| 中文名称 | 猩红酸 |
| 英文名称 | 6,6'-Ureylene-bis(1-naphthol-3-sulfonic acid) |
| CAS号 | 134-47-4 |
| 分子式 | C21H16N2O9S2 |
| 分子量 | 504.49 |
| EINECS号 | 205-142-9 |
| 密度 | 1.798±0.06 g/cm3(Predicted) |
| 溶解度 | 二甲基亚砜:83.33 mg/mL(165.18 mM) |
| 形态 | 固体 |
| 酸度系数(pKa) | -0.17±0.40(Predicted) |
| 颜色 | 浅棕色至棕色 |
| Target | Value |
|
HMT
() | |
|
human PRMT1
() | |
|
yeast Hmt1p
(Cell-free assay) | 3.0 μM |
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 cells |
| Concentration: | 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. |