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Urea J Acid (AMI-1; AMI 1) is a 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.
ln Vitro |
AMI-1 free acid has been shown to inhibit the in vitro methylation processes of all five recombinantly active PRMTs (PRMT1, -3, -4, and -6, as well as Hmt1p)[2]. AMI-1 free acid inhibits both type I PRMTs (PRMT1, 3, 4, and 6) and type II PRMT5 [2]. In vitro, AMI-1 free acid inhibits arginine methyltransferase activity but not lysine, and it does not compete with AdoMet for the binding site[3]. Free acid prevents the methylation of GFP-Npl3 and cellular proteins[3]. AMI-1 free acid (0.6-2.4 mM; 48-96 hours) reduces sarcoma cell survival in S180 and U2OS cells in a time- and dose-dependent manner in vitro[4]. AMI-1 free acid (1.2-2.4 mM; 48-72 hours) lowers S180 cell viability by inducing cell death [4].
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ln Vivo |
S180 viability is inhibited in vivo by AMI-1 free acid (0.5 mg; intratumorally; daily; for 7 days)[4]. In a tumor xenograft model, AMI-1 free acid (0.5 mg; intratumorally; daily; for 7 days) downregulates PRMT5 but does not control PRMT7 expression[4]. In a tumor xenograft model, AMI-1 free acid (0.5 mg; intratumorally; daily; for 7 days) reduces the levels of H4R3me2s and H3R8me2s[4].
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Cell Assay |
Cell Viability Assay[4]
Cell Types: S180 cells, U2OS cells Tested Concentrations: 0.6mM, 1.2mM, 2.4mM Incubation Duration: 48 hrs (hours), 72 hrs (hours), 96 hrs (hours) Experimental Results: Inhibited the cell viability. Apoptosis Analysis[4] Cell Types: S180 cells Tested Concentrations: 1.2mM, 2.4mM Incubation Duration: 48 hrs (hours), 72 hrs (hours) Experimental Results: Increased the percentages of cells undergoing apoptosis. |
Animal Protocol |
Animal/Disease Models: 6- 7 weeks old male Kunming mice (18-22 g), with S180 cells xenograft[4]
Doses: 0.5 mg Route of Administration: Intratumorally, daily, for 7 days Experimental Results: diminished tumor weight. |
References |
[1]. 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.
[2]. Baolai Zhang, et al. Arginine Methyltransferase inhibitor-1 Inhibits Sarcoma Viability in vitro and in vivo. Oncol Lett. 2018 Aug;16(2):2161-2166. [3]. Donghang Cheng, et al. Small Molecule Regulators of Protein Arginine Methyltransferases. J Biol Chem. 2004 Jun 4;279(23):23892-9. |
Molecular Formula |
C21H16N2O9S2
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Molecular Weight |
504.4897
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CAS # |
134-47-4
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Related CAS # |
AMI-1;20324-87-2
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SMILES |
S(C1=C([H])C(=C2C([H])=C([H])C(=C([H])C2=C1[H])N([H])C(N([H])C1C([H])=C([H])C2=C(C([H])=C(C([H])=C2C=1[H])S(=O)(=O)O[H])O[H])=O)O[H])(=O)(=O)O[H]
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~165.18 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.12 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9822 mL | 9.9110 mL | 19.8220 mL | |
5 mM | 0.3964 mL | 1.9822 mL | 3.9644 mL | |
10 mM | 0.1982 mL | 0.9911 mL | 1.9822 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.