mllt1

SGC-iMLLT is a potent and selective MLLT1/3-histone interactions inhibitor(IC50 = 0.26 μM),and is a first-in-class chemical probe displaying cellular target engagement of MLLT1(Kd = 0.129 μM) and MLLT3(Kd = 0.077 μM).

PROTAC MLLT1 Degrader-1 is a PROTAC degrader that specifically targets MLLT1. It effectively inhibits the proliferation and activity of AML cells and suppresses tumor growth in human AML xenograft models. Additionally, it can block oncogenic transcription programs. PROTAC MLLT1 Degrader-1 is employed in research related to MLL-rearranged acute myeloid leukemia (AML).

PFI-6N is the negative control compound for PFI-6. By methylating the amide group of PFI-6, PFI-6N is rendered completely inactive against YEATS domains (MLLT1/3 and YEATS2/4).

PFI-6 is a selective and non-cytotoxic probe targeting the YEATS domain of MLLT1 (ENL/YEATS1) and MLLT3 (AF9/YEATS3), with IC50 values of 140 nM for MLLT1 and 160 nM for MLLT3. It serves as a molecular tool to investigate the role of MLLT1/3 in diseases and genome validation studies [1].