SF2535

SF2535 is a small molecule dual inhibitor of Phosphoinositide 3-kinase (PI3K) and Bromodomain-containing protein 4 (BRD4), developed by Signal Rx Pharma. It is a thieno-pyranone derivative designed to simultaneously target the PI3K/AKT signaling pathway and the epigenetic regulator BRD4. SF2535 exhibits selectivity for the PI3K-delta isoform (IC50 = 27 nM) over other PI3K isoforms and potently inhibits both bromodomains of BRD4. This dual-action approach is intended to suppress MYC activity by both enhancing its degradation (via PI3K inhibition) and blocking its transcription (via BRD4 inhibition). It has been investigated in preclinical models for various cancers, including neuroblastoma and other solid tumors.