| Name | Selisistat S-enantiomer |
| Description | Selisistat S-enantiomer (EX-527 S-enantiomer) is an effective and specific SIRT1 inhibitor (IC50 = 98 nM) and shows >200-fold selectivity against SIRT2/3. |
| In vitro | 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]. |
| In vivo | 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]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 20 mg/mL (80.41 mM), Sonication is recommended.
Ethanol : 5 mg/mL (20.1 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (8.04 mM), Sonication is recommended.
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| Keywords | Sirtuin | SIRT1 | Selisistat S-enantiomer | Selisistat Senantiomer | Selisistat S enantiomer | Inhibitor | inhibit | EX-527 | EX527 | EX 527 | (S)-Selisistat |
| Inhibitors Related | JGB1741 | Nicotinamide riboside malate | Sirtinol | Selisistat | MDL-800 | Dihydrocoumarin | SRT 2104 | Nicotinamide riboside | MC3482 | Fisetin | SIRT5 inhibitor 8 | Nicotinamide |
| Related Compound Libraries | DNA Damage & Repair Compound Library | Histone Modification Compound Library | Bioactive Compound Library | Anti-Cancer Clinical Compound Library | Antioxidant Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Mitochondria-Targeted Compound Library | Anti-Aging Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
