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AMI5

Katalog-Nr.GC17546 Copy One-Click Copy Product Info

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AMI5 Chemische Struktur

Cas No.: 17372-87-1

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100mg
38,00 $
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Sample solution is provided at 25 µL, 10mM.



Description of AMI5

IC50: 0.78 and 1.41 μM for Hmt1p and PRMT1, respectively

AMI5 is a non-selective protein methyltransferase inhibitor.

Post-translational protein methylation at lysine and arginine residues is related to the gene expression regulation. The enzymatic activities of protein methyltransferases serve to do covalent modifications in the control of gene transcription.

In vitro: AMI-5 has been identified as a competitive inhibitor of SAM binding and had been shown to inhibit not only PRMTs but also lysine methylation by the Set7 and disruptor of telomeric silencing 1-like (DOT1L) MTases in vitro. Both AMI-5 and its analog AMI-1 have been used as lead compounds for the development of novel MTase-specific inhibitors. Moreover, it was found that AMI-5 could inhibit Set7 in vitro and decrease H3K4m1 in vascular endothelial cells. [1].

In vivo: Currently, there is no animal study reported.

Clinical trial: Up to now, AMI-5 is still in the preclinical development stage.

Reference:
[1] Okabe J,Fernandez AZ,Ziemann M,Keating ST,Balcerczyk A,El-Osta A.  Endothelial transcriptome in response to pharmacological methyltransferase inhibition. ChemMedChem.2014 Aug;9(8):1755-62.

Chemical Properties of AMI5

Cas No. 17372-87-1 SDF
Chemical Name sodium 2-(2,4,5,7-tetrabromo-6-oxido-3-oxo-3H-xanthen-9-yl)benzoate
Canonical SMILES BrC1=C([O-])C(Br)=C2C(C(C3=CC=CC=C3C([O-])=O)=C4C=C(Br)C(C(Br)=C4O2)=O)=C1.[Na+].[Na+]
Formula C20H6Br4Na2O5 M.Wt 691.85
Löslichkeit ≥ 69.2mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of AMI5

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.4454 mL 7.227 mL 14.454 mL
5 mM 289.1 μL 1.4454 mL 2.8908 mL
10 mM 144.5 μL 722.7 μL 1.4454 mL
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In vivo Formulation Calculator (Clear solution) of AMI5

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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 saline, 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 36 reference(s) in Google Scholar.)

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