SGC-iMLLT is an inhibitor of the YEATS domain-containing proteins MLLT1 and MLLT3.1 It binds to the MLLT1 YEATS1 and MLLT3 YEATS3 domains (Kds = 129 and 77 nM, respectively).1 It is selective for YEATS1 and -3 over YEATS2 and -4 (IC50s = >10 ?M), as well as a panel of 48 bromodomains at 50 ?M. SGC-iMLLT inhibits the interaction of histone H3.3 with MLLT3 (IC50 = 400 nM in a reporter assay) and decreases expression of the tumorigenic genes MYC and DDN in MV-4-11 leukemia cells when used at a concentration of 1 ?M.
1.Moustakim, M., Christott, T., Monteiro, O.P., et al.Discovery of an MLLT1/3 YEATS domain chemical probeAngew. Chem. Int. Ed. Engl.57(50)16302-16307(2018)