AMI-1
Based on 7 publication(s) in Google Scholar
AMI-1 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 exerts PRMTs inhibitory effects by blocking peptide-substrate binding.
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- Pureza: 98.0%
- No. CAS: 20324-87-2
- Fòrmula: C21H14N2Na2O9S2
- Peso molecular:548.45
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) AMI-1
More- Clin Mol Hepatol. 2026 Apr;32(2):843-865. [Abstract]
- Nat Commun. 2023 Feb 23;14(1):1011. [Abstract]
- Cell Death Dis. 2024 Nov 11;15(11):814. [Abstract]
- Cell Death Dis. 2023 Sep 22;14(9):624. [Abstract]
- Genes Dis. 2023 Mar 28;10(6):2622-2638. [Abstract]
- Cell Rep. 2024 Aug 22;43(9):114662. [Abstract]
- Cell Rep. 2024 Jul 24;43(8):114537. [Abstract]
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Actividad biológica
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PRMT1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
>100 μM
Compound: AMI-1
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Cytotoxicity against human A375 cells by MTT assay
Cytotoxicity against human A375 cells by MTT assay
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[PMID: 26428871] |
| Daoy | IC50 |
>100 μM
Compound: AMI-1
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Cytotoxicity against human DaOY cells assessed as reduction in cell viability after 72 hrs by CellTiter-blue assay
Cytotoxicity against human DaOY cells assessed as reduction in cell viability after 72 hrs by CellTiter-blue assay
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[PMID: 28927791] |
| DLD-1 | IC50 |
>100 μM
Compound: AMI-1
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Cytotoxicity against human DLD1 cells by MTT assay
Cytotoxicity against human DLD1 cells by MTT assay
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[PMID: 26428871] |
| HepG2 | IC50 |
51.17 μM
Compound: AMI-1
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Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by CellTiter-blue assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by CellTiter-blue assay
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[PMID: 28927791] |
| MCF7 | IC50 |
>100 μM
Compound: AMI-1
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Cytotoxicity against human MCF7 cells by MTT assay
Cytotoxicity against human MCF7 cells by MTT assay
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[PMID: 26428871] |
| MCF7 | IC50 |
>100 μM
Compound: AMI-1
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Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by CellTiter-blue assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by CellTiter-blue assay
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[PMID: 28927791] |
| SH-SY5Y | IC50 |
>100 μM
Compound: AMI-1
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Cytotoxicity against human SH-SY5Y cells by MTT assay
Cytotoxicity against human SH-SY5Y cells by MTT assay
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[PMID: 26428871] |
| T-24 | IC50 |
>100 μM
Compound: AMI-1
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Cytotoxicity against human T24 cells by MTT assay
Cytotoxicity against human T24 cells by MTT assay
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[PMID: 26428871] |
| UMUC3 | IC50 |
>100 μM
Compound: AMI-1
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Cytotoxicity against human UM-UC-3 cells by MTT assay
Cytotoxicity against human UM-UC-3 cells by MTT assay
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[PMID: 26428871] |
AMI-1 can inhibit the in vitro methylation reactions performed by all five recombinantly active PRMTs (PRMT1, -3, -4, and -6 and Hmt1p)[2].
AMI-1 not only inhibits type I PRMTs (PRMT1, 3, 4 and 6) but also type II PRMT5[2].
AMI-1 specifically inhibits arginine, but not lysine, methyltransferase activity in vitro and does not compete for the AdoMet binding site[3].
AMI-1 inhibits methylation of GFP-Npl3 and cellular proteins[3].
AMI-1 (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 (1.2-2.4 mM; 48-72 hours) reduces S180 cell viability through the induction of cell apoptosis[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:S180 cells, U2OS cells
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Concentration:0.6 mM, 1.2 mM, 2.4 mM
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Incubation Time:48 hours, 72 hours, 96 hours
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Result:Inhibited the cell viability.
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Cell Line:S180 cells
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Concentration:1.2 mM, 2.4 mM
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Incubation Time:48 hours, 72 hours
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Result:Increased the percentages of cells undergoing apoptosis.
