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Results for "

ERα breast cancer

" in MedChemExpress (MCE) Product Catalog:

By Targets:	17β-HSD (1) Androgen Receptor (2) Apoptosis (15) Aryl Hydrocarbon Receptor (1) Autophagy (1) Bacterial (1) Bcl-2 Family (3) Biochemical Assay Reagents (1) Caspase (1) Cytochrome P450 (3) Deubiquitinase (2) Drug Metabolite (1) Endogenous Metabolite (1) Environmental Pollutants (2) Estrogen Receptor/ERR (72) FATP (1) Fluorescent Dye (1) Histone Acetyltransferase (2) Histone Demethylase (1) Histone Methyltransferase (1) IAP (2) IFNAR (1) Insecticide (3) Isotope-Labeled Compounds (7) Large Tumor Suppressor (LATS) (1) LDLR (1) Ligands for Target Protein for PROTAC (1) MDM-2/p53 (1) Microtubule/Tubulin (2) NF-κB (1) Parasite (4) Phospholipase (1) PROTACs (11) Reference Standards (1) Ser/Thr Kinase (1) Sodium Channel (1) Src (2) Steroid Sulfatase (1) TNF Receptor (1) TRP Channel (2)
By Research Areas:	Cancer (81) Endocrinology (1) Infection (4) Metabolic Disease (4) Neurological Disease (1)
Click Chemistry:	Tetrazine (1)

Inhibitors & Agonists

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: BCRP BRK

Cat. No.	Nombre del producto	Target	Áreas de investigación	Chemical Structure

HY-19822

Elacestrant Maximum Cited Publications 17 Publications Verification 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-N0401A

(Z)-Ligustilide 5 Publications Verification	Bacterial Estrogen Receptor/ERR FATP	Infection Metabolic Disease Cancer
(Z)-Ligustilide is extracted from Ligusticum chuanxiong Hort, has antimicrobial and antifungal activity, exhibits an average antifungal score of 5.6 . (Z)-Ligustilide is orally active, it inhibits the expression of FATP5 and DGAT, inhibits fatty acid uptake and esterification in mice and has potential as therapeutics for nonalcoholic fatty liver disease (NAFLD) . (Z)-Ligustilide is also able to reactivate ERα, has epigenetic regulation, and is used in the study of tamoxifen-resistant breast cancer .

HY-B0723

Ospemifene 2 Publications Verification FC-1271a	Estrogen Receptor/ERR Caspase	Neurological Disease Endocrinology Cancer
Ospemifene (FC-1271a) is an orally active and non-estrogenic selective estrogen receptor modulator (SERM) with K_i values of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene inhibits caspase-3 activity. Ospemifene inhibits neuronal degeneration, prevents bone loss, and increases vaginal weight and vaginal epithelial height. Ospemifene has anticancer activity against breast cancer .

HY-B0412

Estriol 5 Publications Verification Oestriol	Estrogen Receptor/ERR Endogenous Metabolite	Cancer
Estriol (Oestriol), an orally active estrogen, is a *ERα* and ERβ agonist. Estriol is a potent GPR30 antagonist in estrogen receptor-negative breast cancer cells. Estriol can ameliorate disease severity through immunomodulatory mechanisms that decrease tissue inflammation. Estriol has powerful proconvulsant effects .

HY-19822A

Elacestrant dihydrochloride Maximum Cited Publications 17 Publications Verification 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-147165

VT02956 1 Publications Verification	Ser/Thr Kinase Large Tumor Suppressor (LATS)	Cancer
VT02956 is a LATS inhibitor (IC₅₀: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids . VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-150505

DC-U4106 1 Publications Verification	Deubiquitinase Apoptosis	Cancer
DC-U4106 is a USP8 targeting inhibitor with the K_dvalue of 4.7 μM and the IC₅₀ value of 1.2 μM. DC-U4106 can target the ubiquitin pathway and facilitate the degradation of *Erα. DC-U4106 inhibits tumor growth with minimal toxicity and has the potential for the research of breast* cancer .

