PRODUCT INFORMATION
Names
| Name | 7,7'-(Carbonylbis(azanediyl))bis(4-hydroxynaphthalene-2-sulfonic acid) |
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| Synonym | More Synonyms |
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AMI-1 free acid Biological Activity
| Description | AMI-1 free acid is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding[1]. |
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| Related Catalog | Research Areas >> Cancer Signaling Pathways >> Epigenetics >> Histone Methyltransferase |
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| Target | IC50: 8.8 μM (PRMT1), 3.0 μM (yeast-Hmt1p)[1] |
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| In Vitro | AMI-1 free acid can inhibit the in vitro methylation reactions performed by all five recombinantly active PRMTs (PRMT1, -3, -4, and -6 and Hmt1p)[2]. AMI-1 free acid not only inhibits type I PRMTs (PRMT1, 3, 4 and 6) but also type II PRMT5[2]. AMI-1 free acid specifically inhibits arginine, but not lysine, methyltransferase activity in vitro and does not compete for the AdoMet binding site[3]. AMI-1 free acid inhibits methylation of GFP-Npl3 and cellular proteins[3]. AMI-1 free acid (0.6-2.4 mM; 48-96 hours) inhibits the cell viability of sarcoma in S180 and U2OS cells in a time-dependent and dose-dependent manner in vitro[4]. AMI-1 free acid (1.2-2.4 mM; 48-72 hours) reduces S180 cell viability through the induction of cell apoptosis[4]. Cell Viability Assay[4] Cell Line: S180 cells, U2OS cells Concentration: 0.6 mM, 1.2 mM, 2.4 mM Incubation Time: 48 hours, 72 hours, 96 hours Result: Inhibited the cell viability. Apoptosis Analysis[4] Cell Line: S180 cells Concentration: 1.2 mM, 2.4 mM Incubation Time: 48 hours, 72 hours Result: Increased the percentages of cells undergoing apoptosis. |
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| In Vivo | AMI-1 free acid (0.5 mg; intratumorally; daily; for 7 days) inhibits S180 viability in vivo[4]. AMI-1 free acid (0.5 mg; intratumorally; daily; for 7 days) downregulates PRMT5 but does not regulate the expression of PRMT7 in a tumor xenograft model[4]. AMI-1 free acid (0.5 mg; intratumorally; daily; for 7 days) decreases the levels of H4R3me2s and H3R8me2s in a tumor xenograft model[4]. Animal Model: 6-7 weeks old male Kunming mice (18-22 g), with S180 cells xenograft[4] Dosage: 0.5 mg Administration: Intratumorally, daily, for 7 days Result: Decreased tumor weight. |
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| References | [1]. Donghang Cheng, et al. Small Molecule Regulators of Protein Arginine Methyltransferases. J Biol Chem. 2004 Jun 4;279(23):23892-9. [2]. Zhang, B., et al. Targeting protein arginine methyltransferase 5 inhibits colorectal cancer growth by decreasing arginine methylation of eIF4E and FGFR3. Oncotarget. 2015 Sep 8;6(26):22799-811. [3]. Donghang Cheng, et al. Small Molecule Regulators of Protein Arginine Methyltransferases. J Biol Chem. 2004 Jun 4;279(23):23892-9. [4]. Baolai Zhang, et al. Arginine Methyltransferase inhibitor-1 Inhibits Sarcoma Viability in vitro and in vivo. Oncol Lett. 2018 Aug;16(2):2161-2166. |
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Chemical & Physical Properties
| Density | 1.798 g/cm3 |
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| Melting Point | 86-88 °C |
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| Molecular Formula | C21H16N2O9S2 |
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| Molecular Weight | 504.49000 |
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| Exact Mass | 504.03000 |
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| PSA | 207.09000 |
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| LogP | 5.84920 |
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| Index of Refraction | -45 ° (C=1, AcOH) |
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Company Profile
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