AMI-1 (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 (0.5 mg; intratumorally; daily; for 7 days) decreases the levels of H4R3me2s and H3R8me2s in a tumor xenograft model[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-7 weeks old male Kunming mice (18-22 g), with S180 cells xenograft[4]
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Dosage:0.5 mg
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Administration:Intratumorally, daily, for 7 days
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Result:Decreased tumor weight.
Chemical Information
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No. CAS 20324-87-2
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Appearance Solid
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Peso molecular 548.45
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Fòrmula C21H14N2Na2O9S2
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Color Light brown to brown
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SMILES
O=C(NC1=CC2=CC(S(=O)(O[Na])=O)=CC(O)=C2C=C1)NC3=CC4=CC(S(=O)(O[Na])=O)=CC(O)=C4C=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (7)
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Journal Impact Factor
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Most Recent
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Clin Mol Hepatol
PRMT1-mediated asymmetric dimethylation of arginine residue 602 in DDX1 promotes cholangiocarcinoma progression. [Abstract]2026 Apr;32(2):843-865. PMID: 41668296 -
Nat Commun
PHGDH arginine methylation by PRMT1 promotes serine synthesis and represents a therapeutic vulnerability in hepatocellular carcinoma. [Abstract]2023 Feb 23;14(1):1011. PMID: 36823188
AMI-1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 23;14(1):1011. [Abstract]
AMI-1 or adenosine dialdehyde (AdOx) markedly reduces the arginine methylation of PHGDH in HEK293T, Huh7, and PLC/PRF/5 cells.
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Cell Death Dis
PRMT1-mediated methylation of ME2 promotes hepatocellular carcinoma growth by inhibiting ubiquitination. [Abstract]2024 Nov 11;15(11):814. PMID: 39528487 -
Cell Death Dis
Methylation of BRD4 by PRMT1 regulates BRD4 phosphorylation and promotes ovarian cancer invasion. [Abstract]2023 Sep 22;14(9):624. PMID: 37737256 -
Genes Dis
PRMT1 promotes the proliferation and metastasis of gastric cancer cells by recruiting MLXIP for the transcriptional activation of the β-catenin pathway. [Abstract]2023 Mar 28;10(6):2622-2638. PMID: 37554218 -
Cell Rep
CRISPR screening identifies PRMT1 as a key pro-ferroptotic gene via a two-layer regulatory mechanism. [Abstract]2024 Aug 22;43(9):114662. PMID: 39178116 -
Cell Rep
Arginine methylation-enabled FUS phase separation with SMN contributes to neuronal granule formation. [Abstract]2024 Jul 24;43(8):114537. PMID: 39052476
Solvente y solubilidad
H2O : 62.5 mg/mL (113.96 mM; ultrasonic and warming and heat to 60°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (182.33 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
[3]. Donghang Cheng, et al. Small Molecule Regulators of Protein Arginine Methyltransferases. J Biol Chem. 2004 Jun 4;279(23):23892-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.8233 mL | 9.1166 mL | 18.2332 mL | 45.5830 mL |
| 5 mM | 0.3647 mL | 1.8233 mL | 3.6466 mL | 9.1166 mL | |
| 10 mM | 0.1823 mL | 0.9117 mL | 1.8233 mL | 4.5583 mL | |
| 15 mM | 0.1216 mL | 0.6078 mL | 1.2155 mL | 3.0389 mL | |
| 20 mM | 0.0912 mL | 0.4558 mL | 0.9117 mL | 2.2792 mL | |
| 25 mM | 0.0729 mL | 0.3647 mL | 0.7293 mL | 1.8233 mL | |
| 30 mM | 0.0608 mL | 0.3039 mL | 0.6078 mL | 1.5194 mL | |
| 40 mM | 0.0456 mL | 0.2279 mL | 0.4558 mL | 1.1396 mL | |
| 50 mM | 0.0365 mL | 0.1823 mL | 0.3647 mL | 0.9117 mL | |
| 60 mM | 0.0304 mL | 0.1519 mL | 0.3039 mL | 0.7597 mL | |
| 80 mM | 0.0228 mL | 0.1140 mL | 0.2279 mL | 0.5698 mL | |
| 100 mM | 0.0182 mL | 0.0912 mL | 0.1823 mL | 0.4558 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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