HY-153468

ErSO-TFPy TEQ103; Sera2	Sodium Channel TRP Channel	Cancer
ErSO-TFPy (TEQ103) is an ERα+ tumor cell inhibitor with low nanomolar cytotoxic activity against ERα+ breast cancer cells. ErSO-TFPy activates the sodium channel TRPM4, causes an imbalance of intracellular calcium and sodium ions. ErSO-TFPy dysregulates calcium homeostasis in ERα+ tumor cells, triggers the anticipatory unfolded protein response, and induces rapid immune cell-independent necrotic cell death. ErSO-TFPy can be used for the research of estrogen receptor alpha positive breast cancer .

HY-162312

LLK203	Deubiquitinase Apoptosis	Cancer
LLK203 is a potent USP2/USP8 dual-target inhibitor with IC₅₀s of 0.89 μM and 0.52 μM, respectively. LLK203 leads a degradation of ERα and induces apoptosis of breast cancer MCF-7 cells. LLK203 demonstrates antitumor activities against the 4T1 tumor mice model .

HY-12825

BHPI	Estrogen Receptor/ERR Phospholipase	Cancer
BHPI is a nuclear receptor *ERα* inhibitor. BHPI activates PLCγ and UPR. BHPI has antitumor activity against breast, endometrial, and ovarian cancers .

HY-16023A

Acolbifene 2 Publications Verification 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-103457

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

HY-137144

Fulvestrant-3-boronic acid ZB716	Estrogen Receptor/ERR	Cancer
Fulvestrant-3-boronic acid is an orally active *ERα* inhibitor, which binds to ERα competitively (IC₅₀ = 4.1 nM) and effectively degrades ERα in breast cancer cells .

HY-149480

ERD-3111	PROTACs Estrogen Receptor/ERR	Cancer
ERD-3111 (Compound 44) is an orally active PROTAC *ERα* degrader (DC₅₀: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer .

HY-159957

BAY-184	Histone Acetyltransferase Estrogen Receptor/ERR
BAY-184 is a selective and orally active KAT6A and KAT6B inhibitor. BAY-184 inhibits KAT6A/KAT6B activity with an IC₅₀ of 71 nM and 83 nM. respectively BAY-184 inhibits *ERα* transcriptional activity. BAY-184 inhibits proliferation of diverse breast cancer subtypes, and inhibits tumor growth .

HY-145341

GNE-149	Estrogen Receptor/ERR	Cancer
GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC₅₀=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer .

HY-149295

PROTAC ERα Degrader-4	PROTACs Estrogen Receptor/ERR Apoptosis	Cancer
PROTAC ERα Degrader-4 (Compound ZD12) is a highly potent and selectivePROTAC *ERα* degrader (K_i: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER ⁺ breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.

HY-175785

X15695	Estrogen Receptor/ERR Aryl Hydrocarbon Receptor Apoptosis MDM-2/p53	Cancer
X15695 is selective and orally active estrogen receptor (ERα) degrader. X15695 is an aryl hydrocarbon receptor (AHR) ligand. X15695 enables AHR to form a complex with the ERα, promoting its proteasomal degradation. X15695 inhibits the breast cancer cells proliferation, promotes cell cycle block and induces apoptosis. X15695 can be used for the study of breast cancer .

HY-107835

Flumethrin FCR 2769	Environmental Pollutants Apoptosis Bcl-2 Family Parasite Insecticide	Infection Cancer
Flumethrin (FCR 2769) is a pyrethroid insecticide and acaricide . Flumethrin targets voltage-gated sodium channels and estrogen receptor α (ERα). Flumethrin induces cytotoxicity, apoptosis, genotoxicity and DNA damage in breast cancer cells by regulating the expression of BCL2, BAX, TP53 and P21 genes. Flumethrin is applicable to relevant studies on ectoparasite infections (tick and flea burdens) in dogs and cats, as well as breast cancer .

HY-177445

KAT6-IN-4	Histone Acetyltransferase Estrogen Receptor/ERR	Cancer
KAT6-IN-4 (Compound Example 2) is a selective lysine acetyltransferase 6 (KAT6) inhibitor. KAT6-IN-4 suppresses transcription of oncogenes like ERα. KAT6-IN-4 demonstrates potent antitumor efficacy in ER ⁺/HER2 ^- breast cancer xenografts. KAT6-IN-4 is promising for research of KAT6-driven malignancies (e.g., breast cancer, NSCLC) .

