HY-B2158S
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- HY-14247B
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CGS 16949A hemihydrate; (Rac)-FAD286 hydrochloride hemihydrate
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Cytochrome P450
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Endocrinology
Cancer
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Fadrozole hydrochloride hemihydrate is an orally active, potent, selective and nonsteroidal aromatase inhibitor, with an IC50 of 6.4 nM. Fadrozole hydrochloride hemihydrate inhibits the production of estrogen and progesterone, with IC50 values of 0.03 and 120 μM. Fadrozole hydrochloride hemihydrate shows prevention of spontaneous tumours. Fadrozole hydrochloride hemihydrate can be used for the research of estrogen-dependent disease and cancer .
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- HY-W106688
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Estrogen Receptor/ERR
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Endocrinology
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Triisopropyl phosphate inhibits TFF1 and EGR3 gene expression, exhibits anti-estrogenic activity that inhibits Estradiol (HY-B0141)-induced MCF-7 cell proliferation with an EC50 of 341 μM. Triisopropyl phosphate inhibits the estrogen response element (ERE)-stimulated luciferase activity in MVLN cells with an EC50 of 900 μM .
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- HY-B2158R
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Reference Standards
Estrogen Receptor/ERR
COX
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Cardiovascular Disease
Endocrinology
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Chlorotrianisene (Standard) is the analytical standard of Chlorotrianisene. This product is intended for research and analytical applications. Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood .
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- HY-169063
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- HY-131404
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TPBM
1 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-146424
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- HY-135581
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Estrogen Receptor/ERR
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Endocrinology
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Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
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- HY-135582
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Estrogen Receptor/ERR
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Endocrinology
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Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
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- HY-W010062
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Drug Derivative
Cytochrome P450
Estrogen Receptor/ERR
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Metabolic Disease
Cancer
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4-Chlorophenylacetic acid is a halogenated phenylacetic acid derivative. 4-Chlorophenylacetic acid is a potent aromatase inhibitor and antagonizes estrogen signaling. 4-Chlorophenylacetic acid can provide carbon and energy for Pseudomonas sp. strain CBS3. 4-Chlorophenylacetic acid is effective against estrogen-induced mammary tumorigenesis .
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- HY-B0141A
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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-B1100
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- HY-123247
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Cytochrome P450
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Endocrinology
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LY113174 is an orally active aromatase inhibitor (IC50 = 24 nM). LY113174 blocks testosterone induced increase in uterine weight in rat, and inhibits ovarian estrogen biosynthesis .
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- HY-173279
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Cytochrome P450
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Endocrinology
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CYP19A1-IN-1 (Compound 9) is a CYP19A1 inhibitor with an IC50 of 271 nM. CYP19A1-IN-1 inhibits the activity of converting androgens to estrogens by binding to CYP19A1. CYP19A1-IN-1 can be used in the research of sex hormone-related diseases such as estrogen-dependent breast cancer .
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- HY-N3943
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Tyrosinase
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Neurological Disease
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Glabrene, an isoflavene derived from licorice root, shows estrogen-like activity. Glabrene is a tyrosinase inhibitor with an IC50 of 3.5 μM .
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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-124403
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Estrogen Receptor/ERR
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Cancer
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D 15413 is an orally active antagonist for nonsteroidal estrogen. D 15413 inhibits growth of estrogen receptor positive MCF-7 cell with an inhibition rate of 70% at 10 -7 M. D 15413 exhibits antitumor efficacy against DMBA (HY-W011845) or MNU (HY-34758)-induced breast cancer .
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- HY-135581S1
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Isotope-Labeled Compounds
Estrogen Receptor/ERR
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Endocrinology
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Raloxifene 6-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
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- HY-135582S1
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Isotope-Labeled Compounds
Estrogen Receptor/ERR
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Endocrinology
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Raloxifene 4'-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 4'-glucuronide. Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
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- HY-129433
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17β-HSD
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Endocrinology
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17β-HSD1-IN-2 (PBRM) is a non-estrogenic and steroidal covalent irreversible inhibitor of 17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) (Ki=368 nM). 17β-HSD1-IN-2 can be used for the research of estrogen-dependent disorders .
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- HY-137391
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Estrogen Receptor/ERR
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Metabolic Disease
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2-Bromoestradiol is a estrogen 2-hydroxylase inhibitor. 2-Bromoestradiol decreases irreversible binding of radiolabeled estradiol metabolite(s) to microsomal proteins .
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- HY-135582S
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Estrogen Receptor/ERR
Isotope-Labeled Compounds
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Endocrinology
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Raloxifene 4'-glucuronide-d4 is deuterated labeled Raloxifene 4'-glucuronide (HY-135582). Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
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- HY-13757A
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Tamoxifen
Maximum Cited Publications
139 Publications Verification
ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen
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Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
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Endocrinology
Cancer
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Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER transgenic mouse .
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- HY-B0887
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NRDC-143
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Parasite
Mitochondrial Metabolism
Sodium Channel
Na+/K+ ATPase
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Infection
Neurological Disease
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Permethrin (NRDC-143) is an insecticide, acaricide and a high selectively inhibitor of the Mitochondrial complex I, found in sediment and water samples. Permethrin shows estrogenic in vivo and anti-estrogenic activity in vitro. Permethrin also acts as a neurotoxin affecting neuron membranes by prolonging Sodium channel activation. Permethrin decreases resistance to bacterial infections in medaka (Oryzias latipes) .
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- HY-19822S3
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RAD1901-d6
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Isotope-Labeled Compounds
Estrogen Receptor/ERR
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Cancer
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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-121149B
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(E/Z)-3-Hydroxytamoxifen
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Estrogen Receptor/ERR
Apoptosis
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Cancer
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(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 .
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- HY-18719B
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- HY-18719E
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- HY-163712
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Estrogen Receptor/ERR
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Endocrinology
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17-Epiestriol is an estrogen metabolite and a selective estrogen receptor (ER) β agonist. 17-epiestriol inhibits the mRNA and protein expression of the vascular cell adhesion molecule VCAM-1 induced by tumor necrosis factor α (TNFα). 17-epiestriol also inhibits TNFα-induced VCAM-1 expression and prevents NF-κB migration to the nucleus. 17-Epiestriol also induces the mRNA and protein expression of endothelial nitric oxide synthase .
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- HY-14248
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CGS 20267
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Cytochrome P450
Autophagy
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Cancer
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Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer .
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- HY-W010062R
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Reference Standards
Cytochrome P450
Estrogen Receptor/ERR
Drug Derivative
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Metabolic Disease
Cancer
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4-Chlorophenylacetic acid (Standard) is the analytical standard of 4-Chlorophenylacetic acid. This product is intended for research and analytical applications. 4-Chlorophenylacetic acid is a halogenated phenylacetic acid derivative. 4-Chlorophenylacetic acid is a potent aromatase inhibitor and antagonizes estrogen signaling. 4-Chlorophenylacetic acid can provide carbon and energy for Pseudomonas sp. strain CBS3. 4-Chlorophenylacetic acid is effective against estrogen-induced mammary tumorigenesis .
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- HY-19822S
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RAD1901-d4
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Isotope-Labeled Compounds
Estrogen Receptor/ERR
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Cancer
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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-117726
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- HY-13757
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ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate
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Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
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Cancer
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Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis . Tamoxifen Citrate also can induce gene knockout of CreER transgenic mouse .
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- HY-125263B
-
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Estrogen Receptor/ERR
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Cancer
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(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.
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- HY-137449
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G1T48
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Estrogen Receptor/ERR
CDK
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Cancer
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Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a CDK4/6 inhibitor .
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- HY-168644
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- HY-135590
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Estrogen Receptor/ERR
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Endocrinology
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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 .
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- HY-135584
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Estrogen Receptor/ERR
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Endocrinology
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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 .
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- HY-N6714
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Topoisomerase
Androgen Receptor
Estrogen Receptor/ERR
Apoptosis
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Infection
Cancer
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Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .
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- HY-13757AS1
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ICI 47699-d3; (Z)-Tamoxifen-d3; trans-Tamoxifen-d3
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Isotope-Labeled Compounds
Estrogen Receptor/ERR
Apoptosis
Autophagy
HSP
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Cancer
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Tamoxifen-d3 is the deuterium labeled Tamoxifen . Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse .
