AMI-1 is an effective and selective Histone Methyltransferase (HMT) inhibitor (IC50: 3.0/8.8 μM, for yeast Hmt1p, and human PRMT1).

Hmt1p (yeast):3.0 μM, PRMT1 (human):8.8 μM

在HeLa细胞中，AMI-1抑制GFP-Npl3融合蛋白和内源性PRMT1样活性的甲基化水平。AMI-1还能抑制MCF7细胞中核受体介导的荧光素酶报告基因的激活。[1] 此外，AMI-1抑制HIV-1 RT聚合酶活性，IC50为5 μM，并阻断HIV-1 RT与DNA的结合，Kd为2 μM。[2] 在INS-1细胞中，AMI-1通过调控FOXO1的磷酸化和甲基化，改善INS-1细胞功能，并促进FOXO1与PDX-1在细胞内的转位。[4]

在慢性AIPI大鼠中，AMI-1（5 μg/大鼠）改善了COX2表达和哮喘指标，并减少了气道和肺泡损伤、粘液分泌以及肺部的胶原沉积。[3]

INS-1 832/13 cells are suspended in RPMI medium containing 11 mM glucose and the supplements described above. These cells are seeded at a density of 2×104?cells/well in a 96-well black plate coated with poly-D-lysine, and 1% BSA and 0.1% DMSO alone (control), palmitic acid (62.5, 125, 250, 500, and 1000 μM), oleic acid (62.5, 125, 250, 500, and 1000 μM), or TAK-875 (6.25, 12.5, 25, 50, and 100 μM) is added to the plate with 1% BSA and 0.1% DMSO, followed by culture for 72 h. After the culture, caspase 3/7 activity is measured with the Apo-one homogeneous caspase 3/7 assay according to the manufacturer's instructions. Fluorescence intensity is measured at an excitation of 485 nm and an emission at 535 nm.