HY-163561

CARM1-IN-6	Histone Methyltransferase Estrogen Receptor/ERR IFNAR	Cancer
CARM1-IN-6 is a potent CARM1 inhibitor that inhibits CARM1 enzymatic activity with an IC₅₀ of 12.3 μM and a K_d of 0.6785 μM. CARM1-IN-6 suppresses oncogenic estrogen/ERα-target gene expression, activates type I interferon (IFN) and IFN-induced genes (ISGs), induces cell cycle arrest, and inhibits breast cancer cell proliferation both in vitro and in vivo. CARM1-IN-6 can be used for the research of breast cancer .

HY-W008581

Estradiol 3-methyl ether 3-O-Methyl estradiol; 17β-Estradiol 3-methyl ether; 3-Methoxyestradiol	Biochemical Assay Reagents TRP Channel Microtubule/Tubulin Autophagy	Metabolic Disease Cancer
Estradiol 3-methyl ether (EDME) is a highly selective TRPML1 ion channel antagonist and microtubule (microtubule) depolymerizing agent, with IC₅₀ values of 0.22 μM and 3.8 μM against TRPML1 and TRPML2, respectively; it shows no activity against TRPML3. Estradiol 3-methyl ether induces the disruption of cytoplasmic microtubule networks in mammalian cells, with an EC₅₀ of 9 μM. Independent of estrogen receptors, Estradiol 3-methyl ether blocks autophagy (autophagy), TFEB nuclear translocation, and inhibits the migration and invasion of triple-negative breast cancer cells by suppressing TRPML1. Estradiol 3-methyl ether is applicable for relevant research on triple-negative breast cancer .

HY-18719S

Endoxifen-d5 (Z-isomer)	Isotope-Labeled Compounds Cytochrome P450 Estrogen Receptor/ERR Drug Metabolite Parasite	Cancer
Endoxifen-d₅ (Z-isomer) is the deuterium labeled Endoxifen (Z-isomer) (HY-18719). Endoxifen (Z-isomer) is an oral active Tamoxifen (HY-13757A) metabolite, inducing an anti-estrogenic effect in breast cancer cells expressing ERα. Endoxifen (Z-isomer) inhibits hERG. This effect is concentration-dependent, with an IC₅₀ value of 1.6 μM .

HY-179433

PROTAC AR Degrader-12	PROTACs Androgen Receptor Estrogen Receptor/ERR Src	Cancer
PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS). PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer .

HY-174453

PROTAC ERα Degrader-12	PROTACs Estrogen Receptor/ERR Apoptosis	Cancer
PROTAC ERα Degrader-12 is a potent and selective Erα PROTAC degrader. PROTAC ERα Degrader-12 has antiproliferative effects in multiple breast cancer cell lines with wild-type or mutant ERα. PROTAC ERα Degrader-12 can halt the cell cycle and induce cell apoptosis. PROTAC ERα Degrader-12 exhibits excellent antitumor and ERα degradation activity. PROTAC ERα Degrader-12 can be used for research on breast cancer. (Pink: ER ligand-11 (HY-174475); Blue: VHL ligand (HY-112078); Black: Linker (HY-W088749); VHL ligand + Linker ( HY-W998310)) .

HY-176955

ER degrader 12	Estrogen Receptor/ERR	Cancer
ER degrader 12 (Example 1) is an estrogen receptor (ER) degrader with IC₅₀ values for *ERα* and ERβ of 2.3 and 80.2 nM respectively (TR-FRET experiment). ER degrader 12 inhibits the proliferation of MCF-7 cells, with an IC₅₀ of 1.53 nM. ER degrader 12 can be used for research on breast cancer .

