GNE-987 (E1664-GRP)

GNE-987 is a BRD4-degradating PROTAC consisting of BRD4B1 and BRD4B2 (BRD4 bromodomains 1 and 2) and the VHL E3-ubiquitin ligase. It exhibits BRD4 degradation activity with DC50 of 0.03 nM for the EOL-1 AML cell line. GNE-987 inhibits cell proliferation and induces apoptosis by promoting the rapid and sustained degradation of BRD4 and inhibiting its downstream targets. It also demonstrates potent antitumor activity in AML cell lines.