Description
SGC-iMLLT is a first-in-class chemical probe and a potent, selective inhibitor of MLLT1/3-histone interactions with an IC 50 of 0.26 µM. SGC-iMLLT shows high binding activity towards MLLT1 YEATS domain (YD) and MLLT3 YD (AF9/YEATS3) with K d s of 0.129 and 0.077 µM, respectivelyIn VivoSGC-iMLLT shows moderate metabolic resistance with t 1/2 of 53 min and 48 % remaining after 60 min, and the primary process for metabolism is N demethylation. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:IC50: 0.26 µM (MLLT1 YD), Kd: 0.077 µM (MLLT3 YD), 0.129 µM (MLLT1 YD)