HY-176225

BY13	PROTACs Src Estrogen Receptor/ERR Apoptosis	Cancer
BY13 is a SRC-3 PROTAC degrader with a DC₅₀ of 0.031 μM. BY13 selectively blocks the ER signaling pathway over that of androgen receptor (AR)) through down-regulating ERα level. BY13 potently overcomes endocrine resistance in breast cancer by inducing cell cycle arrest in G1 phase and apoptosis, with superior effect over Fulvestrant (HY-13636). BY13 significantly inhibits the growth of drug-resistant breast tumors without obvious toxicity in LCC2 xenograft mice model . Pink: SRC-3 ligand (SI-2) (HY-101447); Blue: CRBN ligase ligand (HY-41547); Black: linker (HY-176226)

HY-174870

PROTAC ERα Degrader-11	PROTACs Estrogen Receptor/ERR Apoptosis Fluorescent Dye	Cancer
PROTAC ERα Degrader-11 is a selective and intrinsically fluorescent (Ex: 366 nm, Em: 440 nm) *ERα* PROTAC degrader. PROTAC ERα Degrader-11 shows good antiproliferative activity, selective *ERα* degradation and imaging capabilities in MCF-7 breast cancer cell lines. PROTAC ERα Degrader-11 induces G2/M phase arrest and induces apoptosis in MCF-7 cells. PROTAC ERα Degrader-11 is well-tolerated up to a dose of 500 mg/ kg with no acute toxicity in athymic nude mice. PROTAC ERα Degrader-11 can be used for the study of breast cancer.(Pink: ERα ligand (HY-167701), Blue: CRBN Ligand (HY-150831), Black: Linker, E3 ligase ligand-linker conjugate (HY-174880)) .

HY-126932

TTC-352	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-175448

GNE-1567	PROTACs Estrogen Receptor/ERR IAP	Cancer
GNE-1567 is a potent ERα PROTAC degrader and a selective XIAP antagonist with a K_d value of 0.03 μM. GNE-1567 is indicated for breast cancer research. (Pink: ligand for target protein (HY-18719); Black: linker; Blue: ligand for E3 ligase (HY-175449)) .

HY-19822S

Elacestrant-d4 RAD1901-d₄	Isotope-Labeled Compounds Estrogen Receptor/ERR	Cancer
Elacestrant-d₄ (RAD1901-d₄) is a deuterated labeled Elacestrant (HY-19822). Elacestrant (RAD1901) is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC₅₀ values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER ⁺ breast cancer cell lines both in vitro and in vivo.

HY-174131

PVTX-321	Estrogen Receptor/ERR	Cancer
PVTX-321 (Compound 16a) is an orally active estrogen receptor α (ERα) degrader. PVTX-321 can potently degrade ERα (DC₅₀=0.15 nM in MCF-7 cells) and also has inhibitory activity against mutant ERα (IC₅₀=59 nM). PVTX-321 is promising for research of ER+/HER2- breast cancer .

HY-175260

ZN-c5	Estrogen Receptor/ERR	Cancer
ZN-c5 is a selective and orally active estrogen receptor degrader. ZN-c5 exhibits high potency in the cellular assay (MCF-7, IC₅₀ = 0.3 nM) and binds with high affinity to *ERα* and ERβ (IC₅₀ = 0.4 nM and 0.8 nM, respectively). ZN-c5 inhibits tumor growth in MCF-7 mouse xenograft model and WHIM20 xenograft model. ZN-c5 can be used for the study of breast cancer .

HY-16023

Acolbifene hydrochloride 2 Publications Verification 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-155492

ERα degrader 7	Estrogen Receptor/ERR	Cancer
ERα degrader 7 (compound B1) is a potent *ERα* degrader with an IC₅₀ of 14.6 nM and a DC₅₀ of 9.7 nM, respectively. ERα degrader 7 shows excellent antitumor activity, indicating its potential to evolve as a promising selective estrogen-receptor degrader (SERD) for breast cancer research .

HY-144138

Estrogen receptor antagonist 2	Estrogen Receptor/ERR	Cancer
Estrogen receptor antagonist 2 is a selective estrogen receptor downregulator. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. Estrogen receptor antagonist 2 has the potential for the research of breast cancer diseases (extracted from patent WO2021228210A1, compound 3) .

HY-144137

Estrogen receptor antagonist 1	Estrogen Receptor/ERR	Cancer
Estrogen receptor antagonist 1 is a selective estrogen receptor antagonist. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. Estrogen receptor antagonist 1 has the potential for the research of breast cancer diseases (extracted from patent WO2021249533A1, compound 4) .

HY-132194

ERα degrader-2	Estrogen Receptor/ERR	Cancer
ERα degrader-2 is a selective estrogen receptor degrader (SERD) with potent binding affinity with *ERα* (IC₅₀=17.1 nM), good degradation efficacy (EC₅₀=0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent agentgability, can be used for HER ⁺ breast cancer research .

