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ER antagonist/degraders

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By Targets:	Apoptosis (2) Bcl-2 Family (1) Caspase (1) CDK (1) Estrogen Receptor/ERR (13) Histone Acetyltransferase (1) IAP (4) Ligands for E3 Ligase (1) NF-κB (1) NOD-like Receptor (NLR) (1) Potassium Channel (1) PROTACs (2) TNF Receptor (1)
By Research Areas:	Cancer (15) Inflammation/Immunology (1)

Targets Recommended: ER-phagy

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-145572

Imlunestrant 1 Publications Verification LY-3484356	Estrogen Receptor/ERR	Cancer
Imlunestrant (LY-3484356) is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC) .

HY-145572A

Imlunestrant tosylate 1 Publications Verification LY-3484356 tosylate	Estrogen Receptor/ERR	Cancer
Imlunestrant (LY-3484356) tosylate is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant tosylate results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant tosylate can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC) .

HY-12870

AZD9496 Maximum Cited Publications 28 Publications Verification	Estrogen Receptor/ERR	Cancer
AZD9496 is an effective, selective estrogen receptor (ERα) antagonist with an IC₅₀ of 0.28 nM. AZD9496 is an orally active, selective estrogen receptor degrader (SERD).

HY-133017

Amcenestrant 3 Publications Verification SAR439859	Estrogen Receptor/ERR	Cancer
SAR439859 (compound 43d) is an orally active, non-steroidal, and selective estrogen receptor degrader (SERD). SAR439859 is an effective ER antagonist with ER degradation activity, an EC₅₀ of 0.2 nM. SAR439859 can show potent anti-tumor effects and limited cross-resistance in ER ⁺ breast cancer.

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-12870A

AZD9496 maleate Maximum Cited Publications 28 Publications Verification	Estrogen Receptor/ERR	Cancer
AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC₅₀ of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD).

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-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-175446

GDC-0152-acetamide	IAP Apoptosis	Cancer
GDC-0152-acetamide is a pan-inhibitor of apoptosis protein (IAP) antagonist. GDC-0152-acetamide induces cIAP1/2 autoubiquitination and degradation, activating the non-canonical NF-κB pathway to promote TNF-α secretion and tumor cell apoptosis. GDC-0152-acetamide is promising for research of ERα-positive breast cancer .

HY-170377

ER degrader 10	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-155406

Estrogen receptor modulator 10	Estrogen Receptor/ERR Caspase Bcl-2 Family	Cancer
Estrogen receptor modulator 10 (compound G-5b) is an estrogen receptor (ER) antagonist (IC₅₀=6.7 nM) and degrader (DC₅₀=0.4 nM). Estrogen receptor modulator 10 is developed based on the Fulvestrant (HY-13636) molecule and can rapidly degrade ER receptors through the proteasome pathway. Estrogen receptor modulator 10 can induce cell apoptosis and block cells in the G1/G0 phase and can be used in cancer research .

HY-124627

THIQ 40	Estrogen Receptor/ERR	Cancer
THIQ-40 is a tetrahydroisoquinoline-based, orally active, and selective estrogen receptor ERα degrader (SERD) (IC₅₀=17 nM), with antitumor efficacy. THIQ-40 possesses functional ERα antagonistic activity, promotes ERα degradation and forms stable ERαLBD complexes. THIQ-40 shows the characteristic of rapid racemization in multi-species plasma. THIQ-40 can be widely applied to studies on the relevant mechanisms and drug development of ERα-positive breast cancer .

HY-181345

OP-1690	Estrogen Receptor/ERR	Cancer
OP-1690 is a complete estrogen receptor (ERα) antagonist (CERAN), with pIC₅₀ values of 7.5 and 7.9 in alkaline phosphatase (AP) activity assay and TR-FRET assay, respectively. OP-1690 modulates receptor function by inducing ERα tetramerization, effectively induces ERα degradation, inhibits target gene transcription, but exhibits low antiproliferative potency. OP-1690 can be used for breast cancer research .

HY-182468

OP-3136	Histone Acetyltransferase Estrogen Receptor/ERR CDK	Cancer
OP-3136 is a selective KAT6 inhibitor. OP-3136 reduces the proliferative capacity of cancer cells and inhibits cell growth in ER ⁺ breast cancer cell models with overexpressed KAT6. When combined with ER antagonists/degraders or CDK4/6 inhibitors, OP-3136 exhibits synergistic anti-tumor activity in mouse xenograft models. OP-3136 can be used in studies related to HR ⁺/HER2 ^- breast cancer .

HY-175445

GNE-5472	PROTACs Estrogen Receptor/ERR IAP NF-κB TNF Receptor Apoptosis	Cancer
GNE-5472 is a potent bifunctional ERα PRRTAC degrader, with its E3 ligand being a pan-IAP antagonist. GNE-5472 antagonizes cIAP1/2, activating the non-classical NF-κB pathway, resulting in a significant upregulation of TNFα expression. GNE-5472 inhibits the proliferation of breast cancer cells and induces cell apoptosis. GNE-5472 can be used for the study of breast cancer .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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ER antagonist/degraders

Inhibitors & Agonists