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    AMI-1 disodium salt
    AMI-1 disodium salt

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0388
    CAS #: 20324-87-2Purity ≥98%

    Description: AMI-1 (AMI 1) disodium salt is a novel, cell-permeable and selective inhibitor of Histone Methyltransferase (HMT) with anti-inflammatory activity. It inhibits HMT with an IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively. 

    References: J Biol Chem. 2004 Jun 4;279(23):23892-9; J Immunol. 2015 Jul 1;195(1):298-306.

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    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


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    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.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    AMI-1

    TGF-β is the main component in ISEM that induced PRMT1 upregulation in fibroblasts. ISEM from epithelial cells, TGF-β Ab, and TGF-β Ab were used to stimulate HFL1 cells, and the expressions of prmt1, cox2, and vegf were detected by RT-qPCR (A–C). The expressions of PRMT1 and COX2 protein were detected by Western blot (D and E). TGF-β with or without AMI-1 (5 and 10 μM), the pan PRMT enzymatic activity inhibitor, was used to stimulate HFL1, and COX2 expression was detected by Western blot (F).  2015 Jul 1;195(1):298-306.

    AMI-1

    Expressions of cox2 and vegf and concentrations of IgE and NO in serum from chronic AIPI rats with or without AMI-1 administration. The expressions of cox2 (A) and vegf (B) were detected by RT-qPCR in lung tissues from control rats, AIPI rats, and AIPI rats with administration of AMI-1. Total IgE (C) and NO concentrations (D) in serum were detected by ELISA and the Griess method.   2015 Jul 1;195(1):298-306.

    AMI-1

    Histopathological changes and remodeling in chronic AIPI rats with and without the administration of AMI-1. Representative images of the histopathological changes by H&E staining (A), PAS staining (B), and Masson staining (D) were from lung sections of E3 rats without Ag challenge, with Ag challenge for 8 wk, and with both Ag challenge and AMI-1 administration for 8 wk, respectively.  2015 Jul 1;195(1):298-306.


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