Cambinol

14513-15-6

C21H16N2O2S

H2O : < 0.1 mg/mL (insoluble); DMSO : 50 mg/mL (138.72 mM; Need ultrasonic)

Epigenetics; Cell Cycle/DNA Damage

Cambinol is a SIRT1 and SIRT2 inhibitor with IC₅₀ values of 56 and 59 uM, respectively. IC50 & Target: IC50: 56 uM (SIRT1), 59 uM (SIRT2)^[1] In Vitro: Cambinol inhibits NAD-dependent deacetylase activity of human SIRT1 and SIRT2. Inhibition of SIRT1 activity with cambinol during genotoxic stress leads to hyperacetylation of key stress response proteins and promotes cell cycle arrest. Treatment of BCL6-expressing Burkitt lymphoma cells with cambinol as a single agent induces apoptosis, which is accompanied by hyperacetylation of BCL6 and p53. Cambinol has only weak inhibitory activity against SIRT5 (42% inhibition at 300 uM) and no activity against SIRT3^[1]. In Vivo: Cambinol is well tolerated in mice (100 mg/kg) and inhibits growth of Burkitt lymphoma xenografts. No significant weight loss occurs in cambinol-treated animals relative to controls. Inhibitors of NAD-dependent deacetylases may constitute novel anticancer agents^[1].