Home >> MG 149
Related Products
MG 149 HAT inhibitor

Catalog No.B3276
Size Price Stock Qty
5mg
$103.00
In stock
25mg
$334.00
In stock
100mg
$679.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

      

Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Li Z, Mbonye U, et al. "The KAT5-Acetyl-Histone4-Brd4 axis silences HIV-1 transcription and promotes viral latency." PLoS Pathog. 2018 Apr 23;14(4):e1007012. PMID:29684085

Quality Control

Chemical structure

MG 149

Related Biological Data

MG 149

Protocol

Kinase experiment [1]:

Binding assays

Radioisotope-labeled acetyltransferase assays were carried out at 30°C in a reaction volume of 30 μL. The reaction buffer contained 50 mM HEPES at pH 8.0, 0.1 mM EDTA, 50 μg/mL BSA, 1 mM dithiothreitol, 0.1% Triton-X100, and 2% DMSO. 14C-labeled Ac-CoA was used as the acetyl donor. The peptide containing the N-terminal 20-amino acid sequence of histone H4 (i.e. H4-20) was used as substrate for p300 and Tip60, and the peptide containing the N-terminal 20-amino acid sequence of histone H3 (i.e. H3-20) was employed as substrate for PCAF. The HAT reaction was initiated with the HAT enzyme after the other components (Ac-CoA, peptide substrate, and the inhibitor) were equilibrated at 30°C for 5 min. After the reaction, the mixture was loaded onto a Waterman P81 filter paper and then washed with 50 mM sodium bicarbonate (pH 9.0) for three times. The paper was air dried and the amount of radioactivity incorporated into the peptide substrate was quantified by liquid scintillation counting.

Cell experiment [1]:

Cell lines

HeLa cells

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Applications

MG 149 inhibited the activity of HAT in nuclear extracts from HeLa cells using biotinylated histone H3 or histone H4 peptides as substrates.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Ghizzoni M, Wu J, Gao T, Haisma HJ, Dekker FJ, George Zheng Y. 6-alkylsalicylates are selective Tip60 inhibitors and target the acetyl-CoA binding site. Eur J Med Chem. 2012 Jan;47(1):337-44.

MG 149 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

MG 149 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 1243583-85-8 SDF Download SDF
Synonyms N/A
Chemical Name 2-(4-heptylphenethyl)-6-hydroxybenzoic acid
Canonical SMILES CCCCCCCC1=CC=C(CCC2=C(C(O)=O)C(O)=CC=C2)C=C1
Formula C22H28O3 M.Wt 340.46
Solubility >114mg/mL in DMSO Storage Store at RT
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

MG 149 is an inhibitor of histone acetyltransferases (HAT) with IC50 values of 74μM and 47μM for Tip60 and MOF, respectively [1].

MG 149 is an anacardic acid derivative. It shows selective inhibition towards the MYST type of HATs: Tip60 and MOF with IC50 values of 74μM and 47μM, respectively. The docking study shows that the inhibition of Tip60 by MG 149 is competitive with respect to Ac-CoA in the Ac-CoA binding pocket of Tip60. MG 149 also inhibits the activity of HAT in nuclear extracts from HeLa cells using biotinylated histone H3 or histone H4 peptides as substrates. It is found to be more potent for histone H3 compared to histone H4. Additionally, DNA microarrays demonstrate that MG149 inhibits p53 and NF-kB pathways as well as a very limited number of other pathways [1, 2].

References:
[1] Ghizzoni M, Wu J, Gao T, Haisma HJ, Dekker FJ, George Zheng Y. 6-alkylsalicylates are selective Tip60 inhibitors and target the acetyl-CoA binding site. Eur J Med Chem. 2012 Jan;47(1):337-44.
[2] Dekker FJ, van den Bosch T, Martin NI. Small molecule inhibitors of histone acetyltransferases and deacetylases are potential drugs for inflammatory diseases. Drug Discov Today. 2014 May;19(5):654-60.