Product Description: UNC6535 is a potent and reversible SETDB1 triple Tudor domain (3TD) ligand, with an IC50 of 3.4 µM. UNC6535 occupies simultaneously both the TD2 and TD3 reader binding sites. UNC6535 weakly inhibits SETDB1 methyltransferase activity, with an IC50 of 84 µM for the full-length protein. UNC6535 lacks selectivity for the 3TD and may also interact with the SET domain[1].
Formula: C25H44N6O2
References: [1]Uguen M, et, al. Potent and selective SETDB1 covalent negative allosteric modulator reduces methyltransferase activity in cells. Nat Commun. 2025 Feb 24;16(1):1905.
Molecular Weight: 460.66
Research Area: Cancer
Target: Histone Methyltransferase