Revumenib Citrate Hydrate

Revumenib Citrate Hydrate 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).

Method: Human acute myeloid leukemia (AML) cell lines MV4;11, MOLM13, OCI-AML3, and HL-60 were treated with Revumenib (50 nM) for 24–96 h. Apoptosis (Annexin V) and differentiation (CD11b) were assessed by flow cytometry, protein expression by Western blot, gene expression by RT-qPCR, and metabolic activity by PrestoBlue assay.
Results: Treatment with Revumenib alone for 72 h induced apoptosis in 32.1% of MV4;11 cells. In MOLM13 and OCI-AML3 cells, Revumenib upregulated CD11b expression by 1.5-fold and 1.6-fold, respectively. Revumenib downregulated mRNA expression of MEIS1, PBX3, CDK6, and JMJD1C, and reduced BCL-2 protein levels. No significant effects were observed in HL-60 cells [1].
Method: Primary patient-derived PBMCs from AML patients (harboring KMT2Ar or NPM1c mutations) were treated with Revumenib (50 nM) for 72 h. Apoptosis and surface marker expression (CD11b, CD34, CD38) were measured by flow cytometry, and protein expression was analyzed by Western blot.
Results: Revumenib alone induced limited apoptosis in primary AML cells but reduced CD34 expression and decreased the CD34+/CD38− subpopulation, suggesting an effect on early differentiation [1].