RK-9123016 is a potent inhibitor of SIRT2. RK-9123016 inhibits the enzymatic activity of SIRT2 with an IC50value of 0.18 µM but not other human sirtuin members including SIRT1 and SIRT3 at 100 µM. RK-9123016 increases the acetylation level of eukaryotic translation initiation factor 5A (eIF5A), a psiological substrate of SIRT2, and reduces cell viability of human breast cancer cells accompanied with a decrease in c-Myc expression.
References:
[1]. Asad Ali Shah, et al. Identification of a Selective SIRT2 Inhibitor and Its Anti-breast Cancer Activity. Biol Pharm Bull. 2016;39(10):1739-1742.