Estrogen Receptor/ERR Degrader

PROTAC ERα Degrader-10 is an orally active estrogen receptor α (ERα) PROTAC degrader, with DC₅₀ values of 0.37, 1.1, and 0.47 nM in MCF7, T47D, and CAMA-1 cells, respectively. PROTAC ERα Degrader-10 exhibits significant anti-tumor activity both in vitro and in vivo, and can be used for breast cancer research.

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.

PROTAC ER Degrader-12 (Compound 70) is an estrogen receptor PROTAC degrader (DC₅₀: <10 nM), and inhibits MCF-7 proliferation (DC₅₀: <10 nM). PROTAC ER Degrader-12 has anticancer effect.

ER degrader 7 is an estrogen receptor α (ERα) degrader and a tubulin (tubulin) inhibitor. ER degrader 7 inhibits the cell viability of various cancer cell lines. ER degrader 7 disrupts the microtubule network in breast cancer cells, induces G2/M phase cell cycle arrest, and exhibits concentration-dependent accumulation in Tamoxifen-resistant LCC2 cells. ER degrader 7 suppresses tumor growth in vivo without causing body weight loss. ER degrader 7 can be applied in studies related to breast cancer.

ERα degrader 13 is an orally active, methylene blue-Raloxifene (HY-13738) conjugated photoactivatable ERα degrader with a K_d value of 27.1 nM. Upon irradiation at 660 nm, ERα degrader 13 generates ROS and heat near the ligand-binding domain of ERα, triggering oxidation, residue unfolding, and ERα degradation via the ubiquitin-proteasome system. ERα degrader 13 inhibits cancer cell proliferation and induces tumor regression in breast cancer xenograft models. ERα degrader 13 can be used in breast cancer-related research.

ER degrader 13 (Compound 37) is an estrogen receptor (ER) degrader. ER degrader 13 has a significant inhibitory effect on the proliferation of ER-positive breast cancer MCF-7 cells.

CV2a is a 14-3-3-directed molecular glue-based PROTAC that selectively targets the ERα protein complex with an EC₅₀ of 0.10 μM. CV2a cooperatively recruits VHL to the 14-3-3/ERα complex and promotes robust polyubiquitination of the 14-3-3ζ/ERα complex.

PROTAC ERα Degrader-9 is a dual-target degrader of estrogen receptor α (ERα) and aromatase (ARO/CYP19A), with a K_i value of 0.25 μM against human ERα and an IC₅₀ value of 4.6 μM against human ARO. PROTAC ERα Degrader-9 degrades ERα and ARO via the ubiquitin-proteasome system, and inhibits the transcriptional activity of ERα and the enzymatic activity of ARO. PROTAC ERα Degrader-9 selectively inhibits cancer cell proliferation, induces cell cycle arrest, and triggers apoptosis. PROTAC ERα Degrader-9 exhibits antiproliferative activity and ERα-degrading activity against cancer cells carrying ERα mutations. PROTAC ERα Degrader-9 can be used in cancer-related research such as breast cancer.

PROTAC ERα Degrader-7 (compound i-320) is a potent estrogen receptor alpha(ERα) PROTAC degrader with a DC₅₀ value of 0.000006 µM. PROTAC ERα Degrader-7 comprises a cereblon-binding moiety LBM linked to a ligand ERBM that binds ERα and comprises a benzofused partially saturated 6-membered carbocyclic or heterocyclic ring.

NEP168 is an ERα PROTAC degrader designed based on the GID4 E3 ligase. NEP168 can be used for the study of breast cancer.

Arg-TERRα is a mini-PROTAC targeting ERRα. Arg-TERRα induces ERRα degradation via the N-end rule pathway, thereby in inhibiting the proliferation and migration of MCF7 breast cancer cells. Arg-TERRα can be used for breast cancer research.

ER degrader 6 (compound 35s) is a potent Estrogen Receptor (ER)α degrader. ER degrader 6 disrupts the microtubule network by restraining tubulin polymerization. ER degrader 6 suppresses tumor growth without noticeable poisonousness.

ERB-2 is a selective ERβ PROTAC degrader. ERB-2 removes the inhibitory effect of ERβ on ROS, leading to the accumulation of ROS, mitochondrial damage, and ultimately triggering cell apoptosis (apoptosis). ERB-2 significantly inhibits tumor growth in the nude mouse model of NCI-H1975OR tumors. ERB-2 can be used for the study of non-small cell lung cancer.

ER degrader 5 is a potent estrogen receptor (ER) degrader. ER degrader 5 shows anti-proliferation activity. ER degrader 5 can be used for the research of breast 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.

ERD-1233 is an orally active ERα PROTAC degrader with a DC₅₀ of 0.9 nM. ERD-1233 exhibits plasma stability and microsomal stability across multiple species, and shows no significant inhibitory effect on major cytochrome P450 subtypes and hERG channels. ERD-1233 inhibits tumor growth and degrades ERα protein levels in xenograft tumor models, with favorable biosafety. ERD-1233 can be used in breast cancer-related research.

ERα degrader 10 is a selective and orally active estrogen receptor α (ERα) degrader. ERα degrader 10 exhibits potent ERα binding affinity (IC₅₀ of 24.0 nM) and degradation ability (EC₅₀ of 5.3 nM). ERα degrader 10 degrades ERα through the proteasome-mediated pathway. ERα degrader 10 can be used for the study of breast cancer.

PROTAC HDAC6/ERα degrader 1 is a dual-target PROTAC that targets HDAC6/ERα, with DC₅₀ values of 1.21 μM (HDAC6), 0.28 μM (ERα) in MCF-7 cells and 0.67 μM (HDAC6), 0.14 μM (ERα) in LCC2 cells, respectively. PROTAC HDAC6/ERα degrader 1 selectively degrades ERα and HDAC6 via the proteasomal pathway, inhibits the transcriptional activation of ERα and blocks the estrogen signaling pathway. PROTAC HDAC6/ERα degrader 1 inhibits the function of HDAC6, attenuates hormone responses, and disrupts autophagy-lysosome function. PROTAC HDAC6/ERα degrader 1 induces cell cycle arrest, apoptosis and ferroptosis, and exhibits antiproliferative activity in breast cancer cells. PROTAC HDAC6/ERα degrader 1 can be used for breast cancer research.

GNE-1567 is a potent ERα PROTAC degrader and a XIAP antagonist with a K_d of 0.03 μM. GNE-1567 induces ubiquitination and degradation of ERα by recruiting the E3 ubiquitin ligase XIAP, thereby achieving the dual effects of ERα protein elimination and abrogation of XIAP-mediated apoptosis inhibition simultaneously. GNE-1567 can be used in studies related to ERα-dependent breast cancer.

ERα/RAD51 degrader 1 is a ERα and RAD51 HyT degrader as well as an apoptosis (Apoptosis) inducer. ERα/RAD51 degrader 1 induces conformational changes in helices 11-12 of ERα, promotes the recruitment of Hsp70, and drives the degradation of ERα and RAD51 via the ubiquitin-proteasome pathway. ERα/RAD51 degrader 1 downregulates the expression of BRCA1/2. ERα/RAD51 degrader 1 acts on tamoxifen (HY-13757A)-sensitive and tamoxifen-resistant breast cancer in both in vitro and in vivo models. ERα/RAD51 degrader 1 is applicable to breast cancer-related research (hydrophobic tag: (HY-B0402)).