MG 149 (Synonyms: Tip60 HAT inhibitor) |
| Catalog No.GC11439 |
HAT inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1243583-85-8
Sample solution is provided at 25 µL, 10mM.
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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.
| Kinase experiment [1]: | |
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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]: | |
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Cell lines |
HeLa cells |
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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. |
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Applications |
MG 149 inhibited the activity of HAT in nuclear extracts from HeLa cells using biotinylated histone H3 or histone H4 peptides as substrates. |
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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. |
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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. |
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| Cas No. | 1243583-85-8 | SDF | |
| Synonyms | Tip60 HAT inhibitor | ||
| 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 -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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9372 mL | 14.686 mL | 29.372 mL |
| 5 mM | 0.5874 mL | 2.9372 mL | 5.8744 mL |
| 10 mM | 0.2937 mL | 1.4686 mL | 2.9372 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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.)
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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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