2. Epigenetics
  3. Histone Methyltransferase
  4. AMI-1

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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AMI-1 Chemical Structure

AMI-1 Chemical Structure

CAS No. : 20324-87-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
 USD 33 In-stock
Solution
10 mM * 1 mL in Water USD 33 In-stock
Solid
10 mg USD 30 In-stock
25 mg USD 50 In-stock
50 mg USD 85 In-stock
100 mg USD 145 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of AMI-1:

AMI-1 Related Antibodies

Top Publications Citing Use of Products

    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.

    View All Histone Methyltransferase Isoform Specific Products:

    View All Isoforms
    EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1].

    IC50 & Target

    PRMT1

     

    In Vitro

    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.

    AMI-1 Related Antibodies

    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.
    In Vivo

    AMI-1 (0.5 mg; intratumorally; daily; for 7 days) inhibits S180 viability in vivo[4].
    ? 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.

    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.
    Molecular Weight

    548.45

    Formula

    C21H14N2Na2O9S2
    CAS No.
    Appearance

    Solid

    Color

    Light brown to brown

    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    H2O : 62.5 mg/mL (113.96 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8233 mL 9.1166 mL 18.2332 mL
    5 mM 0.3647 mL 1.8233 mL 3.6466 mL
    View the 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.

    * 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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.

    • Protocol 1

      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.
    • Protocol 2

      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.

    • Protocol 1

      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

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: ≥98.0%

    COA (247 KB) HNMR (187 KB)

    Handling Instructions (2659 KB)
    References

    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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    AMI-1 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    AMI-120324-87-2AMI1AMI 1Histone Methyltransferaseprotein arginine N-methyltransferasesPRMTsyeast-Hmt1pPRMT1Hmt1pInhibitorinhibitorinhibit

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