menin and mll interaction

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

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.

VTP50469 is a highly selective and orally active small molecule inhibitor of the Menin-MLL protein-protein interaction with potent anti-leukemic activity with a Ki of 104 pM.

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

ML399 is the menin--MLL interaction inhibitor that demonstrates strong and selective effects in MLL leukemia cells, and ML399 validates a specific mechanism of action by blocking oncogenic menin-MLL signaling, providing a valuable chemical probe for functional genomics and leukemia-targeted therapeutic strategy development while enabling comprehensive mechanistic and translational hematologic cancer research.

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.

VTP50469 fumarate is a highly selective and orally active inhibitor of Menin-MLL interaction (Ki: 104 pM), and has potently anti-leukemia activity.

M-525 binds to menin (IC50: 3 nM) and achieves low nanomolar potencies in cell growth inhibition and in the suppression of MLL regulated gene expression in MLL leukemia cells. M-525 is a first-in-class, highly potent, irreversible, and covalent menin-MLL

Enzomenib is a menin protein inhibitor that disrupts the interaction between menin and mixed lineage leukemia fusion proteins, thereby modulating transcriptional programs driven by MEN gene dysregulation and providing a targeted research tool for mechanistic studies and therapeutic exploration in hematological malignancies associated with menin-dependent oncogenic signaling.

Balomenib is an inhibitor of the menin-MLL interaction, effectively blocking the men1-MLL4-43 interaction with an IC50 of less than 0.075 μM. It inhibits cell growth in MV4-11 (CC50 < 0.1 μM), MOLM-13 (CC50 0.1~0.5 μM), and HEK293 (CC50 < 2 μM) cells. Balomenib also exhibits antitumor activity.

Menin-MLL inhibitor-25 (compound A6) is a potent inhibitor of the Menin-MLL interaction, with an IC50 of 0.38 µM. It exhibits antiproliferative activity, induces apoptosis and G0/G1 cell cycle arrest, and can reverse differentiation arrest.

MJ-26 is an inhibitor targeting Menin, characterized by a high binding affinity (Ki: 0.56 μM) and significant antiproliferative activity. It functions by inhibiting Menin-MLL interaction and promoting the degradation of Menin protein. MJ-26 demonstrates notable antitumor effects against acute myeloid leukemia (AML) and is applicable for AML research.

Menin-MLL inhibitor MI-2 dihydrochloride is a competitive and selective inhibitor of the Menin-MLL interaction, with an IC50 value of 446 nM and a Ki value of 158 nM. It reduces the expression of target genes such as HOXA9 and MEIS1, inhibits the proliferation of leukemic cells, and induces apoptosis and differentiation. Menin-MLL inhibitor MI-2 dihydrochloride shows potential for research in MLL-rearranged acute leukemias, such as acute myeloid leukemia and acute lymphoblastic leukemia.

MI-1481 is an effective MML1 inhibitor (IC50: 3.6 nM). MI-1481 showed very potent inhibition of the menin-MLL1 interaction (IC50: 3.6 nM). MI-1481 also demonstrates pronounced activity in MLL leukemia cells and in vivo in MLL leukemia models.

DCYM21 is an inhibitor of menin-MLL interaction. DCYM21 demonstrates potent and selective blockage of proliferation and induces both cell cycle arrest and differentiation of leukemia cells harboring MLL translocations.

MI-2-2 is an inhibitor of bivalent protein-protein interaction between menin and MLL with an IC50 of 46 nM. MI-2-2 binds to menin with Kd of 22 nM.

Ziftomenib (KO-539) is an inhibitor of menin-MLL interaction with antitumor activity, suitable for leukemia research.

M-808 is a potent and efficacious covalent inhibitor, targeting the interaction between Menin and MLL. It demonstrates a high binding affinity with an IC50 value of 2.6 nM.

M 1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression.

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.

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].

MI-463 is a potent and orally bioavailable inhibitor of the menin-mLL interaction (IC50: 15.3 nM).