MLL

Revumenib (SNDX-5613) is a potent and selective oral inhibitor of menin-KMT2A interaction with Ki of 0.149 nM and IC50 between 10 and 20 nM, which can be used in the study of acute leukemia with MLL gene rearrangement.

Menin-MLL inhibitor MI-2 (MI2) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.

Menin-MLL inhibitor 4 has antitumor activity.Menin-MLL inhibitor 4 is an inhibitor of Menin- MLL (mixed-lineage leukemia protein) interaction .

Menin-MLL inhibitor 34 (Compound 37) is a selective and potent inhibitor of Menin-MLL, exhibiting an IC50 of 18.21 nM against Menin. This compound effectively reduces Menin protein levels and downregulates MEN1 transcription, demonstrating sustained anti-leukemia effects.

M‑89 is a Highly Potent Inhibitor of the Menin-Mixed Lineage Leukemia (Menin-MLL) Protein−Protein Interaction (Kd = 1.4 nM; IC50 = 25nM). M-89 binds to menin with a Kd value of 1.4 nM and effectively engages cellular menin protein at low nanomolar concentrations. M-89 inhibits cell growth in the MV4;11 and MOLM-13 leukemia cell lines carrying MLL fusion with IC50 values of 25 and 55 nM, respectively, and demonstrates >100-fold selectivity over the HL-60 leukemia cell line lacking MLL fusion.

(1s,4s)-Menin-MLL Inhibitor-23, an enantiomer of Menin-MLL Inhibitor-23 (Example 99A), functions as an inhibitor of the menin-MLL interaction [1].

Menin-MLL inhibitor 26 is a Menin-MLL inhibitor. Menin-MLL inhibitor 26 also is an active reference. Menin-MLL inhibitor 26 can inhibits cell growth. Menin-MLL inhibitor 26 can be used for the research of leukemia .

Menin-MLL inhibitor 27 effectively inhibits the interaction between Menin and MLL, serving as a potential tool in cancer research, particularly for acute myeloid leukemia (AML) [1].

Menin-MLL Inhibitor 29 (Compound C1) is a Menin-MLL protein-protein interaction (PPI) inhibitor that demonstrates high affinity to Menin with a dissociation constant (K D) of 138 nM and impedes Menin's interaction with Menin-binding motif 1 (MBM1), as evidenced by an inhibition constant (IC 50) of 46 nM. Additionally, it exhibits anti-proliferative activity against HepG2 and Hep3B hepatoma cell lines with IC 50 values of 0.31 μM and 0.71 μM, respectively, and has been shown to inhibit tumor growth [1].

Menin-MLL inhibitor 20 is an irreversible inhibitor of the menin-MLL interaction, exhibiting antitumor activities.

Menin-MLL inhibitor 31 (compound 18) effectively disrupts the menin-MLL interaction, demonstrating a potent IC 50 value of 4.6 nM [1].

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).

NVS-MLLT-1 is a selective inhibitor of YEATS domain of MLLT1 and MLLT3.

MIV-6R inhibits Menin-MLL interaction (IC50: 56 nM) and can be used to study leukemia.

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

MM-102 (HMTase Inhibitor IX) is a potent inhibitor of WDR5 MLL interaction with IC50 of 2.4 nM and Ki of less than 1 nM in a WDR5 binding assay. MM-102 can also specifically inhibit cell growth and induce apoptosis in leukemia cells carrying MLL1 fusion protein.

OICR-9429 is a potent antagonist of the interaction that WDR5 effect with peptide regions of MLL and Histone 3. It reduces the viability of acute myeloid leukemia cells in vitro.

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.

MI-538 is an interaction between menin and MLL fusion proteins inhibitor(IC50 of 21 nM).

BRD4-IN-4 is a selective BRD4 inhibitor with an IC50 value of 6.83 μM for BRD4.BRD4-IN-4 selectively inhibits the proliferation of the MV4-11 cell line and arrests the cells in G1 phase.BRD4-IN-4 can be used to study MLL leukemias.

M-89, a highly potent and specific inhibitor of the menin-mixed lineage leukemia (Menin-MLL) protein-protein interaction, exhibits a Kd of 1.4 nM for menin binding. This compound holds potential for treating MLL leukemia.

MM-589 is a potent WD repeat domain 5 (WDR5) inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.

MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and a modulator of mixed lineage leukemia (MLL) protein-protein interaction.

OICR-0547 is a closely related derivative of OICR-9429. OICR-9429 is a novel small-molecule Wdr5-MLL interaction antagonist.