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.

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 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.

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.

Revumenib Citrate (SNDX-5613) is a potent and specific inhibitor of the Menin-MLL interaction. Revumenib Citrate can be used for research on acute leukemias harboring MLL gene rearrangements, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML).

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).