腥红酸 AMI-1 free acid CAS#:134-47-4

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首页化工产品目录有机原料羧酸类化合物及衍生物羧酸的卤化、磺化、硝化或亚硝化衍生物腥红酸

腥红酸

产品纠错

CAS号：134-47-4 | 英文名称：AMI-1 free acid

分子式 C₂₁H₁₆N₂O₉S₂

分子量 504

EINECS号 205-142-9

MDL MFCD00035715

Smiles

InChIKey

乙二醇化学百科

基本信息

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

物化性质

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

安全信息

生产及用途

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.

用途

为偶氮染料用的中间体，用于制造直接橙S、直接耐酸大红4BS等

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