QCA570

QCA570 is an exceptionally potent small-molecule Proteolysis-Targeting Chimera (PROTAC) designed to induce the degradation of Bromodomain-containing protein 4 (BRD4) and other members of the Bromodomain and Extra-Terminal (BET) family. Developed by researchers at the University of Michigan, QCA570 functions by recruiting the Cereblon (CRBN) E3 ubiquitin ligase to the BET proteins, leading to their ubiquitination and subsequent proteasomal degradation. It exhibits picomolar to low nanomolar degradation potency, with a DC50 of approximately 1 nM in various cancer cell lines. By eliminating the BRD4 protein rather than merely inhibiting its bromodomains, QCA570 effectively suppresses the transcription of critical oncogenic drivers such as c-MYC and EZH2. Preclinical studies have demonstrated its lethal activity against multiple malignancies, including bladder cancer and acute myeloid leukemia (AML), where it induces robust apoptosis and cell cycle arrest.