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AMI-1 Histone Methyltransferase inhibitor

Name: AMI-1
Brand: Selleck Chemicals
SKU: S7884
Availability: InStock
Rating: 5 (7 reviews)

Cat.No.S7884

AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively.

Chemical Structure

Molecular Weight: 548.45

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Quality Control

Batch: Purity: 99.02%

99.02

Related Targets	HDAC JAK BET PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Other Histone Methyltransferase Inhibitors	Pinometostat (EPZ5676) 3-Deazaneplanocin A (DZNep) Hydrochloride BIX-01294 Trihydrochloride UNC1999 EPZ015666 (GSK3235025) EPZ004777 MM-102 (HMTase Inhibitor IX) Chaetocin SGC 0946 EPZ005687

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (182.33 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 22 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	PBS Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	22.000mg/ml (40.11mM)	Taking the 1 mL working solution as an example, add 22 mg of this product to 1 ml of PBS, mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	548.45	Formula	C₂₁H₁₄N₂Na₂O₉S₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	20324-87-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC2=C(C=C(C=C2C=C1NC(=O)NC3=CC4=CC(=CC(=C4C=C3)O)S(=O)(=O)[O-])S(=O)(=O)[O-])O.[Na+].[Na+]

Mechanism of Action

Targets/IC₅₀/Ki	yeast Hmt1p (Cell-free assay) 3.0 μM human PRMT1 (Cell-free assay) 8.8 μM
In vitro	In HeLa cells, AMI-1 inhibits methylation levels of GFP-Npl3 fusion and endogenous PRMT1-like activity. This compound also inhibits nuclear receptor-mediated transactivation of a luciferase reporter in MCF7 cells. In addition, it inhibits HIV-1 RT polymerase activity with IC50 of 5 μM and inhibits DNA binding to HIV-1 RT with Kd of 2 μM. In INS-1 cells, this chemical improves INS-1 cell function and mediates translocations of FOXO1 and PDX-1 intracellularly by regulating FOXO1 phosphorylation and methylation.
In vivo	In chronic AIPI rats, AMI-1 (5 μg/rat) ameliorates COX2 expression and asthmatic indexes, and decreases the airway and alveoli lesions, mucus secretion, and collagen deposition in lungs.
References	[1] https://pubmed.ncbi.nlm.nih.gov/15056663/ [2] https://pubmed.ncbi.nlm.nih.gov/12642128/ [3] https://pubmed.ncbi.nlm.nih.gov/26026059/ [4] https://pubmed.ncbi.nlm.nih.gov/25874535/

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Handling Instructions

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