| Description | PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s > 100 μM)[1]. |
| In vitro | PROTAC Sirt2 Degrader-1 (Compound 12; 10 μM, 1-6 hours) induces Sirt2 degradation in HeLa cells[1]. |
| Target activity | SIRT2:0.25 μM |
| molecular weight | 852.94 |
| Molecular formula | C40H40N10O8S2 |
| CAS | 2098487-75-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 100 mg/mL (117.24 mM) |
| References | 1. Schiedel M, et al. Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals). J Med Chem. 2018 Jan 25;61(2):482-491. |