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Menin-MLL inhibitor-22 (compound C20) is an orally active inhibitor of the interaction between menin and mixed lineage leukemia (MLL) (IC50=7 nM). Menin-MLL inhibitor-22 binds menin protein and inhibits cancer cell growth (MV4 cells, IC50=0.3 μM). Menin is a putative tumor suppressor associated with multiple endocrine neoplasia type 1 (MEN-1 syndrome) .
Bleximenib (Menin-MLL inhibitor 24) (compound A) is a menin-mixed-lineage leukemia 1 (menin-MLL) inhibitor. Bleximenib can be used for the research of cancer .
Menin-MLL inhibitor 34 (Compound 37) is a selective and potent Menin-MLL inhibitor, with an IC50 of 18.21 nM for Menin. Menin-MLL inhibitor 34 has long-lasting anti-leukemic effects by reducing Menin protein levels and down-regulating MEN1 transcription .
Menin-MLL inhibitor 29 (Compound C1) is a Menin-MLL PPI inhibitor. Menin-MLL inhibitor 29 binds to Menin with a KD value of 138 nM, and inhibits the binding of Menin to MBM1 (Menin-binding motif 1) with an IC50 value of 46 nM. Menin-MLL inhibitor 29 inhibits HepG2 and Hep3B hepatoma cell proliferation (IC50s: 0.31 μM and 0.71 μM). Menin-MLL inhibitor 29 inhibits tumor growth .
Menin-MLL inhibitor-25 (compound A6) is a potent Menin-MLL interaction inhibitor with an IC50 value of 0.38 µM. Menin-MLL inhibitor-25 shows anti-proliferative activity. Menin-MLL inhibitor-25 induces apoptosis and cell cycle arrest at G0/G1 phase. Menin-MLL inhibitor-25 reverses the differentiation arrest .
Menin-MLL inhibitor 33 (compound 15-a) is a potent Menin-MLL inhibitor with an IC50 value of 3.6 nM. Menin-MLL inhibitor 33 shows antiproliferative activity .
Menin-MLL inhibitor 4 is an inhibitor of Menin- MLL (mixed-lineage leukemia protein) interaction extracted from patent WO2017214367, compound example 1. Menin-MLL inhibitor 4 has antitumor activity .
Menin-MLL inhibitor 21 (example 9) is a specific, irreversible inhibitor of Menin-MLL interaction, useful for the study of autoimmune diseases, heteroimmune diseases, cancer, and other diseases dependent on menin-MLL.
Menin-MLL inhibitor 19, a potent exo-aza spiro inhibitor of menin-mll interaction, example A17, extracted from patent WO2019120209A1. Menin-MLL inhibitor 19 can be used for the reseaech of various diseases, such as cancer, myelodysplastic syndrome (MDS) and diabetes .
Emilumenib (Menin-MLL inhibitor 26) is a Menin-MLL inhibitor. Emilumenib also is an active reference. Emilumenib can inhibits cell growth. Emilumenib can be used for the research of leukemia .
BN-104 (BNM-1192) is an effective selective brain membrane protein inhibitor with oral activity, and it's also a Menin inhibitor, it can block the Menin-MLL interaction and leads to the degradation of Menin protein. BN-104 is a weak hERG inhibitor, with an IC50 greater than 100 μM. BN-104 has anti-tumor activity and can be used in cancer research, such as for acute myeloid leukemia .
(1s,4s)-Menin-MLL inhibitor-23 is the enantiomer of Menin-MLL inhibitor-23 (HY-148367). Menin-MLL inhibitor-23 (Example 99A) is a menin-MLL interaction inhibitor .
(S)-Bleximenib ((S)-Menin-MLL inhibitor 24) oxalate is a S-Enantiomer of (S)-Menin-MLL inhibitor 24 oxalate (HY-148669A). (S)-Bleximenib oxalate is a menin-mixed-lineage leukemia 1 (menin-MLL) inhibitor, and can be used for the research of cancer .
Enzomenib is an inhibitor of the menin protein encoded by the multiple endocrine neoplasia (MEN) gene. Enzomenib can block the binding of the menin protein to mixed lineage leukemia (MLL) fusion proteins and can be used in the study of hematological malignancies .
Revumenib (SNDX-5613) is a potent and specific Menin-MLL inhibitor with a binding Ki of 0.149 nM and a cell based IC50 of 10-20 nM. Revumenib can be used for the research of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML) .
M-89 is a highly potent and specific menin inhibitor, with a Kd of 1.4 nM for binding to menin. M-89 inhibits the menin-mixed lineage leukemia (Menin-MLL) protein-protein interaction and has potential to treat MLL leukemia .
MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (Kd=22nM) and very effectively disrupts the bivalent protein-protein interaction between menin and MLL. MI-2-2 has specific and very pronounced activity in MLL leukemia cells, including inhibition of cell proliferation, down-regulation of Hoxa9 expression, and differentiation .
M-525 is a first-in-class, highly potent, irreversible and covalent menin-MLL protein-protein interaction inhibitor. M-525 binds to menin with an IC50 of 3 nM and achieves low nanomolar potencies in cell growth inhibition and in suppression of MLL regulated gene expression in MLL leukemia cells. Anti-leukemia activity .
VTP50469 fumarate is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 fumarate has potently anti-leukemia activity .
VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 has potently anti-leukemia activity .
MIV-6 is a small molecule inhibitor that inhibits menin-mixed lineage leukemia (MLL) interaction and exhibits strong selective activity in MLL leukemia cells with IC50 = 56 nM.
