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AMI-1 disodium salt
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AMI-1 disodium salt图片
CAS NO:20324-87-2
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)548.45
FormulaC21H14N2Na2O9S2
CAS No.20324-87-2
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 100 mg/mL (182.3 mM)
Water: 10 mg/mL (18.2 mM)
Ethanol: <1 mg/mL
Solubility (In vivo) PBS: 22mg/mL
Chemical Name Disodium 7,7'-(carbonyldiimino)bis(4-hydroxynaphthalene-2-sulphonate)
SMILES Code 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+]
Synonyms AMI-1 disodium salt; AMI 1; AMI1; AMI-1
实验参考方法
In Vitro

In vitro activity: 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. 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. It is cell permeable and does not compete for the AdoMet (S-adenosyl-L-methionine, SAM) binding site. AMI-1 inhibits protein arginine N-methyltransferases (PRMTs), including human PRMT1 (IC50 = 8.8μM) and yeast-Hmt1p (IC50 = 3.0μM), by blocking peptide-substrate binding. AMI-1 is also a potent scavenger of NADPH-oxidase-derived superoxide and can modulate nuclear receptor-regulated transcription from estrogen and androgen response elements.


Kinase Assay: AMI-1 is a potent, cell-permeable and specific inhibitor of Histone Methyltransferase (HMT) with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively. It is cell permeable and does not compete for the AdoMet (S-adenosyl-L-methionine, SAM) binding site. AMI-1 inhibits protein arginine N-methyltransferases (PRMTs), including human PRMT1 (IC50 = 8.8μM) and yeast-Hmt1p (IC50 = 3.0μM), by blocking peptide-substrate binding.


Cell Assay: In HeLa cells, AMI-1 inhibits methylation levels of GFP-Npl3 fusion and endogenous PRMT1-like activity. AMI-1 also inhibits nuclear receptor-mediated transactivation of a luciferase reporter in MCF7 cells. In addition, AMI-1 inhibits HIV-1 RT polymerase activity with IC50 of 5 μM and inhibits DNA binding to HIV-1 RT with Kd of 2 μM. In INS-1 cells, AMI-1 improves INS-1 cell function and mediates translocations of FOXO1 and PDX-1 intracellularly by regulating FOXO1 phosphorylation and methylation

In VivoIn chronic AIPI rats, AMI-1 (5 μg/rat) ameliorates COX2 expression and asthmatic indexes, and decreases the airway and alveoli lesions, mucus secretion, and collagen deposition in lungs.
Animal modelChronic AIPI rats
Formulation & DosageDissolved in PBS; 50 μL at a concentration of 0.1 mg/mL; Intranasal injection
ReferencesJ Biol Chem. 2004 Jun 4;279(23):23892-9; J Immunol. 2015 Jul 1;195(1):298-306.