HY-144070A

(Rac)-ErSO-DFP	Estrogen Receptor/ERR	Cancer
(Rac)-ErSO-DFP is a derivative of ErSO-DFP and a selective small molecule *Erα* biomodulator. (Rac)-ErSO-DFP againsts *ERα+* breast cancer (including resistant tumors) by hyperactiving the Erα-dependent a-UPR (extracted from patent WO2022087234A1) .

HY-123773

SR-16157 NSC 732011; HLX-801	Steroid Sulfatase Estrogen Receptor/ERR	Cancer
SR-16157 (NSC 732011; HLX-801) is a dual-action steroid sulfatase (STS) inhibitor (IC₅₀ = 0.1 uM) and selective *ERα* modulator. SR-16157 exhibits STS inhibitory and anti-estrogenic effects in breast cancer cells. SR-16157 may be used in breast cancer research .

HY-144306

ERα degrader 4	Estrogen Receptor/ERR Apoptosis	Cancer
ERα degrader 4 is an excellent and selective estrogen receptor α (ERα) degrader (IC₅₀ of 0.31, 0.41 and 0.48 μM in MDA-MB-231, MCF-7 and MCF-7/ADR cells, respectively). ERα degrader 4 has potent inhibitory activity against MCF-7 cell lines. ERα degrader 4 is a potential SERDs candidate for the research of breast cancer .

HY-178463

F0840-0093	Estrogen Receptor/ERR	Cancer
F0840-0093 is a highly selective estrogen receptor α (ERα) degrader. F0840-0093 exhibits potent antiproliferative activity against T47D cells with an IC₅₀ value of 4.65 μM. F0840-0093 is promising for research of estrogen receptor-positive (ER+) breast cancer .

HY-179232

ERα antagonist 2	Estrogen Receptor/ERR	Cancer
ERα antagonist 2 (Compound 5b) is an *ER-α* antagonist with an IC₅₀ value of 1729 nM. ERα antagonist 2 exhibits significant inhibitory activity against breast cancer cell lines, and is still effective against ER-negative cells (MDA-MB-231), suggesting the existence of ER-independent pathways. ERα antagonist 2 can be used for the study of breast cancer .

HY-179045

ERα degrader 14	Estrogen Receptor/ERR Apoptosis	Cancer
ERα degrader 14 (Compound B7) is a potent *ERα* degrader. ERα degrader 14 exhibits significantly potent and selective anti-proliferative activity on two ERα-positive breast cancer cell lines (MCF-7 and T47D). ERα degrader 14 induces cell cycle arrest, inhibits cell migration, and induces cell apoptosis. ERα degrader 14 effectively inhibits tumor growth in mouse models. ERα degrader 14 can be used for the study of breast cancer .

HY-172937

ERα degrader 13	Estrogen Receptor/ERR	Cancer
ERα degrader 13 (compound MR3) is potent *ERα* degrader with an IC₅₀ of 0.55 μM. ERα degrader 13 induces an obvious tumor regression in the breast cancer xenograft mouse model .

HY-149081

ERα degrader 6	Estrogen Receptor/ERR Cytochrome P450	Cancer
ERα degrader 6 (Compound 31q) is an *ERα* degrader (K_I: 75 nM). ERα degrader 6 also inhibits ARO with an IC₅₀ of 37.7 nM. ERα degrader 6 inhibits tumor growth in MCF-7 tumor xenograft model. ERα degrader 6 can be used for breast cancer research .

HY-138089

17β-Hydroxy exemestane	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-119418

Desketoraloxifene	Estrogen Receptor/ERR	Cancer
Desketoraloxifene is an estrogen receptors alpha (ERα) activator at an AP-1 site. Desketoraloxifene can be used for the research of osteoporosis and breast cancer .

HY-176486

ER degrader 11	Estrogen Receptor/ERR	Cancer
ER degrader 11 (Compound 5) is an orally active, brain-penetrant and selective estrogen receptor (ER) degrader (ERα IC₅₀=1.6 nM). ER degrader 11 is promising for research of breast cancer brain metastasis .

