Description: PFI-1 (PF-6405761), a specific BET (bromodomain-containing protein) inhibitor for BRD4, is with the IC50 of 0.22 µM in a cell-free assay. Target: Autophagy, Apoptosis, Epigenetic Reader Domain. Smiles: COc1ccccc1S(=O)(=O)Nc1ccc2NC(=O)N(C)Cc2c1. References: Fish PV, et al. J Med Chem, 2012, 55(22),...

Bromodomains recognize acetylated lysine residues and recruit regulatory complexes to acetylated nucleosomes, thereby controlling chromatin structure and gene expression. The isolated individual or tandem bromodomains of bromodomain-containing protein (BRD) 2 and BRD4 bind acetylated histone tails, which couples...

Solid. Soluble in DMSO. MPI_5a is a potent selective inhibitor of HDAC6. HDAC6 is a predominantly cytoplasmic enzyme that targets alpha-tubulin, cortactin and heat shock protein 90, and other substrates. MPI-5a has an IC50 of 36nM in tumour cell models and inhibits the acetylation of tubulin in cells with an IC50...

PFI-1 is an inhibitor of BET bromodomains (BRDs) that prevents the association of BET with histones, it acts as an acyl-lysine (Kac) mimetic inhibitor, binding the Kac site of BRD2 and BRD4. PFI-1 exhibits anti-inflammatory and anticancer activities. In H202-treated bronchial epithelial cells, PFI-1 decreases...