Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AMI-1 free acid is a potent, cell-permeable, and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), demonstrating inhibitory concentration 50 (IC50) values of 8.8 μM for human PRMT1 and 3.0 μM for yeast-Hmt1p. It achieves its PRMTs inhibitory activity by obstructing peptide-substrate binding [1].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
10 mg | 5 days | $ 54.00 | |
1 mL * 10 mM (in DMSO) | 5 days | $ 48.00 |
Description | AMI-1 free acid is a potent, cell-permeable, and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), demonstrating inhibitory concentration 50 (IC50) values of 8.8 μM for human PRMT1 and 3.0 μM for yeast-Hmt1p. It achieves its PRMTs inhibitory activity by obstructing peptide-substrate binding [1]. |
In vitro | AMI-1 free acid effectively inhibits methylation reactions facilitated by all five recombinantly active PRMTs (protein arginine methyltransferases) [2], specifically PRMT1, -3, -4, -6, and Hmt1p, covering both type I and II enzymes. Notably, its inhibitory function is geared towards arginine methyltransferase activity, without affecting lysine methyltransferases, and it does not target the AdoMet (S-Adenosyl methionine) binding site [3]. Experimentally, AMI-1 free acid has been shown to block the methylation of GFP-Npl3 and various cellular proteins [3]. Its application ranges from 0.6 to 2.4 mM over 48 to 96 hours, significantly reducing cell viability in sarcoma lines (S180 and U2OS) through a mechanism that is both time and dose-dependent [4]. At concentrations of 1.2 to 2.4 mM for 48 to 72 hours, it also notably induces apoptosis in S180 cells, thereby diminishing cell viability [4]. |
In vivo | Administering AMI-1 free acid (0.5 mg; intratumorally; daily; for 7 days) directly into tumors of 6-7 week old male Kunming mice (18-22 g) bearing S180 cell xenografts effectively reduces tumor viability and weight. In this model, AMI-1 simultaneously downregulates PRMT5 levels and lowers the methylation of histone 4 arginine 3 (H4R3me2s) and histone 3 arginine 8 (H3R8me2s), though it does not affect PRMT7 expression [4]. |
Molecular Weight | 504.49 |
Formula | C21H16N2O9S2 |
CAS No. | 134-47-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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AMI-1, free acid 134-47-4 AMI1, free acid AMI 1, free acid inhibitor inhibit