20324-87-2
20324-87-2 結(jié)構(gòu)式
基本信息
猩紅酸鈉鹽
6,6'-(1,3-亞脲基)雙(1-萘酚-3-磺酸鈉)
AMI 1
AMI1
AMI-1 disodium salt
AMI-1 - AMI-1 sodium salt
J acid urea,disodiuM salt 70%
Disodium 6,6'-ureylenebis[1-naphthol-3-sulfonate]
Sodium 6,6'-(1,3-ureylene) bis(1-naphthol-3-sulfonate)
SODIUM 6,6'-(1,3-UREYLENE) BIS(1,1'-NAPHTHOL)-3,3'-SULFONATE
Disodium 7,7'-(carbonyldiimino)bis(4-hydroxynaphthalene-2-sulphonate)
7,7'-(carbonyldiimino)bis(4-hydroxy-2-naphthalenesulfonic acid) disodium salt
4-hydroxy-7-[(5-hydroxy-7-sulfonatonaphthalen-2-yl)carbamoylamino]naphthalene-2-sulfonate
物理化學(xué)性質(zhì)
常見問題列表
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. |