HY-114770

(E,E)-GLL398	Estrogen Receptor/ERR	Cancer
(E,E)-GLL398 is a selective estrogen receptor degrader with potent binding activity to ERα (IC₅₀ = 1.14 nM). (E,E)-GLL398 can effectively degrade ERα in MCF-7 breast cancer cells (IC₅₀ = 0.21 μM). The introduced boronic acid group of (E,E)-GLL398 gives it superior oral bioavailability, with an AUC of 36.9 μg·h/mL in rats, which is significantly higher than that of GW7604 .

Cat. No.	Nombre del producto	Target	Research Area

HY-P10843

R4K1	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-P10393

ERα17p 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 .

Cat. No.	Nombre del producto	Target	Research Area	Image

HY-P991578

SNG-8023	Estrogen Receptor/ERR	Cancer
SNG-8023 is an anti-ERα humanized monoclonal antibody. SNG-8023 can be used for cancer research, such as breast cancer .

Cat. No.	Nombre del producto	Category	Target	Chemical Structure

HY-N0401A

(Z)-Ligustilide 5 Publications Verification	Structural Classification Productos naturales Classification of Application Fields Metabolic Disease Dicerothamnus rhinocerotis Umbelliferae Plants Disease Research Fields Source Classification	Bacterial Estrogen Receptor/ERR FATP
(Z)-Ligustilide is extracted from Ligusticum chuanxiong Hort, has antimicrobial and antifungal activity, exhibits an average antifungal score of 5.6 . (Z)-Ligustilide is orally active, it inhibits the expression of FATP5 and DGAT, inhibits fatty acid uptake and esterification in mice and has potential as therapeutics for nonalcoholic fatty liver disease (NAFLD) . (Z)-Ligustilide is also able to reactivate ERα, has epigenetic regulation, and is used in the study of tamoxifen-resistant breast cancer .

HY-B0412

Estriol 5 Publications Verification Oestriol	Monophenols Immune System Disorder Classification of Application Fields Disease markers Phenols Endocrine diseases Endogenous metabolite Disease Research Fields Steroids Cancer Source Classification	Estrogen Receptor/ERR Endogenous Metabolite
Estriol (Oestriol), an orally active estrogen, is a *ERα* and ERβ agonist. Estriol is a potent GPR30 antagonist in estrogen receptor-negative breast cancer cells. Estriol can ameliorate disease severity through immunomodulatory mechanisms that decrease tissue inflammation. Estriol has powerful proconvulsant effects .

Cat. No.	Nombre del producto	Chemical Structure

HY-18719S

Endoxifen-d5 (Z-isomer)
Endoxifen-d₅ (Z-isomer) is the deuterium labeled Endoxifen (Z-isomer) (HY-18719). Endoxifen (Z-isomer) is an oral active Tamoxifen (HY-13757A) metabolite, inducing an anti-estrogenic effect in breast cancer cells expressing ERα. Endoxifen (Z-isomer) inhibits hERG. This effect is concentration-dependent, with an IC₅₀ value of 1.6 μM .

HY-19822S

Elacestrant-d4
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-19822S2

Elacestrant-d10
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-B0723S2

Ospemifene-d5
Ospemifene-d₅ (FC-1271a-d₅) is deuterium labeled Ospemifene. Ospemifene is a non-estrogen selective estrogen receptor modulator (SERM), with K_is of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene can be used for the research of vaginal atrophy and breast cancer .

HY-19822S3

Elacestrant-d6
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-107835S

Flumethrin-d5

Flumethrin-d₅ (FCR 2769-d₅) is the deuterium labeled Flumethrin (HY-107835). Flumethrin (FCR 2769) is a pyrethroid insecticide and acaricide . Flumethrin targets voltage-gated sodium channels and estrogen receptor α (ERα). Flumethrin induces cytotoxicity, apoptosis, genotoxicity and DNA damage in breast cancer cells by regulating the expression of BCL2, BAX, TP53 and P21 genes. Flumethrin is applicable to relevant studies on ectoparasite infections (tick and flea burdens) in dogs and cats, as well as breast cancer .

HY-19822S4

Elacestrant-d5
Elacestrant-d₅ (RAd₁₉01-d₅) is the deuterium labeled Elacestrant (HY-19822). 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 .

Cat. No.	Nombre del producto		Classification