| Bioactivity | Brusatol (NSC 172924) is a unique inhibitor of the Nrf2 pathway that sensitizes a broad spectrum of cancer cells to Cisplatin and other chemotherapeutic agents. Brusatol enhances the efficacy of chemotherapy by inhibiting the Nrf2-mediated defense mechanism. Brusatol can be developed into an adjuvant chemotherapeutic agent[1]. Brusatol increases cellular apoptosis[2]. |
| Invitro | Brusatol (0.05, 0.15, 0.45, 1.35, 4.05 and 12.15 μg/mL) reduces the viability of CT-26 cells in a dose-dependent manner with IC50 value of 0.27±0.01μg/mL. When Brusatol is combined with Cisplatin (CDDP) at a constant concentration ratio of 1:1, cell growth inhibition is markedly enhanced compared with single-agent treatment; the IC50 value of Brusatol and CDDP cotreatment is 0.19±0.02μg/mL[2].Brusatol provokes a rapid and transient depletion of Nrf2 protein, through a posttranscriptional mechanism, in mouse Hepa-1c1c7 hepatoma cells. Brusatol sensitizes mammalian cells to chemical toxicity-implications for therapeutic targeting of Nrf2[3]. Cell Viability Assay[2] Cell Line: |
| Name | Brusatol |
| CAS | 14907-98-3 |
| Formula | C26H32O11 |
| Molar Mass | 520.53 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen) |