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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 µM), as well as a panel of 48 bromodomains at 50 µM. 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 µM.
WARNING This product is not for human or veterinary use.
1. Discovery of an MLLT1/3 YEATS domain chemical probe. Angew. Chem. Int. Ed. Engl. 57(50), 16302-16307 (2018).