猩红酸钠盐

生物活性靶点体外研究体内研究

猩红酸钠盐

CAS号:20324-87-2
英文名:Disodium 7,7'-(carbonyldiimino)bis(4-hydroxynaphthalene-2-sulphonate)
中文名:猩红酸钠盐
CBNumber:CB3855058
分子式:C21H17N2NaO9S2
分子量:528.48
MOL File:20324-87-2.mol

猩红酸钠盐化学性质

储存条件 :under inert gas (nitrogen or Argon) at 2-8°C
溶解度 :insoluble in EtOH; insoluble in DMSO; ≥19.1 mg/mL in H2O
形态 :Brown solid.
颜色 :Light brown to brown
EPA化学物质信息 :2-Naphthalenesulfonic acid, 7,7'-(carbonyldiimino)bis[4-hydroxy-, disodium salt (20324-87-2)

猩红酸钠盐性质、用途与生产工艺

生物活性 AMI-1 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 通过阻断肽-底物结合对 PRMTs 发挥抑制作用。
靶点

IC50: 8.8 μM (PRMT1), 3.0 μM (yeast-Hmt1p)

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.

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.

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.