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- HY-N7501
-
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Others
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Metabolic Disease
Inflammation/Immunology
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Isoformononetin is an analog of Daidzein (HY-N0019) and has immunoprotective effects. Isoformononetin inhibits the differentiation of Th17 and B-cells lymphopoesis to promote osteogenesis in estrogen-deficient bone loss conditions .
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- HY-W087008
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Cytochrome P450
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Endocrinology
Cancer
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7-Hydroxyflavanone is a potent inhibitor of aromatase (CYP19) activity with the IC50 of 65 μM. 7-Hydroxyflavanone exerts various biological effects, including anticarcinogenic, antioxidant and (anti-)estrogenic effects, and modula
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- HY-113986B
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(S)-Fadrozole; (S)-CGS 16949A free base; (S)-FAD286
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Cytochrome P450
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Inflammation/Immunology
Endocrinology
Cancer
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(S)-Dexfadrostat ((S)-Fadrozole) is an aromatase inhibitor with an IC50 of 4.6 nM in human placental microsomes in vitro. (S)-Dexfadrostat can be used in the study of estrogen-dependent breast cancer, gynecomastia, and systemic lupus erythematosus .
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- HY-B0141AS
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Alfatradiol-d3; Epiestradiol-d3; Epiestrol-d3
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5 alpha Reductase
Endogenous Metabolite
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Inflammation/Immunology
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Alpha-Estradiol-d3 is the deuterium labeled Alpha-Estradiol. Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.
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- HY-W778408
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ICI 47699-13C6; (Z)-Tamoxifen-13C6; trans-Tamoxifen-13C6
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Isotope-Labeled Compounds
Apoptosis
Autophagy
HSP
Estrogen Receptor/ERR
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Endocrinology
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Tamoxifen- 13C6 (ICI 47699- 13C6) is the 13C-labeled Tamoxifen (HY-13757A). Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER transgenic mouse .
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- HY-13757AR
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ICI 47699(Standard); (Z)-Tamoxifen(Standard); trans-Tamoxifen (Standard)
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Reference Standards
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
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Endocrinology
Cancer
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Tamoxifen (Standard) is the analytical standard of Tamoxifen (HY-13757A). This product is intended for research and analytical applications. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse .
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- HY-N0250
-
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- HY-B0141AS1
-
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- HY-N15524
-
-
- HY-19498
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SIM-688
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NF-κB
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Inflammation/Immunology
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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.
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- HY-N12023
-
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Bacterial
Fungal
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Infection
Cancer
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Deacetylnomilin can be isolated from Citrus reticulata and has antibacterial and antifungal activity. Deacetylnomilin is a potent inhibitor of cell proliferation with an IC50 value of 0.005 ug/mL against estrogen receptor-positive (ER+) cells .
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- HY-W774926
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NRDC-143-d6
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Isotope-Labeled Compounds
Na+/K+ ATPase
Parasite
Sodium Channel
Mitochondrial Metabolism
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Infection
Neurological Disease
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Permethrin-d6 (NRDC-143-d6) is deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide and a high selectively inhibitor of the Mitochondrial complex I, found in sediment and water samples. Permethrin shows estrogenic in vivo and anti-estrogenic activity in vitro. Permethrin also acts as a neurotoxin affecting neuron membranes by prolonging Sodium channel activation. Permethrin decreases resistance to bacterial infections in medaka (Oryzias latipes) .
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- HY-B1100R
-
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Reference Standards
Estrogen Receptor/ERR
Apoptosis
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Endocrinology
Cancer
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Estradiol cypionate (Standard) is the analytical standard of Estradiol cypionate. This product is intended for research and analytical applications. Estradiol cypionate is the 17β-cypionate ester of Estradiol, which inhibits ET-1 synthesis by acting on estrogen receptors .
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- HY-P2413
-
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Androgen Receptor
Src
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Others
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Ac-PPPHPHARIK-NH2 (compound S1) is a compound that inhibits the interaction between androgen receptor and Src. It can inhibit the binding of androgen or estrogen-induced receptor and Src in cancer cells, as well as the activation of related signaling pathways, and can also inhibit cell cycle progression and tumor growth.
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- HY-107550
-
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HDAC
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Cancer
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TCS HDAC6 20b is a HDAC6-selective inhibitor. TCS HDAC6 20b blocks the growth of estrogen receptor α-positive breast cancer MCF-7 cells .
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- HY-150542
-
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Steroid Sulfatase
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Cancer
|
Steroid sulfatase -IN-2 is an active steroid sulfatase (STS) inhibitor with an IC50 value of 109.5 nM. Steroid sulfatase-IN-2 can be used for the research of hormone-dependent cancers, such as estrogen-dependent breast and endometrial cancer .
|
-
- HY-N1581
-
Nigakilactone D
|
Parasite
|
Infection
Endocrinology
|
Quassin (Nigakilactone D) is a bioactive triterpenoid from stem bark extract of Quassia amara. Quassin inhibits P. falciparum with an IC50 of 0.15 μM. Quassin possesses reversible antifertility, anti-estrogenic and anti-plasmodial activity .
|
-
- HY-18719ES
-
|
Cytochrome P450
Estrogen Receptor/ERR
Drug Metabolite
Parasite
|
Cancer
|
Endoxifen-d5 is the deuterium labeled Endoxifen. Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen has the potential for breast cancer study .
|
-
- HY-B0141AR
-
Alfatradiol(Standard); Epiestradiol(Standard); Epiestrol (Standard)
|
Reference Standards
5 alpha Reductase
Endogenous Metabolite
Bacterial
|
Inflammation/Immunology
|
Alpha-Estradiol (Standard) is the analytical standard of Alpha-Estradiol. This product is intended for research and analytical applications. Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.
|
-
- HY-W653896
-
|
Isotope-Labeled Compounds
Androgen Receptor
Apoptosis
Topoisomerase
Estrogen Receptor/ERR
|
Infection
|
Alternariol-d2 is deuterium labeled Alternariol. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .
|
-
- HY-N6714R
-
|
Reference Standards
Topoisomerase
Androgen Receptor
Estrogen Receptor/ERR
Apoptosis
|
Infection
Cancer
|
Alternariol (Standard) is the analytical standard of Alternariol. This product is intended for research and analytical applications. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .
|
-
- HY-13757S
-
ICI 46474-d3 hydrochloride; (Z)-Tamoxifen-d3 hydrochloride; trans-Tamoxifen-d3 hydrochloride
|
Apoptosis
Estrogen Receptor/ERR
Autophagy
HSP
Isotope-Labeled Compounds
|
Cancer
|
Tamoxifen-d3 hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis .Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .
|
-
- HY-13757R
-
ICI 46474 (Standard); (Z)-Tamoxifen Citrate (Standard); trans-Tamoxifen Citrate (Standard)
|
Reference Standards
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
Tamoxifen (Citrate) (Standard) is the analytical standard of Tamoxifen (Citrate). This product is intended for research and analytical applications. Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis .Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .
|
-
- 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-N7128
-
|
Cytochrome P450
ERK
p38 MAPK
NF-κB
MMP
PAI-1
|
Cancer
|
Flavanone is a naturally occurring flavone. Flavanone has inhibitory activity for human estrogen synthetase (aromatase). Flavanone is the inhibitor for ERK/p38/NF-κB signaling pathway. Flavanone exhibits oral activity and antitumor efficacy .
|
-
- HY-163712S
-
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Endocrinology
|
17-Epiestriol-d5-1 is the deuterium labeled 17-Epiestriol (HY-163712). 17-Epiestriol is an estrogen metabolite and a selective estrogen receptor (ER) β agonist. 17-epiestriol inhibits the mRNA and protein expression of the vascular cell adhesion molecule VCAM-1 induced by tumor necrosis factor α (TNFα). 17-epiestriol also inhibits TNFα-induced VCAM-1 expression and prevents NF-κB migration to the nucleus. 17-Epiestriol also induces the mRNA and protein expression of endothelial nitric oxide synthase .
|
-
- HY-B0005A
-
Z-Toremifene; NK 622 free base; FC-1157a free base
|
Estrogen Receptor/ERR
|
Infection
Cancer
|
Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively .
