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PsammaplinA是一种海洋代谢产物,是HDAC和DNA甲基转移酶(DNAmethyltransferases)的有效抑制剂。PsammaplinA是一种高效的选择性HDAC1抑制剂,IC50为0.9nM,对HDAC1的选择性是DAC6的360倍,对HDAC7和HDAC8的效力低1000倍以上。PsammaplinA对革兰氏阳性细菌(Gram-positivebacteria)具有抗菌作用,并抑制DNA合成和DNA促旋酶(DNAgyrase)活性。抗肿瘤活性。
Psammaplin A, a marine metabolite, is a potent inhibitor of HDAC and DNA methyltransferases. Psammaplin A ia a highly potent and selective DAC1 inhibitor with an IC50 of 0.9 nM. Psammaplin A possess the antimicrobial effect on the Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Antitumor Activity[1][2].
[1]. Matthias G J Baud, et al. Defining the Mechanism of Action and Enzymatic Selectivity of Psammaplin A Against Its Epigenetic Targets. J Med Chem. 2012 Feb 23;55(4):1731-50. [2]. Psammaplin A, a Natural Bromotyrosine Derivative From a Sponge, Possesses the
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