PLX-3618 is characterized as a molecular glue that facilitates the degradation of BRD4 with a DC50 of 12.2 nM. It achieves this by promoting the polyubiquitination and subsequent proteasomal degradation of BRD4 through the recruitment of the E3 ligase substrate receptor, DCAF11. This compound has demonstrated the ability to inhibit the proliferation of various cancer cells, induce apoptosis in acute myeloid leukemia cells, and show antitumor activity in mouse models.
- Functions as a molecular glue.
- Promotes degradation of BRD4.
- Inhibits proliferation of various cancer cells.
- Induces apoptosis in acute myeloid leukemia cells.
- Exhibits antitumor activity in mouse models.