| 中文名称 | 猩红酸钠盐 |
| 英文名称 | Disodium 7,7'-(carbonyldiimino)bis(4-hydroxynaphthalene-2-sulphonate) |
| CAS号 | 20324-87-2 |
| 分子式 | C21H17N2NaO9S2 |
| 分子量 | 528.48 |
| EINECS号 | 243-735-4 |
| 溶解度 | 不溶于乙醇;不溶于DMSO;水中≥19.1 mg/mL |
| 形态 | 棕色固体。 |
| 颜色 | 浅棕色至棕色 |
IC50: 8.8 μM (PRMT1), 3.0 μM (yeast-Hmt1p)
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. |
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. |