mll-r

CCI 007 is a selective inhibitor of MLL-r, CALM-AF10 and SET-NUP214 leukemia with IC50 of 3.5 uM against MLL-r leukemia cell line PER-485

SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM); selectively kill mixed lineage leukemia cells.

CCI-006, a selective inhibitor and chemosensitizer for MLL-rearranged leukemia cells, disrupts mitochondrial respiration. This action leads to irreversible mitochondrial depolarization and triggers a pro-apoptotic unfolded protein response in specific MLL-r leukemia cells.

Revumenib (also known as SNDX-5613) is an effective and selective Menin-MLL inhibitor. It is primarily used for the study of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML).

MS2133 is a DOT1L PROTAC degrader. It facilitates the ubiquitination and degradation of DOT1L in THP-1 and MV4-11 cells, with DC50 values of 56 nM and 25 nM, respectively, and reduces H3K79 methylation. MS2133 also inhibits the growth of MLL-r leukemia cells, demonstrating anticancer activity.

AF9/ENL-DOT1L/AF4 PPI-IN-1 is a potent inhibitor of protein-protein interactions (PPI) between AF9/ENL and the histone methyltransferase DOT1L/AF4. It effectively inhibits the interactions of AF9-DOT1L (IC50= 1.5 μM), AF9-AF4 (IC50= 1 μM), and ENL-AF4 (IC50= 1.2 μM). This compound suppresses the expression of MLL target genes, Myc and Meis1, and selectively blocks the proliferation of MLL-r and other leukemia cells. In a mouse model of MLL-r leukemia, AF9/ENL-DOT1L/AF4 PPI-IN-1 demonstrates significant antitumor activity with no notable toxicity. It is a useful agent for studying MLL-r leukemia.