|
-
- HY-A0037
-
CP-336156
|
Estrogen Receptor/ERR
|
Inflammation/Immunology
Cancer
|
Lasofoxifene (CP-336156) is an orally active and selective estrogen receptor modulator (SERM). Lasofoxifene exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene can be used for research of breast cancer and postmenopausal osteoporosis .
|
-
- HY-14248R
-
CGS 20267 (Standard)
|
Cytochrome P450
Reference Standards
Autophagy
|
Cancer
|
Letrozole (Standard) is the analytical standard of Letrozole. This product is intended for research and analytical applications. Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer .
|
-
- 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-D0272
-
|
Estrogen Receptor/ERR
|
Metabolic Disease
|
2,3,4-Trihydroxybenzophenone is a hydroxylated benzophenone UV filter with estrogenic activity. 2,3,4-Trihydroxybenzophenone is a quorum sensing inhibitor and an EC 1.14.18.1 (tyrosinase) inhibitor. 2,3,4-Trihydroxybenzophenone is also a human urinary metabolite, a rat metabolite and a drug metabolite .
|
-
- HY-14248S
-
|
Isotope-Labeled Compounds
Cytochrome P450
Autophagy
|
Cancer
|
Letrozole-d4 (CGS 20267-d4) is the deuterium labeled Letrozole. Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer .
|
-
- HY-19822
-
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 .
|
-
- HY-18719BR
-
|
Cytochrome P450
Reference Standards
Estrogen Receptor/ERR
Drug Metabolite
Parasite
|
Cancer
|
Endoxifen (hydrochloride) (Standard) is the analytical standard of Endoxifen (hydrochloride). This product is intended for research and analytical applications. Endoxifen hydrochloride is a key active metabolite of Tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen hydrochloride has the potential for breast cancer study[1][2].
|
-
- 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 .
|
-
- HY-N0835
-
-
- HY-B0005
-
Z-Toremifene citrate; NK 622; FC-1157a
|
Estrogen Receptor/ERR
Apoptosis
|
Infection
Cancer
|
Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 μM and 2.6 μM, respectively .
|
-
- HY-14590
-
-
- HY-135671
-
|
Aryl Hydrocarbon Receptor
VEGFR
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
AhR modulator-1 (compound 6-MCDF) is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. AhR modulator-1 inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. AhR modulator-1 also possess anti-estrogenic properties in rat uterus .
|
-
- HY-105118A
-
CGS-9343B; KW 5617
|
Calmodulin
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
Zaldaride maleate (CGS-9343B) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride maleate inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM . Zaldaride maleate prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na +, Ca 2+ and K + currents in PC12 cells and inhibits nAChR .
|
-
- HY-N7501R
-
|
Reference Standards
Others
|
Metabolic Disease
Inflammation/Immunology
|
Isoformononetin (Standard) is the analytical standard of Isoformononetin. This product is intended for research and analytical applications. Isoformononetin is an analog of Daidzein (HY-N0019) and has immunoprotective effects. Isoformononetin inhibits the differentiation of Th17 and B-cells lymphopoesis to promote osteogenesis in estrogen-deficient bone loss conditions .
|
-
- HY-A0038
-
CP-336156 tartrate
|
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
Lasofoxifene (CP-336156) tartrate is an orally active and selective estrogen receptor modulator (SERM) . Lasofoxifene tartrate exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene tartrate can be used for the research of breast cancer and postmenopausal osteoporosis .
|
-
- HY-B0845
-
-
- HY-137004
-
Ind-Cl
|
Estrogen Receptor/ERR
COX
|
Inflammation/Immunology
|
Indazole-Cl (Ind-Cl) is an Estrogen receptor (ER)-β-specific agonist with inflammatory effect. Indazole-Cl inhibits cyclooxygenase-2 exression reduction induced by hypoxia. And Indazole-Cl inhibits ROS production. Indazole-Cl also inhibits cell migration and invasion by hypoxia increased by hypoxia. Indazole-Cl is potent inhibitor of hypoxia-induced inflammation in vascular smooth muscle cells (VSMCs) .
|
-
- HY-112746
-
DPC974; GW5638
|
Estrogen Receptor/ERR
|
Cancer
|
Etacstil (GW5638) is a estrogen receptor antagonist that displays minimal uterotropic activity in ovariectomized rats and inhibits the agonist activity of Estradiol (HY-B0141), Tamoxifen (HY-13757A) and Raloxifene (HY-13738) in the environment. Etacstil is promising for research of breast cancer and bone protection .
|
-
- HY-18719
-
|
Estrogen Receptor/ERR
Potassium Channel
|
Cancer
|
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 .
|
-
- HY-W018197
-
-
- HY-105118
-
CGS-9343B free base; KW 5617 free base
|
Calmodulin
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
Zaldaride (CGS-9343B free base) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM . Zaldaride prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na +, Ca 2+ and K + currents in PC12 cells and inhibits nAChR .
|
-
- HY-W699238
-
|
Biochemical Assay Reagents
|
|
S-(-)-Aminoglutethimide D-tartrate is an aromatase inhibitor with activity that blocks adrenal steroidogenesis. S-(-)-Aminoglutethimide D-tartrate can be used to inhibit steroid-related diseases. S-(-)-Aminoglutethimide D-tartrate is often used clinically to control certain types of cancer. S-(-)-Aminoglutethimide D-tartrate effectively reduces testosterone and estrogen levels through an enzyme inhibition mechanism.
|
-
- HY-W116007
-
|
DNA/RNA Synthesis
|
Endocrinology
|
Octamethylcyclotetrasiloxane promotes the anchorage-independent growth of MCF-10A and MCF-10F cells. Octamethylcyclotetrasiloxane induces DNA damage, inhibits the expression of DNA-repairing protein BRCA1 under long-term and high-concentration exposure. Octamethylcyclotetrasiloxane exhibits intrinsic estrogenic activity .
|
-
- HY-N7501S
-
|
Isotope-Labeled Compounds
|
Inflammation/Immunology
|
Isoformononetin-d3 is the deuterium labeled Isoformononetin (HY-N7501). Isoformononetin is an analog of Daidzein (HY-N0019) and has immunoprotective effects. Isoformononetin inhibits the differentiation of Th17 and B-cells lymphopoesis to promote osteogenesis in estrogen-deficient bone loss conditions .
|
-
- HY-150543
-
|
Steroid Sulfatase
|
Cancer
|
Steroid sulfatase-IN-3 (compound 1q) is a potent STS (Steroid sulfatase) inhibitor, with an IC50 of 25.8 nM. Steroid sulfatase-IN-3 shows antiproliferative activity against T-47D estrogen-dependent breast cancer cells, with an IC50 of 1.04 µM .
|
-
- 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-B0005AS
-
Z-Toremifene-d6; NK 622-d6 free base; FC-1157a-d6 free base
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Infection
Cancer
|
Toremifene-d6 is deuterium labeled Toremifene. Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 μM and 2.6 μM, respectively .
|
-
- HY-13636
-
ICI 182780; ZD 9238; ZM 182780
|
Estrogen Receptor/ERR
Autophagy
Apoptosis
|
Cancer
|
Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .
|
-
- HY-135312
-
|
Estrogen Receptor/ERR
PROTACs
|
Cancer
|
AZ'6421 acts as Protcolysis Targeting Chimera (PROTAC) to selectively degrade estrogen receptor alpha. AZ'6421 has a potent anti-tumour effect to inhibit the uncontrolled cellular proliferation which arises from malignant disease. AZ'6421 can be used for the research of cancer such as breast cancer .
|
-
- 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-N7128R
-
|
Cytochrome P450
Reference Standards
ERK
p38 MAPK
NF-κB
MMP
PAI-1
|
Cancer
|
Flavanone (Standard) is the analytical standard of Flavanone. This product is intended for research and analytical applications. Flavanone is a naturally occurring flavone. Flavanone has inhibitory activity for human estrogen synthetase (aromatase). lavanone is the inhibitor for ERK/p38/NF-κB signaling pathway. Flavanone exhibits oral activity and antitumor efficacy .
|
-
- HY-176084
-
|
Aldose Reductase
|
Cancer
|
RJG-2051 is a selective covalent aldo-keto reductase family 1 member C3 (AKR1C3) inhibitor with an IC50 value of 13 nM. RJG-2051 interferes with the metabolic process of substrates such as androgens, estrogens, and prostaglandins by AKR1C3. RJG-2051 is promising for research of cancers .
