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AMI-1

Katalog-Nr.GC17275

A cell permeable inhibitor of PRMTs

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AMI-1 Chemische Struktur

Cas No.: 20324-87-2

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5mg
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25mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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.

Chemical Properties

Cas No. 20324-87-2 SDF
Chemical Name 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+]
Formula C21H12N2O9S2Na4 M.Wt 592.42
Löslichkeit Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.688 mL 8.44 mL 16.8799 mL
5 mM 0.3376 mL 1.688 mL 3.376 mL
10 mM 0.1688 mL 0.844 mL 1.688 mL
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