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

ERα Degrader

ERα Degraders (9):

Cat. No. Product Name Effect Purity
  • HY-133017
    Amcenestrant
    		Degrader 99.79%
    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-168101
    ERα degrader 11
    		Degrader
    ERα degrader 11 (compound B16) is a selective ERα degrader that can be used as an estrogen receptor probe to investigate ER status in ER-positive breast cancer cells.
  • 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-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-157765
    PROTAC ERα Degrader-6
    		Degrader
    PROTAC ERα Degrader-6 (compound A2) is a potent PROTAC degrader of ERα, with IC50 of 0.11 μM in MCE-7 cells. PROTAC ERα Degrader-6 has anti-tumor effect. PROTAC ERα Degrader-6 is a fluorescent probes with Em of 582 nm that enable real-time visualization of ERα protein degradation.
  • HY-149295
    PROTAC ERα Degrader-4
    		Degrader
    PROTAC ERα Degrader-4 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-160562
    PROTAC ERα Degrader-7
    		Degrader
    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.
  • HY-155196
    ER degrader 6
    		Degrader
    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.
  • HY-168099
    ERα degrader 10
    		Degrader
    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.