|
-
- HY-N0250R
-
-
- HY-N1581R
-
Nigakilactone D (Standard)
|
Reference Standards
Parasite
|
Infection
Endocrinology
|
Quassin (Standard) is the analytical standard of Quassin. This product is intended for research and analytical applications. Quassin (Nigakilactone D) is a bioactive triterpenoid from stem bark extract of Quassia amara. Quassin inhibits P. falciparum with an IC50 of 0.15 μM. Quassin possesses reversible antifertility, anti-estrogenic and anti-plasmodial activity .
|
-
- 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 .
|
-
- HY-105184
-
|
Cytochrome P450
|
Endocrinology
|
YM511 is a highly specific non-steroidal aromatase inhibitor. YM511 inhibits aromatase activities in microsomes from rat ovary and human placenta competitively (IC50s of 0.4 and 0.12 nM, respectively). YM511 slightly inhibits production of other steroid hormones. YM511 has the potential for suppressing estrogen-dependent action research without affecting serum levels of other steroid hormones .
|
-
- HY-172783
-
|
Cytochrome P450
Apoptosis
|
Cancer
|
Aromatase-IN-5 (Compound 10) is a potent inhibitor of aromatase with an IC50 value of 0.06 μM. Aromatase-IN-5 effectively blocks estrogen production. Aromatase-IN-5 inhibits the proliferation of breast cancer cell lines like MCF-7, arrests the cell cycle at the G1 phase, and induces apoptosis. Aromatase-IN-5 is promising for research of breast cancer .
|
-
- HY-121779
-
2,4'-DDE; 2,4-Dichlorodiphenyldichloroethylene; 2,4'-DDE; o,p'-Dichlorodiphenyldichloroethylene
|
Insecticide
|
Endocrinology
|
o,p'-DDE (2,4-Dichlorodiphenyldichloroethylene) is a metabolite and degradation product of the organochlorine pesticide DDT. It accumulates in smallmouth buffalo, channel catfish, and largemouth bass, and in sediments from DDT manufacturing plants around the Huntsville Spring Branch-Indian Creek tributary system, where it is considered a persistent organic pollutant (POP). o,p'-DDE inhibits estrogen binding to the rainbow trout estrogen receptor (rtER) with an IC50 value of 3.2 μM. It induces concentration-dependent estradiol secretion in co-cultures of granulosa and theca cells isolated from porcine follicles. In ovo exposure to o,p'-DDE increases follicular degeneration and reduces testis size in Japanese medaka (O. latipes).
|
-
- HY-N10403
-
4-Hydroxy-17β-estradiol
|
Drug Metabolite
Endogenous Metabolite
|
Cancer
|
4-Hydroxyestradiol (4-Hydroxy-17β-estradiol) is an endogenous metabolite of Estradiol (HY-B0141). 4-Hydroxyestradiol is carcinogenic and shows mutagenic activity in breast epithelial cells. 4-Hydroxyestradiol inhibits the binding of Estradiol to the estrogen receptor in a competitive manner, with a Ki of 0.48 nM .
|
-
- HY-B0005S1
-
Z-Toremifene-d6 hydrochloride; NK 622-d6 hydrochloride; FC-1157a-d6 hydrochloride
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Infection
|
Toremifene-d6 (Z-Toremifene-d6) hydrochloride is deuterium labeled Toremifene. Toremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively .
|
-
- HY-B0005S
-
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
Apoptosis
|
Infection
Cancer
|
Toremifene-d6 (citrate) is the deuterium labeled Toremifene citrate. Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 μM and 2.6 μM, respectively .
|
-
- HY-W142080
-
α-Methyltryptophan
|
mTOR
Autophagy
Apoptosis
Amino Acid Derivatives
|
Metabolic Disease
Cancer
|
α-Methyl-DL-tryptophan (α-Methyltryptophan), a tryptophan derivative, is a selective SLC6A14 blocker. In estrogen receptor (ER)-positive breast cancer cells, α-Methyl-DL-tryptophan inhibits mTOR and activates autophagy and apoptosis. α-Methyl-DL-tryptophan also has the effect of reducing weight .
|
-
- HY-14590R
-
Kempferol(Standard); Robigenin (Standard)
|
Reference Standards
Estrogen Receptor/ERR
Autophagy
Mitophagy
Apoptosis
HIV
Parasite
Endogenous Metabolite
|
Cancer
|
Kaempferol (Standard) is the analytical standard of Kaempferol. This product is intended for research and analytical applications. Kaempferol (Kempferol), a flavonoid found in many edible plants, inhibits estrogen receptor α expression in breast cancer cells and induces apoptosis in glioblastoma cells and lung cancer cells by activation of MEK-MAPK. Kaempferol can be uesd for the research of breast cancer .
|
-
- HY-136092
-
|
Cytochrome P450
|
Neurological Disease
Endocrinology
|
Androsta-1,4,6-triene-3,17-dione is a lipophilic and specific aromatase inhibitor with a Ki of 0.18 μM. Androsta-1,4,6-triene-3,17-dione inhibits estrogen biosynthesis and shows antifertility effects. Androsta-1,4,6-triene-3,17-dione induces impairment of spatial memory .
|
-
- HY-B0005R
-
Z-Toremifene citrate (Standard); NK 622 (Standard); FC-1157a (Standard)
|
Reference Standards
Estrogen Receptor/ERR
Apoptosis
|
Infection
Cancer
|
Toremifene (citrate) (Standard) is the analytical standard of Toremifene (citrate). This product is intended for research and analytical applications. Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively .
|
-
- HY-13636S
-
ICI 182780-d3; ZD 9238-d3; ZM 182780-d3
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
Autophagy
Apoptosis
|
Cancer
|
Fulvestrant-d3 is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .
|
-
- 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 .
|
-
- HY-144699
-
|
Estrogen Receptor/ERR
|
Cancer
|
ERRα antagonist-2 (Compound 11) is a potential ERRα (estrogen related receptor α) inverse agonist with an IC50 of 0.80 μM. ERRα antagonist-2 suppresses the migration and invasion of the ER-negative MDA-MB-231 cell line. ERRα antagonist-2 inhibits breast cancer growth in vivo .
|
-
- HY-N6052
-
|
Estrogen Receptor/ERR
|
Cancer
|
(+)-Medicarpin, a pterocarpan, is a type of isoflavonoid isolated from several medicinal plant species with various biological effects, including Sophora japonica, Zollernia paraensis and Platymiscium yucatamun, Machaerium aristulatum, Platymiscium floribundum, and so on. (+)-Medicarpin potently inhibits osteoclastogenesis and promotes bone healing and increases bone mass by osteoblast differentiation with estrogen receptor (ER) β-mediated osteogenic action .
|
-
- 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-A0036
-
TSE-424 acetate
|
Estrogen Receptor/ERR
|
Cancer
|
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 .
|
-
- 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) .
|
-
- HY-A0031
-
TSE-424
|
Estrogen Receptor/ERR
|
Cancer
|
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 .
|
-
- HY-13636R
-
ICI 182780(Standard); ZD 9238(Standard); ZM 182780 (Standard)
|
Reference Standards
Estrogen Receptor/ERR
Autophagy
Apoptosis
|
Cancer
|
Fulvestrant (Standard) is the analytical standard of Fulvestrant. This product is intended for research and analytical applications. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .
|
-
- HY-B0515B
-
|
Apoptosis
|
Metabolic Disease
Cancer
|
Ibandronate Sodium is an orally active, selective inhibitor of farnesyl pyrophosphate synthase (FPP synthase). Ibandronate Sodium can block the mevalonate pathway to inhibit the isoprenylation modification of small GTPases (such as RAS, RHO family proteins), induce tumor cell apoptosis and inhibit bone resorption. Ibandronate Sodium inhibits tumor cell proliferation (such as ER+ breast cancer cells), promotes the expression of the pro-apoptotic gene FAS, and can produce synergistic anti-tumor effects with anti-estrogen compounds. Ibandronate Sodium is used in the study of osteoporosis and bone metastatic tumors (such as breast cancer bone metastasis) .
|
-
- HY-160264
-
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
PROTAC ER Degrader-12 (Compound 70) is an estrogen receptor PROTAC degrader (DC50: <10 nM), and inhibits MCF-7 proliferation (DC50: <10 nM). PROTAC ER Degrader-12 has anticancer effect. Pink: ER ligand (HY-169978); Blue: E3 ligase ligand (HY-138793); Black: linker (HY-30756) .
|
-
- HY-N0835R
-
-
- HY-W018197R
-
-
- HY-113960
-
|
Estrogen Receptor/ERR
|
Cancer
|
ERRα antagonist-1 (Compound A) is a selective and high affinity agonist for estrogen-related receptor α (ERRα). ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively .
|
-
- HY-174231
-
|
EGFR
Apoptosis
|
Cancer
|
EGFR-IN-163 (Compound 13) is a competitive epidermal growth factor receptor (EGFR) inhibitor (IC50=0.079 μM, selective for HER-2 inhibition). EGFR-IN-163 induces tumor cell apoptosis and cell cycle arrest at G₂/M phase. EGFR-IN-163 is promising for research of estrogen receptor-positive (ER+) breast cancer .
