UNC6535

UNC6535 is a potent and reversible ligand for the SETDB1 tri-Tudor domain (3TD), with an IC50 value of 3.4 μM. It simultaneously occupies the TD2 and TD3 reader binding sites. UNC6535 exhibits weak inhibitory effects on SETDB1 methyltransferase activity, with an IC50 of 84 μM for the full-length protein. Additionally, UNC6535 shows a lack of selectivity for the 3TD and may also interact with the SET domain.