Catalog No.: PC-21848Not For Human Use, Lab Use Only.
GNE-0011 is a monovalent, JQ1-based BRD4 degrader that is not linked to an E3 ligase binder, triggers proteasomal and ubiquitin-dependent selective degradation of BRD4 over BRD2 and BRD3.
GNE-0011 is a monovalent, JQ1-based BRD4 degrader that is not linked to an E3 ligase binder, triggers proteasomal and ubiquitin-dependent selective degradation of BRD4 over BRD2 and BRD3.
GNE-0011 shows low nanomolar inhibition of c-Myc in cells (IC50 = 2 nM).
GNE-0011 shows anticance efficacy in a mouse xenograft model (EOL-1) at low doses (3 mg/kg QD IP).
The mechanism by which this monovalent pan-BET binder leads to selective BRD4 degradation is not fully understood.