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-
- HY-A0031A
-
TSE-424 hydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
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 .
|
-
- HY-122416
-
Lonchocarpol A; Senegalensin
|
BCRP
|
Metabolic Disease
Cancer
|
6,8-Diprenylnaringenin (Lonchocarpol A; Senegalensin), a hop prenylflavonoid, is a inhibitor of breast cancer resistance protein (BCRP/ABCG2). 6,8-Diprenylnaringenin inhibits ABCG2-mediated efflux of Mitoxantrone, and 3H-Methotrexate transport (IC50=0.41 μM) in HEK293 cells. 6,8-Diprenylnaringenin exhibits some estrogenicity, but its potency is less than 1% of that of 8-Prenylnaringenin .
|
-
- HY-W716464
-
-
- HY-135594
-
|
Estrogen Receptor/ERR
|
Metabolic Disease
|
4'-Raloxifene-β-D-glucopyranoside, a metabolite of Raloxifene, is a benzothiophene glucuronidated at the 4' postion. 4'-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 4'-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 4'-Raloxifene-β-D-glucopyranoside, example 5, is extracted from patent US5567820A .
|
-
- HY-16023A
-
EM-652; SCH 57068
|
Estrogen Receptor/ERR
|
Cancer
|
Acolbifene (EM-652), the active metabolite of EM800, is an orally active pure antiestrogen and selective estrogen receptor antagonist. Acolbifene (EM-652) inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM). Acolbifene (EM-652) possesses potent and pure anticarcinogenic properties .
|
-
- HY-151199
-
|
Steroid Sulfatase
|
Endocrinology
Cancer
|
Steroid sulfatase/17β-HSD1-IN-1 is a potent steroid sulfatase and 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) inhibitor with an IC50 value of 28 nM for cellular human steroid sulfatase. Steroid sulfatase/17β-HSD1-IN-1 can be used to research estrogen-dependent diseases .
|
-
- HY-135595
-
|
Estrogen Receptor/ERR
Drug Metabolite
|
Metabolic Disease
|
6-Raloxifene-β-D-glucopyranoside, a derivative of Raloxifene, is a benzothiophene glucuronidated at the 6' postion. 6-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 6-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 6'-Raloxifene-β-D-glucopyranoside, compound Ia, is extracted from patent US5567820A .
|
-
- HY-122359A
-
rel-L-Centchroman; Ormeloxifene
|
Estrogen Receptor/ERR
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
rel-Levormeloxifene (rel-L-Centchroman) is the relative configuration of Levormeloxifene (HY-122359). rel-Levormeloxifene is a selective estrogen receptor modulator (SERM). rel-Levormeloxifene inhibits proliferation of leukemia cells with IC50 about 7 μM, arrests cell cycle at G0/G1 phase, and induces apoptosis. rel-Levormeloxifene induces differentation of myelogenesis leukemia, and enhances ROS production in K562 cells .
|
-
- 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-132205
-
|
Estrogen Receptor/ERR
|
Metabolic Disease
|
DS45500853 is an estrogen-related receptor α (ERRα) agonist. DS45500853 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.80 μM. DS45500853 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM) .
|
-
- HY-143201
-
|
Estrogen Receptor/ERR
|
Metabolic Disease
|
DS20362725 is an estrogen-related receptor α (ERRα) agonist. DS20362725 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.6 μM. DS20362725 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM) .
|
-
- HY-B0515
-
BM-210955; RPR-102289A
|
Apoptosis
|
Metabolic Disease
Cancer
|
Ibandronate Sodium Monohydrate (BM-210955; RPR-102289A) is an orally active, selective inhibitor of farnesyl pyrophosphate synthase (FPP synthase). Ibandronate Sodium Monohydrate can block the mevalonate pathway to inhibit the isoprenylation modification of small GTPases (such as RAS, RHO family proteins), induce tumor cell apoptosis and inhibit bone resorption. Ibandronate Sodium Monohydrate inhibits tumor cell proliferation (such as ER + breast cancer cells), promotes the expression of the pro-apoptotic gene FAS, and can produce synergistic anti-tumor effects with anti-estrogen compounds. Ibandronate Sodium Monohydrate is used in the study of osteoporosis and bone metastatic tumors (such as breast cancer bone metastasis) .
|
-
- 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-A0036R
-
TSE-424 acetate (Standard)
|
Reference Standards
Estrogen Receptor/ERR
|
Cancer
|
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 .
|
-
- 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 .
|
-
- 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-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-168869
-
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
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))
|
-
- HY-107850A
-
Allopregnanediol
|
GnRH Receptor
|
Endocrinology
|
5α-Pregnane-3α,20α-diol (Allopregnanediol) is a derivative of progesterone and is one of the various steroids secreted by the ovaries of rats. 5α-Pregnane-3α,20α-diol can significantly stimulate the release of luteinizing hormone (LH) in castrated rats that have been pre-treated with estrogen, while simultaneously inhibiting the secretion of follicle-stimulating hormone (FSH) .
|
-
- HY-151201
-
|
Steroid Sulfatase
|
Cancer
|
Steroid sulfatase/17β-HSD1-IN-3 (compound 19) is a dual inhibitor of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 (17β HSD1). Steroid sulfatase/17β-HSD1-IN-3 irreversibly inhibits hSTS activity with anIC50 value of 27 nM. Steroid sulfatase/17β-HSD1-IN-3 can be used in the study of endometriosis and other estrogen-dependent diseases .
|
-
- HY-N1940
-
Cycloicaritin
|
Interleukin Related
TNF Receptor
MMP
|
Inflammation/Immunology
Cancer
|
β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties . β-Anhydroicaritin ameliorates the degradation of periodontal tissue and inhibits the synthesis and secretion of TNF-α and MMP-3 in diabetic rats . β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca 2+, and markedly decreases iNOS protein expression .
|
-
- HY-N2168
-
(+)-Pinoresinol 4-O-β-D-glucopyranoside
|
Glycosidase
Estrogen Receptor/ERR
Phosphodiesterase (PDE)
|
Neurological Disease
Metabolic Disease
Cancer
|
Pinoresinol 4-O-β-D-glucopyranoside ((+)-Pinoresinol 4-O-β-D-glucopyranoside) is an orally active α-glucosidase inhibitor, with an IC50 of 48.13 μg/mL. Pinoresinol 4-O-β-D-glucopyranoside binds to estrogen receptors. Pinoresinol 4-O-β-D-glucopyranoside inhibits phosphodiesterase. Pinoresinol 4-O-β-D-glucopyranoside exhibits various activities such as antioxidant, anti-inflammatory, anti-hyperglycemic, hepatoprotective and anti-epileptic effects .
|
-
- HY-151202
-
|
Steroid Sulfatase
|
Cancer
|
Steroid sulfatase/17β-HSD1-IN-4 (compound 37) is a dual inhibitor of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 (17β HSD1). Steroid sulfatase/17β-HSD1-IN-4 irreversibly inhibits hSTS activity with anIC50 value of 63 nM. Steroid sulfatase/17β-HSD1-IN-4 can be used in the study of endometriosis and other estrogen-dependent diseases .
