猩红酸

生物活性靶点体外研究体内研究猩红酸试剂级价格

猩红酸

CAS号:134-47-4
英文名:6,6'-Ureylene-bis(1-naphthol-3-sulfonic acid)
中文名:猩红酸
CBNumber:CB2855268
分子式:C21H16N2O9S2
分子量:504.49
MOL File:134-47-4.mol

猩红酸化学性质

密度 :1.798±0.06 g/cm3(Predicted)
储存条件 :Sealed in dry,Room Temperature
溶解度 :DMSO: 83.33 mg/mL (165.18 mM)
酸度系数(pKa) :-0.17±0.40(Predicted)
CAS 数据库 :134-47-4(CAS DataBase Reference)
EPA化学物质信息 :7,7'-(Carbonyldiimino)bis[4-hydroxy-2-naphthalenesulfonic acid] (134-47-4)

猩红酸性质、用途与生产工艺

生物活性 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。
靶点
Target Value
HMT
()
human PRMT1
()
yeast Hmt1p
(Cell-free assay) 3.0 μM

体外研究

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.

体内研究

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.