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| Cas No.: | 20324-87-2 |
| Chemical Name: | Disodium 7,7'-(carbonyldiimino)bis(4-hydroxynaphthalene-2-sulphonate) |
| Synonyms: | Disodium 7,7'-(carbonyldiimino)bis(4-hydroxynaphthalene-2-sulphonate);7,7'-(Carbonyldiimino)bis(4-hydroxy-2-naphthalenesulfonic acid) disodium salt;AMI-1;SODIUM 6,6'-(1,3-UREYLENE)BIS(1-NAPHTHOL-3-SULFONATE);disodium 4-hydroxy-7-[(5-hydroxy-7-sulfonato-2-naphthyl)carbamoylamino]naphthalene-2-sulfonate;Disodium 6,6'-ureylenebis[1-naphthol-3-sulfonate];SODIUM 6,6'-(1,3-UREYLENE) BIS(1,1'-NAPHTHOL)-3,3'-SULFONATE;2-Naphthalenesulfonic acid, 7,7'-(carbonyldiimino)bis[4-hydroxy-, sodium salt (1:2);AMI 1;2-Naphthalenesulfonic acid, 7,7'-(carbonyldiimino)bis(4-hydroxy-, sodium salt (1:2);disodium;4-hydroxy-7-[(5-hydroxy-7-sulfonatonaphthalen-2-yl)carbamoylamino]naphthalene-2-sulfonate;7,7'-(Carbonyldiimino)bis[4-hydroxy-2-n |
| SMILES: | O=C(NC1=CC2=CC(S(=O)([O-])=O)=CC(O)=C2C=C1)NC3=CC4=CC(S(=O)([O-])=O)=CC(O)=C4C=C3.[Na+].[Na+] |
| Formula: | C21H14N2Na2O9S2 |
| M.Wt: | 548.4534 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | 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. |
| In Vivo: | 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 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] |
| 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. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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