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MG 149

现货
Catalog No.
B3276
HAT抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 1,030.00
现货
25mg
¥ 3,340.00
现货
100mg
¥ 6,790.00
Ship with 10-15 days

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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].

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.

文献引用

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

Chemical Properties

StorageStore at RT
M.Wt340.46
Cas No.1243583-85-8
FormulaC22H28O3
Solubility≥114mg/mL in DMSO
Chemical Name2-(4-heptylphenethyl)-6-hydroxybenzoic acid
SDFDownload SDF
Canonical SMILESCCCCCCCC1=CC=C(CCC2=C(C(O)=O)C(O)=CC=C2)C=C1
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

激酶实验 [1]:

结合实验

放射性同位素标记的乙酰转移酶测定在30℃反应体积为30μL下进行。反应缓冲液含有pH 8.0的50 mM HEPES、0.1 mM EDTA、50 μg/mL BSA、1mM二硫苏糖醇、0.1%Triton-X100和2%DMSO。 14C标记的Ac-CoA被用作乙酰供体。将含有组蛋白H4(即H4-20)的N-末端20-氨基酸序列的肽用作p300和Tip60的底物,并且含有组蛋白H3的N-末端20-氨基酸序列的肽(即H3-20)作为PCAF的底物。加入其他组分(Ac-CoA、肽底物和抑制剂)后,在30℃平衡5分钟,用HAT酶引发HAT反应。反应后,将混合物加载到Waterman P81滤纸上,然后用50 mM碳酸氢钠(pH9.0)洗涤三次。将纸风干,通过液体闪烁计数量化掺入到肽底物中的放射性量。

细胞实验 [1]:

细胞系

HeLa 细胞

溶解方法

该化合物在DMSO中的溶解度大于10 mM。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

应用

使用生物素化组蛋白H3或组蛋白H4肽作为底物,MG 149抑制来自HeLa细胞的核提取物中HAT的活性。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

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.

质量控制

化学结构

MG 149

相关生物数据

MG 149

相关生物数据

MG 149