AMI-1 free acid 是一种有效的，具有细胞渗透性和可逆的蛋白精氨酸 N-甲基转移酶 (PRMTs) 抑制剂，对人 PRMT1 和酵母 Hmt1p 作用的IC50值分别为 8.8 μM 和 3.0 μM。AMI-1 free acid 通过阻断肽-底物结合发挥 PRMTs 抑制作用。

AMI-1 free acid is a potent, cell-permeable, and reversible protein arginine N-methyltransferases (PRMTs) inhibitor with IC 50 s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding [1].

AMI-1 free acid can inhibit the in vitro methylation reactions performed by all five recombinantly active PRMTs (PRMT1, -3, -4, and -6 and Hmt1p) [2]. AMI-1 free acid not only inhibits type I PRMTs (PRMT1, 3, 4 and 6) but also type II PRMT5 [2]. AMI-1 free acid specifically inhibits arginine, but not lysine, methyltransferase activity in vitro and does not compete for the AdoMet binding site [3]. AMI-1 free acid inhibits methylation of GFP-Npl3 and cellular proteins [3]. AMI-1 free acid (0.6-2.4 mM; 48-96 hours) inhibits the cell viability of sarcoma in S180 and U2OS cells in a time-dependent and dose-dependent manner in vitro [4]. AMI-1 free acid (1.2-2.4 mM; 48-72 hours) reduces S180 cell viability by inducing cell apoptosis [4]. Cell Viability Assay [4] Cell Line: S180 cells, U2OS cells Concentration: 0.6 mM, 1.2 mM, 2.4 mM Incubation Time: 48 hours, 72 hours, 96 hours Result: Inhibited the cell viability. Apoptosis Analysis [4] Cell Line: S180 cells Concentration: 1.2 mM, 2.4 mM Incubation Time: 48 hours, 72 hours Result: Increased the percentages of cells undergoing apoptosis.

AMI-1 free acid (0.5 mg; intratumorally; daily; for 7 days) inhibits S180 viability in vivo [4]. AMI-1 free acid (0.5 mg; intratumorally; daily; for 7 days) downregulates PRMT5 but does not regulate the expression of PRMT7 in a tumor xenograft model [4]. AMI-1 free acid (0.5 mg; intratumorally; daily; for 7 days) reduces the levels of H4R3me2s and H3R8me2s in a tumor xenograft model [4]. Animal Model: 6-7 weeks old male Kunming mice (18-22 g), with S180 cells xenograft [4] Dosage: 0.5 mg Administration: Intratumorally, daily, for 7 days Result: Decreased tumor weight.

134-47-4

C21H16N2O9S2

504.49

AMI-1, free acid

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years