(1S)-6-氯-2,3,4,9-四氢-1H-咔唑-1-甲酰胺 T7058

Product Introduction
Bioactivity


英文名: Selisistat S-enantiomer

描述: Selisistat S-enantiomer (EX-527 S-enantiomer) 是一种选择性的SIRT1抑制剂，IC50值为 98 nM。

体外活性: Treatment with Selisistat S-enantiomer dramatically increased acetylation at lysine 382 of p53 after different types of DNA damage in primary human mammary epithelial cells and several cell lines. Inhibition of SIRT1 catalytic activity by Selisistat S-enantiomer had no effect on cell growth, viability, or p53-controlled gene expression in cells treated with etoposide [1]. When the function of SIRT1 is inhibited by Selisistat S-enantiomer or its expression is suppressed by RNAi, the upregulated level and release of IL-1β and TNF-α by high glucose are further increased [2]. When HCT116 cells were cultured in 0.1% serum, addition of Selisistat S-enantiomer caused a 90% increase in cell number after 7 days. In the presence of 10% serum, Selisistat S-enantiomer did not change cell number in long term culture [3].

体内活性: The central pretreatment with Selisistat S-enantiomer blunted the ghrelin-induced food intake in rats. Mice lacking p53, a target of SIRT1 action, failed to respond to ghrelin in feeding behavior. Ghrelin failed to phosphorylate hypothalamic AMPK when rats were pretreated with Selisistat S-enantiomer, as it did in p53 KO mice [4]. Selisistat S-enantiomer abolished RSV-induced attenuation of microvascular inflammation in ob/ob septic mice [5].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 20 mg/mL
Ethanol : 5 mg/mL


关键字: EX-527 | Selisistat Senantiomer | EX527 | Sirtuin | Selisistat S-enantiomer | (S)-Selisistat | Selisistat S enantiomer | inhibit | EX 527 | Inhibitor

相关产品: MC3482 | Splitomicin | 5-Feruloylquinic acid | Tenovin-3 | SIRT1 activator 1 | Z26395438 | BML-278 | Sirtuin-1 inhibitor 1 | SRT 2183 | Tenovin-6 Hydrochloride

相关库: Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Epigenetics Compound Library | DNA Damage & Repair Compound Library | Histone Modification Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途