Description
An inhibitor of the YEATS domain-containing proteins MLLT1 and MLLT3; binds to the MLLT1 YEATS1 and MLLT3 YEATS3 domains (Kds = 129 and 77 nM, respectively); selective for YEATS1 and -3 over YEATS2 and -4 (IC50s = >10 µM), as well as a panel of 48 bromodomains at 50 µM; inhibits histone H3.3 interactions with MLLT3 (IC50 = 400 nM in a reporter assay); decreases expression of MYC and DDN in MV-4-11 leukemia cells at 1 µM