NVS-BPTF-1

NVS-BPTF-1 is a potent and selective small molecule ligand for the bromodomain of Bromodomain and PHD Finger-containing Protein (BPTF). BPTF is a critical scaffolding subunit of the Nucleosome Remodeling Factor (NURF) complex, which regulates gene expression by sliding nucleosomes on DNA. While NVS-BPTF-1 itself often shows limited anti-tumor activity as a standalone inhibitor, it has been utilized as a high-affinity targeting ligand in the development of proteolysis-targeting chimeras (PROTACs). These BPTF degraders have demonstrated therapeutic potential in SWI/SNF-mutant lung cancers, including small cell lung cancer (SCLC) and non-small cell lung cancer (NSCLC), by disrupting NURF complex stability and chromatin binding.