STM2457 is an inhibitor of the RNA methyltransferase METTL3 (IC50=16.9 nM) with selective and oral activity.STM2457 can be used in acute myeloid leukemia (AML) studies.

METHODS: Eight human acute myeloid leukemia cells AML were treated with STM2457 (0-100 μM) for 72 h. Cell proliferation was detected using CellTiter 96 AQueous Non-Radioactive Cell Proliferation Assay.
RESULTS: STM2457-treated AML cell lines showed a significant reduction in growth after treatment in a concentration-dependent manner, with IC50s ranging from 0.6-10.3 μM. [1]
METHODS: Human lung cancer cells A549 and H1975 were treated with STM2457 (1-5 μM) for 3-6 days and apoptosis was detected using Flow Cytometry.
RESULTS: STM2457 induced apoptosis in A549 and H1975 cells. [2]

METHODS: To assay anti-tumor activity in vivo, STM2457 (50 mg/kg) was administered intraperitoneally to NSG mice bearing xenografts derived from human AML patients once daily for twelve to fourteen days.
RESULTS: Daily treatment with STM2457 resulted in impaired implantation and AML amplification in vivo and significantly prolonged mouse lifespan. [1]
METHODS: To investigate the role of METTL3 in the pathogenesis of systemic lupus erythematosus (SLE), STM2457 (30 mg/kg) was administered intraperitoneally to a cGVHD lupus mouse model once every three days for ten weeks.
RESULTS: METTL3 inhibition increased antibody production and exacerbated the lupus-like phenotype in cGVHD mice.METTL3 inhibition is involved in the pathogenesis of SLE by participating in the imbalance between CD4+ T cell activation and effector T cell differentiation. [3]