2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Cytochrome P450
  5. Aromatase/CYP19A1 Isoform
  6. Aromatase/CYP19A1 Degrader

Aromatase/CYP19A1 Degrader

Aromatase/CYP19A1 Degrader (1):

Cat. No. Product Name Effect Purity
  • 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))