|
-
- HY-170508
-
|
Cytochrome P450
|
Endocrinology
|
Aromatase-IN-4 (Compound 6a) is an aromatase (Aromatase) inhibitor. Aromatase-IN-4 exhibits anticancer activity, with GI50 values of 2.95 μM, 3.35 μM, 2.27 μM, 8.46 nM, and 1.56 μM against the MDAMB-231, MCF-7, A-549, NCI-H23, and A-498 cell lines, respectively . Aromatase-IN-4 effectively blocks aromatase-dependent estrogen production .
|
-
- HY-16023
-
EM-652 hydrochloride; SCH 57068 hydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
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 .
|
-
- HY-120767
-
KLH-2109 choline; OBE-2109 choline
|
GnRH Receptor
|
Inflammation/Immunology
Cancer
|
Linzagolix choline (KLH-2109 choline) is a non-peptide gonadotropin-releasing hormone (GnRH) antagonist with oral activity. Linzagolix choline inhibits the release of endogenous gonadotropins such as luteinizing hormone LH and follicle-stimulating hormone FSH by binding to the GnRH receptor within the pituitary gland. This inhibition results in a reduction in the production of sex hormones such as estrogen and progesterone, which in turn affects the course of sex hormone-dependent diseases. Linzagolix choline can be used in the study of sex hormone-dependent diseases such as endometriosis and uterine fibroids .
|
-
- HY-131586
-
Resogalangin
|
17β-HSD
Estrogen Receptor/ERR
Aldose Reductase
|
Endocrinology
Cancer
|
3,7-Dihydroxyflavone (Resogalangin) is a flavonoid phytoestrogen, which can be isolated from Adenophora species. 3,7-Dihydroxyflavone is a modulator of estrogen receptors and an inhibitor of human progesterone metabolizing enzyme AKR1C1 and fungal 17β-hydroxysteroid dehydrogenase and a redox inhibitor (IC50=0.6 and 6.0 μM, respectively). 3,7-Dihydroxyflavone is a fluorescent binding substrate for human serum albumin (HSA) with excitation wavelengths of 370 nm (pH 7.4) and 350 nm (pH 3.5), respectively, and emission wavelength of 515 nm .
|
-
- HY-128600
-
ERD-308
1 Publications Verification
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
ERD-308 is a potent estrogen receptor (ER) PROTAC degrader. ERD-308 has DC50 values of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells. ERD-308 can inhibit the proliferation of breast cancer cells and exhibits anti-tumor activity. (Pink: Target Protein Ligand (HY-48027); Black: Linker (HY-172643); Blue: VHL Ligand (HY-112078); VHL Ligand+Linker:(HY-172645))
|
-
- HY-129079
-
-
- HY-129619
-
|
SNIPERs
Estrogen Receptor/ERR
|
Cancer
|
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 .
|
-
- HY-170377
-
|
Estrogen Receptor/ERR
Potassium Channel
|
Cancer
|
ER degrader 10 (Compound 51) is a selective, orally active degrader and antagonist for estrogen receptor (ER) with a DC50 of 0.43 nM and an IC50 of 0.56 nM. ER degrader 10 inhibits the proliferation of ER-positive cells with IC50s of 0-15 nM. ER degrader 10 exhibits a weak inhibitory activity against hERG channel with an IC50 >40 μM. ER degrader 10 is blood-brain barrier penetrable with a brain/plasma ratio (Kp) of 3.05. ER degrader 10 exhibits antitumor efficacy in mice model .
|
-
- HY-W014684
-
|
Keap1-Nrf2
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
|
Endocrinology
|
Lilial is a widely used synthetic fragrance and ester in consumer products. Lilial possesses estrogenic activity in vitro. Lilial can induce a toxic effect on mitochondria that causes a decrease in the viability of HaCaT cells. Lilial can increase NRF2 protein level in vitro. Lilial is able to target respiratory chain complexes, inhibit complexes I and II of the electron transport chain, increase the generation of reactive oxygen species, and decrease the level of intracellular ATP. Lilial can induce systemic toxicity in vivo. Lilial induces significant DNA strand breaks .
|
-
- 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-B0515R
-
BM-210955 (Standard); RPR-102289A (Standard)
|
Reference Standards
Apoptosis
|
Cancer
|
Ibandronate Sodium Monohydrate (BM-210955; RPR-102289A) (Standard) is the analytical standard of Ibandronate Sodium Monohydrate (HY-B0515). This product is intended for research and analytical applications. Ibandronate Sodium Monohydrate (BM-210955; RPR-102289A) is an orally active, selective inhibitor of farnesyl pyrophosphate synthase (FPP synthase). Ibandronate Sodium Monohydrate can block the mevalonate pathway to inhibit the isoprenylation modification of small GTPases (such as RAS, RHO family proteins), induce tumor cell apoptosis and inhibit bone resorption. Ibandronate Sodium Monohydrate inhibits tumor cell proliferation (such as ER + breast cancer cells), promotes the expression of the pro-apoptotic gene FAS, and can produce synergistic anti-tumor effects with anti-estrogen compounds. Ibandronate Sodium Monohydrate is used in the study of osteoporosis and bone metastatic tumors (such as breast cancer bone metastasis) .
|
-
- HY-N2168R
-
(+)-Pinoresinol 4-O-β-D-glucopyranoside (Standard)
|
Glycosidase
Reference Standards
Estrogen Receptor/ERR
Phosphodiesterase (PDE)
|
Neurological Disease
Metabolic Disease
Cancer
|
Pinoresinol 4-O-β-D-glucopyranoside (Standard) is the analytical standard of Pinoresinol 4-O-β-D-glucopyranoside (HY-N2168). This product is intended for research and analytical applications. Pinoresinol 4-O-β-D-glucopyranoside is an orally active α-glucosidase inhibitor, with an IC50 of 48.13 μg/mL. Pinoresinol 4-O-β-D-glucopyranoside binds to estrogen receptors. Pinoresinol 4-O-β-D-glucopyranoside inhibits phosphodiesterase. Pinoresinol 4-O-β-D-glucopyranoside exhibits various activities such as antioxidant, anti-inflammatory, anti-hyperglycemic, hepatoprotective and anti-epileptic effects .
|
-
- HY-173178
-
|
Estrogen Receptor/ERR
|
Cancer
|
LNS8801 is an orally active agonist of the G protein-coupled estrogen receptor (GPER). By activating GPER, LNS8801 mediates downstream signaling pathways, such as promoting the production of cyclic adenosine monophosphate (cAMP) and activating the cAMP response element-binding protein (CREB) signaling, thereby exerting anti-tumor activities including inhibiting tumor cell proliferation, inducing cell differentiation, and enhancing tumor immunogenicity. LNS8801 can be used in the research of various cancers (e.g., melanoma, pancreatic cancer, colorectal cancer, lung cancer, etc.) and relevant studies exploring the roles of GPER in normal physiological and pathological processes .
|
-
- HY-W014684R
-
|
Reference Standards
Keap1-Nrf2
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
|
Endocrinology
|
Lilial (Standard) is the analytical standard of Lilial. This product is intended for research and analytical applications. Lilial is a widely used synthetic fragrance and ester in consumer products. Lilial possesses estrogenic activity in vitro. Lilial can induce a toxic effect on mitochondria that causes a decrease in the viability of HaCaT cells. Lilial can increase NRF2 protein level in vitro. Lilial is able to target respiratory chain complexes, inhibit complexes I and II of the electron transport chain, increase the generation of reactive oxygen species, and decrease the level of intracellular ATP. Lilial can induce systemic toxicity in vivo. Lilial induces significant DNA strand breaks .
|
-
- HY-B1234
-
Octyl methoxycinnamate
|
Androgen Receptor
Estrogen Receptor/ERR
Thyroid Hormone Receptor
Cytochrome P450
|
Metabolic Disease
Endocrinology
|
Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo .
|
-
- HY-B1234S
-
|
Cytochrome P450
Thyroid Hormone Receptor
Androgen Receptor
Estrogen Receptor/ERR
Isotope-Labeled Compounds
|
Metabolic Disease
Endocrinology
|
Octinoxate-13C,d3 is the deuterium labeled Octinoxate (HY-W245806). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo .
