Search Result

Results for "

ERα Inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	17β-HSD (1) Androgen Receptor (2) Apoptosis (13) Aryl Hydrocarbon Receptor (1) Bacterial (1) Caspase (1) COX (1) Cytochrome P450 (4) Deubiquitinase (2) Drug Metabolite (1) Environmental Pollutants (1) Estrogen Receptor/ERR (67) FATP (1) Glycosidase (1) Histone Acetyltransferase (2) Histone Demethylase (1) HSP (1) IAP (2) Isotope-Labeled Compounds (5) LDLR (1) Ligands for E3 Ligase (1) MDM-2/p53 (1) Microtubule/Tubulin (1) NF-κB (2) NOD-like Receptor (NLR) (1) Parasite (1) Phospholipase (1) Pregnane X Receptor (PXR) (1) PROTACs (8) Reference Standards (3) RET (1) Smo (1) SNIPERs (1) Sodium Channel (1) Src (2) Steroid Sulfatase (1) TNF Receptor (1) TRP Channel (1)
By Research Areas:	Cancer (71) Endocrinology (7) Infection (1) Inflammation/Immunology (2) Metabolic Disease (5) Neurological Disease (3)

By Targets:

17β-HSD (1)

Androgen Receptor (2)

Apoptosis (13)

Aryl Hydrocarbon Receptor (1)

Bacterial (1)

Caspase (1)

COX (1)

Cytochrome P450 (4)

Deubiquitinase (2)

Drug Metabolite (1)

Environmental Pollutants (1)

Estrogen Receptor/ERR (67)

FATP (1)

Glycosidase (1)

Histone Acetyltransferase (2)

Histone Demethylase (1)

HSP (1)

IAP (2)

Isotope-Labeled Compounds (5)

LDLR (1)

Ligands for E3 Ligase (1)

MDM-2/p53 (1)

Microtubule/Tubulin (1)

NF-κB (2)

NOD-like Receptor (NLR) (1)

Parasite (1)

Phospholipase (1)

Pregnane X Receptor (PXR) (1)

PROTACs (8)

Reference Standards (3)

RET (1)

Smo (1)

SNIPERs (1)

Sodium Channel (1)

Src (2)

Steroid Sulfatase (1)

TNF Receptor (1)

TRP Channel (1)

By Research Areas:

Cancer (71)

Endocrinology (7)

Infection (1)

Inflammation/Immunology (2)

Metabolic Disease (5)

Neurological Disease (3)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Art. -Nr.	Produktname	Target	Forschungsgebiete	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-A0036

Bazedoxifene acetate 15+ Cited Publications 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-A0031

Bazedoxifene 15+ Cited Publications TSE-424	Estrogen Receptor/ERR	Neurological Disease 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-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-15483

DY131 3 Publications Verification GSK 9089	Estrogen Receptor/ERR Smo	Endocrinology Cancer
DY131 (GSK 9089) is a potent and selective ERRγ and ERRβ agonist. DY131displays inactive against ERRα, ERα and ERβ . DY131 also inhibits Smo signaling .

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-103450

G36	Estrogen Receptor/ERR	Endocrinology Cancer
G-36 is a cell-permeable nonsteroidal antagonist of the G protein-coupled estrogen receptor (GPER/GPR30), which selectively inhibits estrogen-mediated PI3K activation through GPER, rather than Erα. G-36 also inhibits estrogen-mediated calcium mobilization (IC₅₀=112 nM). G-36 is promising for research in the field of cancer .

HY-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-126109

(±)-8-Prenylnaringenin	Estrogen Receptor/ERR Apoptosis	Metabolic Disease Endocrinology Cancer
(±)-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 .

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-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-W036120

Benzophenone-2 2,2′,4,4′-Tetrahydroxybenzophenone	Environmental Pollutants Glycosidase Estrogen Receptor/ERR Pregnane X Receptor (PXR)	Metabolic Disease Endocrinology
Benzophenone-2 (2,2',4,4'-Tetrahydroxybenzophenone) is an organic ultraviolet absorber that is widely used in personal care products and industrial products such as plastics and coatings. Benzophenone-2 is an endocrine disruptor that can interfere with estrogen receptors (ERα receptor) and pregnane X receptor (PXR receptor) activity, leading to reproductive toxicity, immune disorders, and metabolic abnormalities. Benzophenone-2 can inhibit the activity of α-glucosidase (IC₅₀ = 49.72 μM), and can be used for research on diabetes .

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-N4121

Isocurcumenol 1 Publications Verification	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-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-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-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-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-150601

Estrogen receptor-IN-1 1 Publications Verification	Estrogen Receptor/ERR	Metabolic Disease
Estrogen receptor-IN-1 (compound 16) is a potent estrogen receptor (ER) inhibitor with IC₅₀s of 13, 5µM for ERα and Erβ, respectively .

