产品
编 号：F250410
分子式：C21H14N2Na2O9S2
分子量：548.45
分子式：C21H14N2Na2O9S2
分子量：548.45
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CAS No: 20324-87-2
产品详情
生物活性：
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.
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.
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.
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.
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.
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.
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