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

AMI-1 free acid 

Cat. No.: HY-18962A Purity: >98.0%
Handling Instructions

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.

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

AMI-1 free acid Chemical Structure

AMI-1 free acid Chemical Structure

CAS No. : 134-47-4

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10 mM * 1 mL in DMSO USD 100 In-stock
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Based on 1 publication(s) in Google Scholar

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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].

IC50 & Target

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

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.
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.
Molecular Weight

504.49

Formula

C₂₁H₁₆N₂O₉S₂

CAS No.

134-47-4

SMILES

O=C(NC1=CC2=CC(S(=O)(O)=O)=CC(O)=C2C=C1)NC3=CC4=CC(S(=O)(O)=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 : 83.33 mg/mL (165.18 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*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: ≥ 2.08 mg/mL (4.12 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.12 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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AMI-1 free acid
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