HY-129619

SNIPER(ER)-87	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-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-A0031A

Bazedoxifene hydrochloride 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-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-A0036R

Bazedoxifene acetate (Standard) 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-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-19498

WAY-204688 SIM-688	NF-κB	Inflammation/Immunology
WAY-204688 is an estrogen receptor (ER-α) selective, orally active inhibitor of NF-κB transcriptional activity with an IC₅₀ of 122 ± 30 nM for NF-κB-luciferase (NF-κB-luc) in HAECT-1 cells.

HY-168869

Tamoxifen-PEG-Clozapine	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-131404

TPBM 2 Publications Verification	Estrogen Receptor/ERR	Cancer
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 .

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-111484A

GDC-0927 Racemate SRN-927 Racemate	Estrogen Receptor/ERR	Cancer
GDC-0927 Racemate (SRN-927 Racemate) is an estrogen receptor (ER) degrader that can effectively inhibit the activity of *ER-α* with an IC₅₀ value of 0.2 nM and can be used in diseases related to estrogen receptors.

HY-125263

OP-1074	Estrogen Receptor/ERR	Cancer
OP-1074, a pure anti-estrogen drug, is a selective ER degrader (PA-SERD) with specific anti-estrogenic activity against ERα and ERβ, inhibiting 17β-estradiol (E2)-stimulated transcription with IC₅₀ values of 1.6 and 3.2 nM, respectively.

HY-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-175348

XB2M54	Ligands for E3 Ligase IAP NOD-like Receptor (NLR)	Others Inflammation/Immunology Cancer
XB2M54 is a selective XIAP antagonist. XB2M54 inhibits NOD2-mediated inflammatory signaling. XB2M54 is an E3 ligase ligand. XB2M54 can be used for synthesis of PROTAC ERα Degrader-1 (HY-112098) .

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-168205

HSP90-IN-33	HSP Apoptosis	Cancer
HSP90-IN-33 (compound 24e) is a potent Hsp90 inhibitor with K_d values of ≥200, 7.3 µM for Hsp90α, Hsp90β, respectively. HSP90-IN-33 induces apoptosis and cell cycle arrest at G0/G1 phase. HSP90-IN-33 decreases the protein expression of ERα, CDK4 and Akt .

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-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-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-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-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-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-163679

PROTAC ERα Degrader-9	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 K_i of 0.25 μM, inhibits ARO with an IC₅₀ of 4.6 μM. PROTAC ERα Degrader-9 inhibits the proliferation of MCF-7 wildtype (IC₅₀=0.54 μM) and ERα mutants MCF-7 ^EGFR (IC₅₀=0.075 μM), MCF-7 ^D538G (IC₅₀=0.31 μM), MCF-7 ^Y537S (IC₅₀=2.3 μM), downregulates the expressions of ERS1 and MYC. PROTAC ERα Degrader-9 arrests the cell cycle at G2/M, induces apoptosis in MCF-7. PROTAC ERα Degrader-9 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-163680); Black: linker (HY-W007559); Blue: ligand for E3 ligase (HY-112078))

HY-146424

OBHS	Estrogen Receptor/ERR	Neurological Disease Cancer
OBHS is an estrogen receptor α (ERα) inhibitor. OBHS can also be used as a blowing agent .

HY-164924

ERD-12310A	PROTACs Estrogen Receptor/ERR	Cancer
ERD-12310A is a PROTAC targeting Estrogen Receptor α (ERα) with a ED₅₀ value of 47 pM. ERD-12310A has oral activity. ERD-12310A is composed of PROTAC target protein ligand ER ligand-4 (HY-164925) (red part), E3 ligase ligand (S)-Deoxy-thalidomide (HY-168055) (blue part). ERD-12310A can be used in the research of ER ⁺ breast cancer .

HY-19822S2

Elacestrant-d10 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-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 .

Art. -Nr.	Produktname	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 .

Art. -Nr.	Produktname	Category	Target	Chemical Structure

HY-N0401A

(Z)-Ligustilide 5 Publications Verification	Structural Classification Natürliche Produkte 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-126109

(±)-8-Prenylnaringenin	Structural Classification Flavonoids Humulus lupulus L. Flavonones Plants Moraceae Source Classification	Estrogen Receptor/ERR Apoptosis
(±)-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 .

HY-N4121

Isocurcumenol 1 Publications Verification	other families Classification of Application Fields Terpenoids Sesquiterpenes Plants Disease Research Fields Source Classification Cancer	Estrogen Receptor/ERR Apoptosis
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 .

Art. -Nr.	Produktname	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-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-A0031S

Bazedoxifene-d4

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-A0031S2

Bazedoxifene-d4 acetate

Bazedoxifene-d₄ (acetate) is the deuterium labeled Bazedoxifene[1]. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[2][3].

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