PFI-6 is a selective small-molecule chemical probe inhibitor for the YEATS domain of MLLT1 ((ENL/YEATS1)) and MLLT3 (AF9/YEATS3) with IC50 of 140 nM and 160 nM, respectively.
PFI-6 demonstrates good affinity and selectivity for MLLT1/3 over other human YD proteins (YEATS2/4, IC50>30 uM).
PFI-6 exhibits MLLT3 cellular target engagement with IC50 of 0.76 uM in NanoLuciferase Bioluminescent Resonance Energy Transfer (NanoBRET) assays.
PFI-6 exhibits high affinity for YEATS domain of MLLT1 and MLLT3 with Kd values of 82 and 76 nM in ITC assays respectively.
