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MG 149
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MG 149图片
CAS NO:1243583-85-8
规格:98%
分子量:340.46
包装与价格:
包装价格(元)
5mg电议
25mg电议
100mg电议

产品介绍
HAT inhibitor
CAS:1243583-85-8
分子式:C22H28O3
分子量:340.46
纯度:98%
存储:Store at -20°C

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].


参考文献:
[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.