Molecular structure of AMI-1, sodium salt, CAS Number: 20324-87-2
AMI-1, sodium salt (CAS 20324-87-2)
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Alternate Names:
Arginine N-Methyltransferase Inhibitor-1
Application:
AMI-1, sodium salt is a PRMT and HIV-1 RT polymerase inhibitor
CAS Number:
20324-87-2
Purity:
≥98%
Molecular Weight:
592.42
Molecular Formula:
C21H12N2O9S2•4Na
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
AMI-1 is a potent, cell-permeable compound which inhibits protein arginine N-methyltransferases (PRMTs), including human PRMT1 (IC50 = 8.8muM) and yeast-Hmt1p (IC50 = 3.0muM), by blocking peptide-substrate binding. AMI-1 does not compete for the AdoMet (S-adenosyl-L-methionine SAM) binding site and exhibits minimal effects on both SET (Sub39H1, Suv39H2, SET7) and non-SET (DOT1) lysine N-methyltransferases. AMI-1 suppresses the transcriptional coactivator activity of PRMT1 and PRMT4 and it inhibits HIV-1 RT polymerase (IC50 = 5.0muM). PRMT1 methylates histone H4, and is essential for other subsequent histone modifications. AMI-1, a powerful and specific inhibitor of arginine methyltransferase, not only effectively counteracts NADPH-oxidase-derived superoxide, but also influences the transcription of nuclear receptor-regulated genes through estrogen and androgen response elements.
AMI-1, sodium salt (CAS 20324-87-2) References
- A novel mechanism for inhibition of HIV-1 reverse transcriptase. | Skillman, AG., et al. 2002. Bioorg Chem. 30: 443-58. PMID: 12642128
- Small molecule regulators of protein arginine methyltransferases. | Cheng, D., et al. 2004. J Biol Chem. 279: 23892-9. PMID: 15056663
- Inhibitory study of protein arginine methyltransferase 1 using a fluorescent approach. | Feng, Y., et al. 2009. Biochem Biophys Res Commun. 379: 567-72. PMID: 19121292
- An inhibitor of protein arginine methyltransferases, 7,7'-carbonylbis(azanediyl)bis(4-hydroxynaphthalene-2-sulfonic acid (AMI-1), is a potent scavenger of NADPH-oxidase-derived superoxide. | Chen, F. and Fulton, DJ. 2010. Mol Pharmacol. 77: 280-7. PMID: 19903831
- Design, synthesis and biological evaluation of carboxy analogues of arginine methyltransferase inhibitor 1 (AMI-1). | Castellano, S., et al. 2010. ChemMedChem. 5: 398-414. PMID: 20091730
- Single-dose intravenous administration of recombinant human erythropoietin is a promising treatment for patients with acute myocardial infarction - randomized controlled pilot trial of EPO/AMI-1 study -. | Ozawa, T., et al. 2010. Circ J. 74: 1415-23. PMID: 20501957
- Upregulated protein arginine methyltransferase 1 by IL-4 increases eotaxin-1 expression in airway epithelial cells and participates in antigen-induced pulmonary inflammation in rats. | Sun, Q., et al. 2012. J Immunol. 188: 3506-12. PMID: 22387551
- Endothelial transcriptome in response to pharmacological methyltransferase inhibition. | Okabe, J., et al. 2014. ChemMedChem. 9: 1755-62. PMID: 24850797
- 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. | Lv, L., et al. 2015. Endocrine. 49: 669-82. PMID: 25874535
- Protein arginine methyltransferase 1 may be involved in pregnane x receptor-activated overexpression of multidrug resistance 1 gene during acquired multidrug resistant. | Li, T., et al. 2016. Oncotarget. 7: 20236-48. PMID: 26934120
- Arginine methyltransferase inhibitor 1 exhibits antitumor effects against cervical cancer in vitro and in vivo. | Dong, SH., et al. 2018. Pharmazie. 73: 269-273. PMID: 29724292
- Arginine methyltransferase inhibitor-1 inhibits sarcoma viability in vitro and in vivo. | Zhang, B., et al. 2018. Oncol Lett. 16: 2161-2166. PMID: 30008914
- Protein arginine methyltransferase 1 mediates renal fibroblast activation and fibrogenesis through activation of Smad3 signaling. | Zhu, Y., et al. 2020. Am J Physiol Renal Physiol. 318: F375-F387. PMID: 31813251
- Protein Arginine Methyltransferase (PRMT) Inhibitors-AMI-1 and SAH Are Effective in Attenuating Rhabdomyosarcoma Growth and Proliferation in Cell Cultures. | Janisiak, J., et al. 2021. Int J Mol Sci. 22: PMID: 34360791
- Downregulation of PRMT5 by AMI-1 enhances therapeutic efficacy of compound kushen injection in lung carcinoma in vitro and in vivo. | Yang, R., et al. 2023. Mol Cell Biochem. 478: 1031-1044. PMID: 36214894
Inhibitor of:
AI931714, HIV-1 RT, METTL12, Olfr108, OR2G6, PADI6, PRA1, PRMT1, PRMT2, PRMT5, PRMT6, RNF40, and Trimethyl Histone H3.Activator of:
β3Gn-T5, and Monomethyl Histone H4.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
AMI-1, sodium salt, 5 mg | sc-205928 | 5 mg | $114.00 | |||
AMI-1, sodium salt, 25 mg | sc-205928A | 25 mg | $398.00 |