AMI-1 free acid

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AMI-1 free acid 是一种有效的，细胞渗透性的，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-底物结合对 PRMTs 发挥抑制作用。

AMI-1 free acid 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 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding.

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).AMI-1 free acid not only inhibits type I PRMTs (PRMT1, 3, 4 and 6) but also type II PRMT5. AMI-1 free acid specifically inhibits arginine, but not lysine, methyltransferase activity in vitro and does not compete for the AdoMet binding site. AMI-1 free acid inhibits methylation of GFP-Npl3 and cellular proteins.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.AMI-1 free acid (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 cellsConcentration: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.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.AMI-1 free acid (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.

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Others

Other Targets

Histone Methyltransferase

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134-47-4

504.49

C21H16N2O9S2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 83.33 mg/mL (165.18 mM; 超声助溶 )

O=C(NC=1C=CC2=C(O)C=C(C=C2C1)S(=O)(=O)O)NC=3C=CC4=C(O)C=C(C=C4C3)S(=O)(=O)O

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(-20℃)

With Ice Pack

≥ 2 years