|
-
- HY-W014589
-
2,4-DTBP
|
Endogenous Metabolite
Fungal
Apoptosis
RAR/RXR
Amyloid-β
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
2,4-Di-tert-butylphenol (2,4-DTBP) is an orally active RXRα activator and a human estrogen receptor ligand with anti-inflammatory and antioxidant activities, which can induce apoptosis in tumor cells. 2,4-Di-tert-butylphenol can activate the RXRα subtype in LXRα/RXRα, PPARγ/RXRα, and hormone receptor β/RXRα. 2,4-Di-tert-butylphenol also has antiviral and antifungal activities and has the potential to inhibit Aβ-induced neurotoxicity. 2,4-Di-tert-butylphenol can be used as an intermediate in the preparation of antioxidants and UV stabilizers, and is also used in the manufacture of drugs and fragrances .
|
-
- 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-W713284
-
|
Isotope-Labeled Compounds
Cytochrome P450
Estrogen Receptor/ERR
Androgen Receptor
Thyroid Hormone Receptor
|
Endocrinology
|
2-Ethylhexyl (E)-3-(4-(methoxy-d3)phenyl)acrylate is the deuterium labeled Octinoxate (HY-B1234). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo .
|
-
- HY-W014589R
-
2,4-DTBP (Standard)
|
Reference Standards
Endogenous Metabolite
Fungal
Apoptosis
RAR/RXR
Amyloid-β
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
2,4-Di-tert-butylphenol (Standard) is the analytical standard of 2,4-Di-tert-butylphenol (HY-W014589). This product is intended for research and analytical applications. 2,4-Di-tert-butylphenol (2,4-DTBP) is an orally active RXRα activator and a human estrogen receptor ligand with anti-inflammatory and antioxidant activities, which can induce apoptosis in tumor cells. 2,4-Di-tert-butylphenol can activate the RXRα subtype in LXRα/RXRα, PPARγ/RXRα, and hormone receptor β/RXRα. 2,4-Di-tert-butylphenol also has antiviral and antifungal activities, and has the potential to inhibit Aβ-induced neurotoxicity. 2,4-Di-tert-butylphenol can be used as an intermediate in the preparation of antioxidants and UV stabilizers, and is also used in the manufacture of pharmaceuticals and fragrances .
|
-
- HY-W014589S
-
2,4-DTBP-d19
|
Isotope-Labeled Compounds
RAR/RXR
Amyloid-β
Fungal
Apoptosis
Endogenous Metabolite
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
2,4-Di-tert-butylphenol-d19 (2,4-DTBP-d19) is the deuterium labeled 2,4-Di-tert-butylphenol (HY-W014589). 2,4-Di-tert-butylphenol (2,4-DTBP) is an orally active RXRα activator and a human estrogen receptor ligand with anti-inflammatory and antioxidant activities, which can induce apoptosis in tumor cells. 2,4-Di-tert-butylphenol can activate the RXRα subtype in LXRα/RXRα, PPARγ/RXRα, and hormone receptor β/RXRα. 2,4-Di-tert-butylphenol also has antiviral and antifungal activities and has the potential to inhibit Aβ-induced neurotoxicity. 2,4-Di-tert-butylphenol can be used as an intermediate in the preparation of antioxidants and UV stabilizers, and is also used in the manufacture of drugs and fragrances .
|
-
- HY-W749327
-
2,4-DTBP-d21
|
Isotope-Labeled Compounds
RAR/RXR
Amyloid-β
Fungal
Apoptosis
Endogenous Metabolite
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
2,4-Di-tert-butylphenol-d21 (2,4-DTBP-d21) is the deuterium labeled 2,4-Di-tert-butylphenol (HY-W014589). 2,4-Di-tert-butylphenol (2,4-DTBP) is an orally active RXRα activator and a human estrogen receptor ligand with anti-inflammatory and antioxidant activities, which can induce apoptosis in tumor cells. 2,4-Di-tert-butylphenol can activate the RXRα subtype in LXRα/RXRα, PPARγ/RXRα, and hormone receptor β/RXRα. 2,4-Di-tert-butylphenol also has antiviral and antifungal activities and has the potential to inhibit Aβ-induced neurotoxicity. 2,4-Di-tert-butylphenol can be used as an intermediate in the preparation of antioxidants and UV stabilizers, and is also used in the manufacture of drugs and fragrances .
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-
- HY-163679
-
|
Estrogen Receptor/ERR
Cytochrome P450
PROTACs
Apoptosis
|
Cancer
|
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))
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-
Cat. No. |
Product Name |
Type |
-
- HY-W699238
-
|
Cell Assay Reagents
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S-(-)-Aminoglutethimide D-tartrate is an aromatase inhibitor with activity that blocks adrenal steroidogenesis. S-(-)-Aminoglutethimide D-tartrate can be used to inhibit steroid-related diseases. S-(-)-Aminoglutethimide D-tartrate is often used clinically to control certain types of cancer. S-(-)-Aminoglutethimide D-tartrate effectively reduces testosterone and estrogen levels through an enzyme inhibition mechanism.
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3833A
-
-
- HY-W142080
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α-Methyltryptophan
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mTOR
Autophagy
Apoptosis
Amino Acid Derivatives
|
Metabolic Disease
Cancer
|
α-Methyl-DL-tryptophan (α-Methyltryptophan), a tryptophan derivative, is a selective SLC6A14 blocker. In estrogen receptor (ER)-positive breast cancer cells, α-Methyl-DL-tryptophan inhibits mTOR and activates autophagy and apoptosis. α-Methyl-DL-tryptophan also has the effect of reducing weight .
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-
- HY-P3833
-
-
- HY-P2413
-
|
Androgen Receptor
Src
|
Others
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Ac-PPPHPHARIK-NH2 (compound S1) is a compound that inhibits the interaction between androgen receptor and Src. It can inhibit the binding of androgen or estrogen-induced receptor and Src in cancer cells, as well as the activation of related signaling pathways, and can also inhibit cell cycle progression and tumor growth.
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-
- 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 .
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-
- HY-P10393
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ERα (295-311)
|
Apoptosis
|
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 .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N9329
-
-
-
- HY-W010062
-
|
Source classification
|
Drug Derivative
Cytochrome P450
Estrogen Receptor/ERR
|
4-Chlorophenylacetic acid is a halogenated phenylacetic acid derivative. 4-Chlorophenylacetic acid is a potent aromatase inhibitor and antagonizes estrogen signaling. 4-Chlorophenylacetic acid can provide carbon and energy for Pseudomonas sp. strain CBS3. 4-Chlorophenylacetic acid is effective against estrogen-induced mammary tumorigenesis .
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-
-
- HY-B0141A
-
-
-
- HY-B1100
-
-
-
- HY-14248
-
-
-
- HY-N6714
-
-
-
- HY-N7501
-
-
-
- HY-W087008
-
-
-
- HY-N3943
-
-
-
- HY-W010062R
-
|
Microorganisms
Source classification
|
Reference Standards
Cytochrome P450
Estrogen Receptor/ERR
Drug Derivative
|
4-Chlorophenylacetic acid (Standard) is the analytical standard of 4-Chlorophenylacetic acid. This product is intended for research and analytical applications. 4-Chlorophenylacetic acid is a halogenated phenylacetic acid derivative. 4-Chlorophenylacetic acid is a potent aromatase inhibitor and antagonizes estrogen signaling. 4-Chlorophenylacetic acid can provide carbon and energy for Pseudomonas sp. strain CBS3. 4-Chlorophenylacetic acid is effective against estrogen-induced mammary tumorigenesis .
