MG 149

MG 149

Catalog Number:
L002370485APE
Mfr. No.:
APE-B3276
Price:
$299
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      • Overview
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          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].

          [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.

      • Properties
        • Alternative Name
          2-(4-heptylphenethyl)-6-hydroxybenzoic acid
          CAS Number
          1243583-85-8
          Molecular Formula
          C22H28O3
          Molecular Weight
          340.46
          Purity
          98.00%
          Solubility
          ≥114 mg/mL in DMSO; ≥30.5 mg/mL in EtOH; insoluble in H2O
          Storage
          Store at RT

          * For Research Use Only

      • Reference
        • 1. Zichong Li. "Functional characterization of transcription elongation machinery in HIV transcription and latency." University of California. 2019.
          2. 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

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