AMI-1 是一种有效的、细胞渗透性和可逆的蛋白质精氨酸 N-甲基转移酶 (PRMT) 抑制剂，对人 PRMT1 和酵母-Hmt1p 的 IC50 分别为 8.8 μM 和 3.0 μM。 AMI-1 通过阻断肽-底物结合发挥 PRMTs 抑制作用。
| Cas No. | 20324-87-2 |
| 别名 | 猩红酸钠盐,Arginine N - methyltransferase inhibitor - 1 |
| 化学名 | tetrasodium;4-oxido-7-[(5-oxido-7-sulfonatonaphthalen-2-yl)carbamoylamino]naphthalene-2-sulfonate |
| Canonical SMILES | C1=CC2=C(C=C(C=C2C=C1NC(=O)NC3=CC4=CC(=CC(=C4C=C3)[O-])S(=O)(=O)[O-])S(=O)(=O)[O-])[O-].[Na+].[Na+].[Na+].[Na+] |
| 分子式 | C21H12N2O9S2Na4 |
| 分子量 | 592.42 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | AMI-1 is a potent, cell-permeable compound which inhibits protein arginine N-methyltransferases (PRMTs), including human PRMT1 (IC50 = 8.8μM) and yeast-Hmt1p (IC50 = 3.0μM), by blocking peptide-substrate binding.IC50 value: 8.8μM (human PRMT1), 3.0μM (yeast-Hmt1p)Target: human PRMT1, yeast-Hmt1pin vitro: AMI-1 suppresses the transcriptional coactivator activity of PRMT1 and PRMT4 and it inhibits HIV-1 RT polymerase (IC50 = 5.0μM). PRMT1 methylates histone H4, and is essential for other subsequent histone modifications.[1] AMI-1 is the most active nonpeptidic inhibitor reported to be selective against PRMT1. AMI-1 is a selective PRMT inhibitor with a bisanionic structure that is related to compounds known to generate pleiotropic interactions with many proteins, should be further optimized before exploring additional binding pockets. [2]in vivo: AMI-1 is administered intranasally to chronic AIPI rats to determine PRMT effects on asthmatic parameters. AMI-1 inhibited the expression of COX2 in TGF-β-stimulated cells. AMI-1 administered to AIPI rats reduced COX2 production and humoral immune response, and it abrogated mucus secretion and collagen generation.[1] References:
[1]. Sun Q, et al. PRMT1 Upregulated by Epithelial Proinflammatory Cytokines Participates in COX2 Expression in Fibroblasts and Chronic Antigen-Induced Pulmonary Inflammation. J Immunol. 2015 Jul 1;195(1):298-306.
[2]. Castellano S, et al. Design, synthesis and biological evaluation of carboxy analogues of arginine methyltransferase inhibitor 1 (AMI-1). ChemMedChem. 2010 Mar 1;5(3):398-414.
[3]. Lv L, et al. PRMT1 promotes glucose toxicity-induced β cell dysfunction by regulating the nucleo-cytoplasmic trafficking of PDX-1 in a FOXO1-dependent manner in INS-1 cells. Endocrine. 2015 Aug;49(3):669-682.
[4]. Wang J, et al. Pharmacophore-based virtual screening and biological evaluation of small molecule inhibitors for protein arginine methylation. J Med Chem. 2012 Sep 27;55(18):7978-7987. |
