| Description | RK-9123016 is a SIRT2 inhibitor. RK-9123016 increases the acetylation level of eukaryotic translation initiation factor 5A (eIF5A), a physiological substrate of SIRT2, and reduces cell viability of human breast cancer cells accompanied with a decrease in c-Myc expression. |
| In vitro | RK-9123016 inhibited the enzymatic activity of SIRT2 with an IC50 value of 0.18 µM but not other human sirtuin members including SIRT1 and SIRT3 at 100 µM in vitro electrophoretic mobility shift assay. RK-9123016 inhibited the SIRT2 activity in MCF-7 cells by concentration dependent manner (0-30 µM). |
| Synonyms | RK9123016, RK 9123016 |
| molecular weight | 374.42 |
| Molecular formula | C16H18N6O3S |
| CAS | 955900-27-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 3.75 mg/mL (10 mM), Sonication is recommended. |
| References | 1. Shah AA, Ito A, Nakata A, Yoshida M. Identification of a Selective SIRT2 Inhibitor and Its Anti-breast Cancer Activity. Biol Pharm Bull. 2016;39(10):1739-1742. PubMed PMID: 27725455. |