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

AMI-1 

Cat. No.: HY-18962 Purity: >99.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

AMI-1 Chemical Structure

AMI-1 Chemical Structure

CAS No. : 20324-87-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 109 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
25 mg USD 288 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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

IC50: 8.8 μM (PRMT1), 3.0 μM (yeast-Hmt1p)[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

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.

20324-87-2

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 46 mg/mL (83.87 mM)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.1823 mL 0.9117 mL 1.8233 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

*All of the co-solvents are provided by MCE.
References
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Keywords:

AMI-1AMI1AMI 1Histone Methyltransferaseprotein arginine N-methyltransferasesPRMTsyeast-Hmt1pPRMT1Hmt1pInhibitorinhibitorinhibit

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