Estrogen Receptor/ERR Degrader

Imlunestrant-d₄ (LY-3484356-d₄) is the deuterated-labeled Imlunestrant (HY-145572). 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).

ER ligand-2 (Ligands for Target Protein for Compound 24) is the ligand of ER. ER ligand-2 can be used for synthesis PROTAC ER Degrader-11 (HY-168270).

ER degrader 9 is a bifunctional estrogen receptor degrader that mediates ER protein degradation in MCF7 cells.

His-TERRα is a ERRα PROTAC degrader. His-TERRα uses a single amino acid (His) as the E3 ligand and employs the N-end rule pathway to induce the degradation of the target protein, significantly reducing the molecular size, and thus is called a mini-PROTAC. His-TERRα significantly inhibits the proliferation and migration of MCF7 breast cancer cells. His-TERRα can be used for the study of breast 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.

ER degrader 4 is a selective and orally active estrogen receptor degrader. ER degrader 4 has anti-tumor activity.

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)).

Tamoxifen-PEG-Clozapine is a ERα PROTAC degrader. Tamoxifen-PEG-Clozapine induces ubiquitination and degradation of ERα protein. Tamoxifen-PEG-Clozapine mediates ERα degradation by utilizing UBR5 as a component of the ubiquitin-proteasome system. Tamoxifen-PEG-Clozapine exhibits anticancer activity against breast cancer. Tamoxifen-PEG-Clozapine can be used in the research of breast cancer.

PROTAC ER Degrader-11 (Example 26-1) is a potent PROTAC ER degrader, with the IC₅₀ of 0.66 nM. PROTAC ER Degrader-11 plays an important role in cancer research.

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.

ZN-c5 hydrochloride is a selective and orally active estrogen receptor degrader. ZN-c5 hydrochloride 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 hydrochloride inhibits tumor growth in MCF-7 mouse xenograft model and WHIM20 xenograft model. ZN-c5 hydrochloride can be used for the study of breast cancer.

LSZ-102 (Standard) is the analytical standard of LSZ-102 (HY-111486). This product is intended for research and analytical applications. LSZ-102 is a potent, orally bioavailable, selective estrogen receptor degrader (SERD) with an IC₅₀ value of 0.2 nM.

PROTAC ERα Degrader-2 (Standard) is the analytical standard of PROTAC ERα Degrader-2 (HY-111846). This product is intended for research and analytical applications. PROTAC ERα Degrader-2 (Compound 11) is a ERα PROTAC degrader. PROTAC ERα Degrader-2 significantly down-regulates the level of ERα in MCF-7 cells.(Pink: AR ligand (HY-43962), Blue: IAP Ligand (HY-177389), Black: Linker (HY-128833)).

Giredestrant (Standard) (GDC-9545 (Standard); RG6171 (Standard)) is the analytical standard of Giredestrant (HY-109176). This product is intended for research and analytical applications. Giredestrant (GDC-9545) is an orally active, full, selective Estrogen receptor α (ERα) degrader and antagonist with a DC₅₀ of 0.03 nM. Giredestrant promotes the degradation of ERα protein, including the ESR1^Y537S mutant ERα. Giredestrant reduces uterine wet weight in immature rats and induces a low cuboidal phenotype in their endometrial epithelium. Giredestrant induces tumor regression in both ESR1^Y537S mutant and wild-type ERα tumor models. Giredestrant can be used for the research of ER⁺ breast cancer.