MI-136 can specifically inhibit the menin-MLL interaction. It inhibits DHT-induced of androgen receptor (AR) target genes.
MI-463 is a potent inhibitor of Menin-MLL interaction with an IC50 value of 15.3 nM.
MI-503 is a potent and selective Menin-MLL inhibitor with IC50 of 14.7 nM. It shows pronounced growth suppressive activity in a panel of human MLL leukemia cell lines(GI50 at 250 nM-570 nM range), but only a minimal effect in human leukemia cell lines without MLL translocations.
EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM.
OICR-9429 is a potent antagonist of the interaction of WDR5 with peptide regions of MLL and Histone 3 and reduces viability of acute myeloid leukemia cells in vitro. It binds to WDR5 with high affinity (KD = 93 ± 28 nM.
I-BRD9 (GSK602) is a potent and selective BRD9 inhibitor with pIC50 of 7.3, while it displayed a pIC50 of 5.3 against BRD4.
SirReal2 is a potent and selective Sirt2 inhibitor with IC50 of 140 nM.
PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM.