Lys-CoA TFA

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Lys-CoA TFA 

Lys-CoA TFA 是一种选择性 p300 组蛋白乙酰转移酶 (HAT) 抑制剂 (IC50=50-500 nM)。Lys-CoA TFA 对 p300 的选择性是 PCAF 的 100 多倍 (IC50=200 μM)。Lys-CoA TFA 抑制 p300-HAT 活性依赖的转录激活。

Lys-CoA TFA

Lys-CoA TFA Chemical Structure

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生物活性

Lys-CoA TFA is a selective p300 histone acetyltransferase (HAT) inhibitor (IC50=50-500 nM). Lys-CoA TFA displays >100-fold selectivity for p300 over PCAF (IC50=200 μM). Lys-CoA TFA inhibits p300 HAT activity-dependent transcriptional activation[1][2].

IC50 & Target[1]

p300

50-500 nM (IC50)

体外研究
(In Vitro)

Lys-CoA TFA (0.1 and 1 mM; 60 hours) induces a senescent phenotype in human normal melanocytes[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[3]

Cell Line: Normal human melanocytes
Concentration: 0.1 and 1 mM
Incubation Time: 60 hours
Result: Almost completely abolished proliferation, induced high levels of SA-β-Gal, and inhibited cyclin E expression in a dose-dependent manner.

分子量

1108.82

Formula

C33H54F3N10O21P3S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Cebrat M, et al. Synthesis and analysis of potential prodrugs of coenzyme A analogues for the inhibition of the histone acetyltransferase p300. Bioorg Med Chem. 2003;11(15):3307-3313.

    [2]. Lau OD, et al. HATs off: selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF. Mol Cell. 2000;5(3):589-595.

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