MDL 800

一种变构SIRT6激活剂；在无细胞测定中，浓度为100µM时，选择性激活SIRT6脱乙酰酶活性，而非SIRT1-5和-7以及HDAC1-11脱乙酰酶活性；诱导组蛋白脱乙酰化(IC50=23.3µM)并减少BEL-7405HCC细胞增殖(EC50=90.4µM)；抑制原代小鼠小胶质细胞中OGD诱导的TNF-α释放(0.1-5µM)；在50、100和150mg/kg时减少BEL-7405HCC小鼠异种移植模型中的肿瘤重量和体积。An allosteric SIRT6 activator; selectively activates SIRT6 deacetylase activity over SIRT1-5 and -7 and HDAC1-11 deacetylase activity in cell-free assays at 100 µM; induces histone deacetylation (IC50 = 23.3 µM) in and reduces proliferation of BEL-7405 HCC cells (EC50 = 90.4 µM); inhibits OGD-induced TNF-α release in primary mouse microglia from 0.1-5 µM; reduces tumor weight and volume in a BEL-7405 HCC mouse xenograft model at 50, 100, and 150 mg/kg.分子式C21H16BrCl2FN2O6S2分子量626.3CC1=C(NS(C2=C(C(OC)=O)C=C(NS(C3=CC(Cl)=CC(Cl)=C3)(=O)=O)C=C2)(=O)=O)C=C(Br)C(F)=C1