AMI-1 is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 exerts PRMTs inhibitory effects by blocking peptide-substrate binding.
IC50&Target
IC50: 8.8 μM (PRMT1), 3.0 μM (yeast-Hmt1p)
体外研究
AMI-1 can inhibit the in vitro methylation reactions performed by all five recombinantly active PRMTs (PRMT1, -3, -4, and -6 and Hmt1p).
AMI-1 not only inhibits type I PRMTs (PRMT1, 3, 4 and 6) but also type II PRMT5.
AMI-1 specifically inhibits arginine, but not lysine, methyltransferase activity in vitro and does not compete for the AdoMet binding site.
AMI-1 inhibits methylation of GFP-Npl3 and cellular proteins.
AMI-1 (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.
AMI-1 (1.2-2.4 mM; 48-72 hours) reduces S180 cell viability through the induction of cell apoptosis.
Cell Viability Assay
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
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.
体内研究
AMI-1 (0.5 mg; intratumorally; daily; for 7 days) inhibits S180 viability in vivo.
AMI-1 (0.5 mg; intratumorally; daily; for 7 days) downregulates PRMT5 but does not regulate the expression of PRMT7 in a tumor xenograft model.
AMI-1 (0.5 mg; intratumorally; daily; for 7 days) decreases the levels of H4R3me2s and H3R8me2s in a tumor xenograft model.
Animal Model:
6-7 weeks old male Kunming mice (18-22 g), with S180 cells xenograft
Dosage:
0.5 mg
Administration:
Intratumorally, daily, for 7 days
Result:
Decreased tumor weight.
分子式
C21H14N2Na2O9S2
分子量
548.45
CAS号
20324-87-2
运输条件
Room temperature in continental US; may vary elsewhere.