estrogen receptor-alpha (erα)

Alpha-Estradiol (Epiestradiol) is an estrogen that inhibits 5alpha-reductase and has potential in the study of androgenetic alopecia.

MPP dihydrochloride is a highly selective antagonist of estrogen receptor alpha (ERα).

Propyl pyrazole triol (PPT) is a selective agonist of estrogen receptor alpha (ERα), exhibiting a relative binding affinity of 49% for ERα, which is approximately 410 times higher than its affinity for estrogen receptor beta (ERβ: 0.12%).

PAC is a chemical conjugate consisting of an ADCs linker and PROTACs linked to an antibody. When PAC is conjugated to an antibody, it exhibits enhanced degradation of estrogen receptor-alpha (ERα) in comparison to PROTAC alone.

PROTAC ER Degrader-2 serves as a synthesis intermediate for the production of PAC, a compound that incorporates the ADCs linker and PROTACs, which are subsequently conjugated to an antibody. PAC, exhibits a greater capability to degrade estrogen receptor-alpha (ERα) compared to PROTAC (without the presence of an antibody)[1].

PROTAC ER Degrader-3, an intermediate for the synthesis of PAC, specifically compound LP2. PAC serves as the linker for ADCs and PROTACs that are conjugated to an antibody. Notably, when PAC is conjugated to an antibody, it exhibits enhanced degradation of estrogen receptor-alpha (ERα) compared to PROTAC alone [1].

PROTAC ERα Degrader-1 is a chemical compound. It consists of a ubiquitin E3 ligase binding group, a linker, and a protein binding group. This compound serves as a degrader of estrogen receptor-alpha (ERα).

ERα degrader12 (Compound RA3) is an estrogen receptor alpha (ERα) degrader with antitumor properties. It significantly suppresses tumor growth in a xenograft mouse model of breast cancer.

AZD9496 maleate is a highly potent and selective antagonist of the estrogen receptor alpha (ERα), exhibiting an IC50 value of 0.28 nM. This compound, AZD9496 maleate, is an orally bioavailable selective estrogen receptor degrader (SERD).

(Rac)-ErSO-DFP, a derivative of ErSO-DFP, is a selective small molecule that overactivates ERα+-dependent anticipatory unfolded protein responses. It functions as an Erα biomodulator and demonstrates efficacy against anti-estrogen receptor alpha-positive breast cancer, including resistant tumors.

OBHS is an inhibitor of estrogen receptor alpha (ERα).

Estrogen receptor antagonist 2 is a selective down-regulator of the estrogen receptor, with research potential for breast cancer disease. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development.

ERα antagonist 1 is a selective, potent, covalent estrogen receptor alpha (ERα) antagonist that blocks the cell cycle of MCF-7 cells in G0/G1 phase and induces apoptosis.

PROTAC ERα Y537S degrader-1 consists of a ubiquitin E3 ligase binding group, a linker, and a protein binding group, functioning as an estrogen receptor-alpha (ERα) Y537S degrader [1].

PROTAC ERα Degrader-7 (Compound i-320) is a powerful PROTAC degrader targeting the estrogen receptor alpha (ERα), exhibiting a DC50 of 0.000006 µM. This compound consists of a cereblon-binding segment, LBM, connected to ERBM, an ERα-binding ligand that includes a benzofused partially saturated 6-membered carbocyclic or heterocyclic ring [1].