2. Signaling Pathways
  3. Vitamin D Related/Nuclear Receptor
  4. Estrogen Receptor/ERR
  5. ERβ Isoform
  6. ERβ Degrader

ERβ Degrader

ERβ Degraders (7):

Cat. No. Product Name Effect Purity
  • HY-176955
    ER degrader 12
    		Degrader
    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-149295
    PROTAC ERα Degrader-4
    		Degrader 99.06%
    PROTAC ERα Degrader-4 (Compound ZD12) is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER+ breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.
  • HY-161740
    PHTPP-1304
    		Degrader 99.96%
    PHTPP-1304 is a PHTPP-based autophagy targeting chimera (AUTOTAC). PHTPP-1304 induces the degradation of estrogen receptor ERβ through the autophagy pathway, rather than ubiquitination (DC50 ≈ 2 nM, in HEK293T cells; < 100 nM in ACHN renal carcinoma and MCF-7 breast cancer cells). PHTPP-1304 can induce the self-oligomerization of p62. PHTPP-1304 can be used to study various cancers mediated by ERβ.
  • HY-125263
    OP-1074
    		Degrader 99.77%
    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-163679
    PROTAC ERα Degrader-9
    		Degrader
    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 Ki 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-7EGFR (IC50=0.075 μM), MCF-7D538G (IC50=0.31 μM), MCF-7Y537S (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-180850
    ERB-2
    		Degrader
    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.
  • HY-174870
    PROTAC ERα Degrader-11
    		Degrader
    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)).