menin

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

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.

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.

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

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

Menin–KMT2A-IN-1 (Compound 20) is an inhibitor of menin–KMT2A, binding to menin with an IC50 of 8 nM, and disrupting the interaction between menin and lysine methyltransferase 2A (KMT2A). It inhibits hERG channels with an IC50 of 65 μM and suppresses MV4-11 cells with an IC50 of 74 nM. Furthermore, Menin–KMT2A-IN-1 exhibits favorable pharmacokinetic properties in CD-1 mice, with an oral bioavailability of 74%.

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.

Menin-MLL inhibitor 33 (compound 15-a) is a potent Menin-MLL inhibitor, with an IC50 value of 3.6 nM, and exhibits antiproliferative activity.

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.

Menin-MLL-IN-36 (compound 398) is an inhibitor of the Menin/MLL protein interaction, with an IC50 value of 0.043 μM for the expression of MEIS1 mRNA. This compound is applicable to research on cancer, myelodysplastic syndrome (MDS), myeloproliferative neoplasms (MPN), and diabetes.

Menin-MLL-IN-35 (compound 286) is an inhibitor of the Menin/MLL protein interaction, with an IC50 value of 0.096 μM for MEIS1 mRNA expression. It is applicable in research related to cancer, myelodysplastic syndrome (MDS), myeloproliferative neoplasm (MPN), and diabetes.

Menin-MLL-IN-32 (compound 51) is an inhibitor of the Menin-MLL interaction, with an IC50 of 0.042 nM in an HTRF assay. It suppresses MEIS1 mRNA expression with an IC50 of 11 nM. The compound exhibits antiproliferative effects with IC50 values of 8 nM, 24 nM, and 1900 nM for MOLM14, OCI-AML3, and KO-52 cells, respectively. Menin-MLL-IN-32 is applicable for leukemia research.

Menin-MLL-IN-37 is an orally active inhibitor of the Menin-MLL protein complex, with an IC50 of 820.50 nM. It disrupts the interaction between menin and MLL proteins. Additionally, Menin-MLL-IN-37 induces differentiation of acute myeloid leukemia cells and selectively inhibits the proliferation of MLL-rearranged and DNMT3A/NPM1-mutant leukemia cells. This compound is useful for research related to acute myeloid leukemia (AML).

(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 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.

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

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

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