Molecular Formula | C21H16N2O2S |
Molar Mass | 360.43 |
Melting Point | 235 °C(dec.) |
Solubility | DMSO: ≥10mg/mL |
Appearance | White solid |
Color | White to Off-White |
Storage Condition | room temp |
In vitro study | 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 μM) and no activity against SIRT3. |
In vivo study | 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. |
Hazard Symbols | Xn - Harmful |
Risk Codes | 22 - Harmful if swallowed |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.774 ml | 13.872 ml | 27.745 ml |
5 mM | 0.555 ml | 2.774 ml | 5.549 ml |
10 mM | 0.277 ml | 1.387 ml | 2.774 ml |
5 mM | 0.055 ml | 0.277 ml | 0.555 ml |
biological activity | Cambinol is a new and non-competitive nSMase2 inhibitor with a Ki value of 7 μM. |
target | TargetValue nSMase2 (Cell-free say) 7 μM(Ki) |
Target | Value |
nSMase2 (Cell-free assay) | 7 μM(Ki) |
in vitro study | 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 μM) and no activity against SIRT3. |
in vivo study | Cambinol is well tolerated in mice (100 mg/kg) and inhibits growth of Burkitt lymphoma xenografts. No significant weight loss in cambinol-treated animals relative to controls. Inhibitors of NAD-dependent deacetylases may constitute novel anticancer agents. |