MI-nc dihydrochloride is a weak inhibitor of the Menin-MLL fusion protein interaction with an IC50 of 193 μM. MI-nc dihydrochloride can be used as a negative control compound of MI-2 .
MIV-6R is an optimized small molecule inhibitor of menin-mixed lineage leukemia (MLL) interaction with IC50 = 56 nM, and its specific mechanism of action activity has been validated in MLL leukemia cells.
MI-136 is an inhibitor of the menin-MLL protein-protein interaction (PPI), with an IC50 of 31 nM and a Kd of 23.6 nM. MI-136 shows to block AR signaling and has the potential for the study in castration-resistant tumors .
MI-1481 is a highly potent inhibitor of the Menin-MLL1 interaction with IC50 of 3.6 nM. MI-1481 markedly reduces cell growth of murine bone marrow cells transformed and inhibits leukemia progression .
VTP50469 mesylate is a potent, and selective Menin-MLL1 inhibitor that effectively targets MLL-rearranged and NPM1c+ leukemia. VTP50469 mesylate selectively kills cell lines with MLL rearrangements and NPM1c+ mutations. VTP50469 mesylate displaces Menin from protein complexes and inhibits MLL's chromatin occupancy at specific genes, leading to significant changes in gene expression, differentiation, and apoptosis. VTP50469 demonstrates dramatic reductions in leukemia burden in patient-derived xenograft models of MLL-r acute myeloid leukemia and MLL-r acute lymphoblastic leukemia, with some mice remaining disease-free for over a year post-treatment.
ML399 is a second-generation probe optimized for inhibitors of menin-mixed lineage leukemia (MLL) protein-protein interactions. Screening through the Molecular Library Probe Production Network (MLPCN) led to the discovery of several chemical classes, including piperidines, which successfully led to the generation of the first-generation probe ML227. However, metabolic instability, potency, and adjuvant pharmacological activity of ML227 were identified as limiting features. To enhance the utility of menin-MLL inhibitor probes for in vivo mechanistic studies, medicinal chemistry efforts were reinvigorated using a structure-based design approach, which ultimately led to the generation of the announced probe ML399. This study describes the structure-activity relationships and properties of this series of compounds.
DC_YM21 is an inhibitor of menin-MLL interaction with potent and selective proliferation blocking activity. DC_YM21 can induce cell cycle arrest and differentiation of leukemia cells carrying MLL translocation. DC_YM21 shows potential application value in inhibiting MLL leukemia .
BAY-155 is a potent and selective menin-MLL tool inhibitor, with an IC50 of 8 nM. BAY-155 leads to a strong expression down-regulation of the MEIS1 gene and up-regulation of CD11b and MNDA genes. BAY-155 shows anti-proliferative effects in AML/ALL (acute myeloid/lymphoblastic leukemia) models .
MI-3454 is an orally active, highly potent and selective menin-MLL1 interaction inhibitor with an IC50 of 0.51 nM. MI-3454 inhibits proliferation, induces differentiation and complete remission or regression of leukemia in mouse models of MLL1-rearranged or NPM1-mutated leukemia through downregulation of key genes involved in leukemogenesis .
The Menin protein is an important component of the MLL/SET1 HMT complex, which methylates “Lys-4” of histone H3. It acts as a transcriptional regulator, inhibiting telomerase expression and inhibiting cell proliferation through TGFB1. Menin Protein, Human is the recombinant human-derived Menin protein, expressed by E. coli , with tag free. The total length of Menin Protein, Human is 615 a.a., .
The Menin protein is an important component of the MLL/SET1 HMT complex, which methylates “Lys-4” of histone H3. It acts as a transcriptional regulator, inhibiting telomerase expression and inhibiting cell proliferation through TGFB1. Menin Protein, Human (His) is the recombinant human-derived Menin protein, expressed by E. coli , with N-6*His labeled tag. The total length of Menin Protein, Human (His) is 615 a.a., .
The Menin protein is an important component of the MLL/SET1 HMT complex, which methylates “Lys-4” of histone H3. It acts as a transcriptional regulator, inhibiting telomerase expression and inhibiting cell proliferation through TGFB1. Menin Protein, Human (His, M327I) is the recombinant human-derived Menin, expressed by E. coli , with His labeled tag. ,
The Menin protein is an important component of the MLL/SET1 HMT complex, which methylates “Lys-4” of histone H3. It acts as a transcriptional regulator, inhibiting telomerase expression and inhibiting cell proliferation through TGFB1. Menin Protein, Human (His, T349M) is the recombinant human-derived Menin, expressed by E. coli , with His labeled tag. ,
The Menin protein is an important component of the MLL/SET1 HMT complex, which methylates “Lys-4” of histone H3. It acts as a transcriptional regulator, inhibiting telomerase expression and inhibiting cell proliferation through TGFB1. Menin Protein, Human (His, M327V) is the recombinant human-derived Menin, expressed by E. coli , with His labeled tag. ,
The Menin protein is an important component of the MLL/SET1 HMT complex, which methylates “Lys-4” of histone H3. It acts as a transcriptional regulator, inhibiting telomerase expression and inhibiting cell proliferation through TGFB1. Menin Protein, Human (His, G331R) is the recombinant human-derived Menin, expressed by E. coli , with His labeled tag. ,
Menin Antibody (YA1673) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA1673), targeting Menin, with a predicted molecular weight of 68 kDa (observed band size: 68 kDa). Menin Antibody (YA1673) can be used for WB, IP experiment in human, rat background.
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