|
-
-
- HY-N0250
-
-
-
- HY-N15524
-
-
-
- HY-N12023
-
-
-
- HY-N1581
-
-
-
- HY-B0141AR
-
-
-
- HY-N6714R
-
-
-
- HY-N4121
-
-
-
- HY-N7128
-
-
-
- HY-14248R
-
-
-
- HY-N0835
-
-
-
- HY-14590
-
-
-
- HY-N7501R
-
-
-
- HY-W018197
-
-
-
- HY-N7128R
-
-
-
- HY-N0250R
-
-
-
- HY-N1581R
-
-
-
- HY-N10403
-
-
-
- HY-14590R
-
-
-
- HY-N6052
-
-
-
- HY-N0835R
-
-
-
- HY-W018197R
-
-
-
- HY-122416
-
-
-
- HY-N1940
-
-
-
- HY-N2168
-
-
-
- HY-131586
-
-
-
- HY-N2168R
-
-
-
- HY-B1234
-
-
-
- HY-W014589
-
2,4-DTBP
|
Structural Classification
Monophenols
Microorganisms
Classification of Application Fields
Source classification
Phenols
Metabolic Disease
Endogenous metabolite
Disease Research Fields
|
Endogenous Metabolite
Fungal
Apoptosis
RAR/RXR
Amyloid-β
|
2,4-Di-tert-butylphenol (2,4-DTBP) is an orally active RXRα activator and a human estrogen receptor ligand with anti-inflammatory and antioxidant activities, which can induce apoptosis in tumor cells. 2,4-Di-tert-butylphenol can activate the RXRα subtype in LXRα/RXRα, PPARγ/RXRα, and hormone receptor β/RXRα. 2,4-Di-tert-butylphenol also has antiviral and antifungal activities and has the potential to inhibit Aβ-induced neurotoxicity. 2,4-Di-tert-butylphenol can be used as an intermediate in the preparation of antioxidants and UV stabilizers, and is also used in the manufacture of drugs and fragrances .
|
-
-
- HY-W014589R
-
2,4-DTBP (Standard)
|
Structural Classification
Monophenols
Microorganisms
Source classification
Phenols
Endogenous metabolite
|
Reference Standards
Endogenous Metabolite
Fungal
Apoptosis
RAR/RXR
Amyloid-β
|
2,4-Di-tert-butylphenol (Standard) is the analytical standard of 2,4-Di-tert-butylphenol (HY-W014589). This product is intended for research and analytical applications. 2,4-Di-tert-butylphenol (2,4-DTBP) is an orally active RXRα activator and a human estrogen receptor ligand with anti-inflammatory and antioxidant activities, which can induce apoptosis in tumor cells. 2,4-Di-tert-butylphenol can activate the RXRα subtype in LXRα/RXRα, PPARγ/RXRα, and hormone receptor β/RXRα. 2,4-Di-tert-butylphenol also has antiviral and antifungal activities, and has the potential to inhibit Aβ-induced neurotoxicity. 2,4-Di-tert-butylphenol can be used as an intermediate in the preparation of antioxidants and UV stabilizers, and is also used in the manufacture of pharmaceuticals and fragrances .
|
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0141AS1
-
|
Alpha-Estradiol-d2 is the deuterium labeled Alpha-Estradiol. Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia .
|
-
-
- HY-B2158S
-
|
Chlorotrianisene-d9 is the deuterium labeled Chlorotrianisene. Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood .
|
-
-
- HY-135581S1
-
|
Raloxifene 6-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
|
-
-
- HY-135582S1
-
|
Raloxifene 4'-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 4'-glucuronide. Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
|
-
-
- HY-135582S
-
|
Raloxifene 4'-glucuronide-d4 is deuterated labeled Raloxifene 4'-glucuronide (HY-135582). Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
|
-
-
- HY-19822S3
-
|
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-19822S
-
|
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-13757AS1
-
|
Tamoxifen-d3 is the deuterium labeled Tamoxifen . Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse .
|
-
-
- HY-B0141AS
-
|
Alpha-Estradiol-d3 is the deuterium labeled Alpha-Estradiol. Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.
|
-
-
- HY-W778408
-
|
Tamoxifen- 13C6 (ICI 47699- 13C6) is the 13C-labeled Tamoxifen (HY-13757A). Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER transgenic mouse .
|
-
-
- HY-W774926
-
|
Permethrin-d6 (NRDC-143-d6) is deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide and a high selectively inhibitor of the Mitochondrial complex I, found in sediment and water samples. Permethrin shows estrogenic in vivo and anti-estrogenic activity in vitro. Permethrin also acts as a neurotoxin affecting neuron membranes by prolonging Sodium channel activation. Permethrin decreases resistance to bacterial infections in medaka (Oryzias latipes) .
|
-
-
- HY-18719ES
-
|
Endoxifen-d5 is the deuterium labeled Endoxifen. Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen has the potential for breast cancer study .
|
-
-
- HY-W653896
-
|
Alternariol-d2 is deuterium labeled Alternariol. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .
|
-
-
- HY-13757S
-
|
Tamoxifen-d3 hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis .Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .
|
-
-
- HY-163712S
-
|
17-Epiestriol-d5-1 is the deuterium labeled 17-Epiestriol (HY-163712). 17-Epiestriol is an estrogen metabolite and a selective estrogen receptor (ER) β agonist. 17-epiestriol inhibits the mRNA and protein expression of the vascular cell adhesion molecule VCAM-1 induced by tumor necrosis factor α (TNFα). 17-epiestriol also inhibits TNFα-induced VCAM-1 expression and prevents NF-κB migration to the nucleus. 17-Epiestriol also induces the mRNA and protein expression of endothelial nitric oxide synthase .
|
-
-
- HY-14248S
-
|
Letrozole-d4 (CGS 20267-d4) is the deuterium labeled Letrozole. Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer .
|
-
-
- HY-N7501S
-
|
Isoformononetin-d3 is the deuterium labeled Isoformononetin (HY-N7501). Isoformononetin is an analog of Daidzein (HY-N0019) and has immunoprotective effects. Isoformononetin inhibits the differentiation of Th17 and B-cells lymphopoesis to promote osteogenesis in estrogen-deficient bone loss conditions .
|
-
-
- HY-B0005AS
-
|
Toremifene-d6 is deuterium labeled Toremifene. Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 μM and 2.6 μM, respectively .
|
-
-
- HY-19822S2
-
|
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-B0005S1
-
|
Toremifene-d6 (Z-Toremifene-d6) hydrochloride is deuterium labeled Toremifene. Toremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively .
|
-
-
- HY-B0005S
-
|
Toremifene-d6 (citrate) is the deuterium labeled Toremifene citrate. Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 μM and 2.6 μM, respectively .
|
-
-
- HY-13636S
-
|
Fulvestrant-d3 is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .
|
-
-
- HY-W716464
-
|
Prochloraz-d7 (BTS 40542-d7) is the deuterium labeled Prochloraz (HY-B0845). 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 .
|
-
-
- HY-A0031S2
-
|
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-A0031S
-
|
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-B1234S
-
|
Octinoxate-13C,d3 is the deuterium labeled Octinoxate (HY-W245806). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo .
|
-
-
- HY-W713284
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2-Ethylhexyl (E)-3-(4-(methoxy-d3)phenyl)acrylate is the deuterium labeled Octinoxate (HY-B1234). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo .
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- HY-W014589S
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2,4-Di-tert-butylphenol-d19 (2,4-DTBP-d19) is the deuterium labeled 2,4-Di-tert-butylphenol (HY-W014589). 2,4-Di-tert-butylphenol (2,4-DTBP) is an orally active RXRα activator and a human estrogen receptor ligand with anti-inflammatory and antioxidant activities, which can induce apoptosis in tumor cells. 2,4-Di-tert-butylphenol can activate the RXRα subtype in LXRα/RXRα, PPARγ/RXRα, and hormone receptor β/RXRα. 2,4-Di-tert-butylphenol also has antiviral and antifungal activities and has the potential to inhibit Aβ-induced neurotoxicity. 2,4-Di-tert-butylphenol can be used as an intermediate in the preparation of antioxidants and UV stabilizers, and is also used in the manufacture of drugs and fragrances .
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- HY-W749327
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2,4-Di-tert-butylphenol-d21 (2,4-DTBP-d21) is the deuterium labeled 2,4-Di-tert-butylphenol (HY-W014589). 2,4-Di-tert-butylphenol (2,4-DTBP) is an orally active RXRα activator and a human estrogen receptor ligand with anti-inflammatory and antioxidant activities, which can induce apoptosis in tumor cells. 2,4-Di-tert-butylphenol can activate the RXRα subtype in LXRα/RXRα, PPARγ/RXRα, and hormone receptor β/RXRα. 2,4-Di-tert-butylphenol also has antiviral and antifungal activities and has the potential to inhibit Aβ-induced neurotoxicity. 2,4-Di-tert-butylphenol can be used as an intermediate in the preparation of antioxidants and UV stabilizers, and is also used in the manufacture of drugs and fragrances .
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