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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
21 Results for "
human ERα
" in MedChemExpress (MCE) Product Catalog:
Products (21)
21 Results for "human ERα" in MCE Product Catalog:
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Prinaberel (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC50s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. Prinaberel induces ovarian cancer apoptosis .
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3 Cited Publications
Cat. No.: HY-18719
CAS No.: 112093-28-4
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Endoxifen Z-isomer is an orally active selective PKCβ1 inhibitor with an IC50 of 360 nM against human PKCβ1. Endoxifen Z-isomer also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. Endoxifen Z-isomer can be used in research related to ER + breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors .
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3 Cited Publications
Cat. No.: HY-18719A
CAS No.: 1032008-74-4
Endoxifen Z-isomer hydrochloride is an orally active selective PKCβ1 inhibitor with an IC50 of 360 nM against human PKCβ1. It also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer hydrochloride binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer hydrochloride inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. It can be used in research related to ER + breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors .
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Cardiovascular Disease Monophenols Neurological Disease Glycine max (L.) merr Phenols Polyphenols Leguminosae Extract Plants Disease Research Fields
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PROTAC ER Degrader-4 is a potent ERα PROTAC degrader, with an IC50 of 0.8 nM against human ERα. PROTAC ER Degrader-4 recruits the VHL E3 ligase to ERα, and triggers the ubiquitination modification and degradation of ERα via the UP/26S proteasome system. PROTAC ER Degrader-4 can be used in related research on breast cancer .
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Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells .
Cat. No.: HY-W1005067
CAS No.: 2191110-79-7
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EN171 is a covalent 14-3-3σ molecular glue ligand that sequesters neonuclear substrates, including BRD4 and BLC6, into the cytoplasm by recruiting 14-3-3σ. EN171 covalently targets C38 and C96 on 14-3-3 to enhance the interaction between 14-3-3 and ERα, YAP, and TAZ (with EC50 values of 9 μM for human ERα, 45 μM for YAP, and 107 μM for TAZ). EN171 inhibits the transcriptional activity of estrogen receptors and the Hippo pathway in breast cancer cells. EN171 can be used in studies related to breast cancer .
Cat. No.: HY-18719S
CAS No.: 1584173-54-5
Cat. No.: HY-126932
CAS No.: 1607819-68-0
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TTC-352 is an orally bioavailable selective human estrogen receptor (ER) α partial agonist (ShERPA). TTC-352 inhibits the growth of three ER+ breast cancer cells. TTC-352 induces tumor regression accompanied by exit of ERα from the nucleus to extranuclear sites .
Cat. No.: HY-175171
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Anticancer agent 276 (Compound 5) is a multi-target anticancer agent. Anticancer agent 276 has a potent anticancer activity against human tumor cells with IC50s of 6.90 and 4.48 μM for HEPG2 and MCF7 cells, respectively. Anticancer agent 276 shows strong and stable interactions across multiple targets, including Topoisomerase II, VEGFR2, c-Met, EGFR and ERα .
Cat. No.: HY-163679
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PROTAC ERα Degrader-9 is a dual-target degrader of estrogen receptor α (ERα) and aromatase (ARO/CYP19A), with a Ki value of 0.25 μM against human ERα and an IC50 value of 4.6 μM against human ARO. PROTAC ERα Degrader-9 degrades ERα and ARO via the ubiquitin-proteasome system, and inhibits the transcriptional activity of ERα and the enzymatic activity of ARO. PROTAC ERα Degrader-9 selectively inhibits cancer cell proliferation, induces cell cycle arrest, and triggers apoptosis. PROTAC ERα Degrader-9 exhibits antiproliferative activity and ERα-degrading activity against cancer cells carrying ERα mutations. PROTAC ERα Degrader-9 can be used in cancer-related research such as breast cancer .
Cat. No.: HY-164924
CAS No.: 3026007-23-5
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ERD-12310A is an orally active ERα PROTAC degrader, with a Ki value of 0.95 nM against human ERα and a DC50 of 47 pM for ERα in MCF-7 cells. ERD-12310A forms a ternary complex with ERα and the CRBN E3 ubiquitin ligase, thereby inducing ubiquitination and proteasomal degradation of wild-type and ESR1 Y537S mutant ERα. ERD-12310A induces tumor regression in ER+ breast cancer xenografts and inhibits tumor growth in ESR1 Y537S mutant breast cancer xenografts. ERD-12310A can be used in studies related to ER-positive breast cancer and ESR1-mutant breast cancer .
Cat. No.: HY-100583AR
CAS No.: 94105-90-5
Cat. No.: HY-123664
CAS No.: 68307-81-3
Synonyms: LY133314
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Trioxifene mesylate (LY133314) is an orally active and selective estrogen receptor (ER) modulator with human ERα IC50 of 203.49 nM and Ki of 20.84 nM. Trioxifene mesylate binds estradiol receptors, inhibits ERα-mediated gene expression, reduces circulating gonadotrophin levels. Trioxifene mesylate can be used for the research of advanced breast cancer and androgen-independent, metastatic prostatic adenocarcinoma .
Cat. No.: HY-121372
CAS No.: 43000-65-3
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Lactandrate is a D-high nitrogen steroid alkylating agent. It can interact with the ligand-binding domain (LBD) of estrogen receptor-alpha (ERα). Lactandrate has a growth inhibitory effect on breast cancer cells, with a GI50 value ranging from 5 to 65 μM. It shows anti-tumor activity in mouse breast tumors (MXT and CD8F1) as well as in human xenograft MX-1 .
Cat. No.: HY-15731S1
CAS No.: 2734920-42-2
Cat. No.: HY-167151
CAS No.: 2107327-36-4
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PaPE-1 is a pathway-preferential estrogen receptor (ER) agonist that preferentially activates ER non-nuclear-initiated signaling while minimally activating nuclear-initiated signaling. PaPE-1 exhibits Ki values of 10 μM and 25 μM for human ERα and ERβ, respectively. The relatively low ER affinity and rapid receptor dissociation of PaPE-1 facilitate the triggering of non-nuclear mTOR/MAPK/AKT signaling, while reducing the recruitment of ERα to chromatin and sustained nuclear ER-dependent transcription. PaPE-1 is suitable for research related to non-nuclear ER signaling, metabolic disorders, ischemic brain injury, Alzheimer's disease, and ER-positive breast cancer .
Synonyms: ent-β-Estradiol; ent-17β-Estradiol; ent-17β-Oestradiol
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Ent-Estradiol is the enantiomer of Estradiol (HY-B0141). Ent-Estradiol is a highly selective estrogen receptor ligand, but does not possess estrogenic activity. Ent-Estradiol displays IC50 values of 24.9 nM, 9.59 nM and 8.17 nM for human, rat and mouse ERβ, and 151 nM, 246 nM and 268 nM for human, rat and mouse ERα, respectively. Ent-Estradiol can be used for the study of menopausal physiological changes .
Cat. No.: HY-135529
CAS No.: 63619-84-1
Synonyms: LY133314 free base
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Trioxifene (LY133314 free base) is an orally active and selective estrogen receptor (ER) modulator with human ERα IC50 of 203.49 nM and Ki of 20.84 nM. Trioxifene binds estradiol receptors, inhibits ERα-mediated gene expression, reduces circulating gonadotrophin levels. Trioxifene can be used for the research of advanced breast cancer and androgen-independent, metastatic prostatic adenocarcinoma .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
