Brusatol, Inhibitor

Brusatol

Cat. Num. AAA5764464

• Purity: 99.35%
• Synonyms: Brusatol; NSC 172924; inhibitor

• Purity/Purification: 99.35%
• Form/Format: Solid. Powder

• Solubility: DMSO: 90mg/mL (172.9mM); Water: Insoluble; (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C26H32O11
• SMILES: CC([C@](C[C@@](O1)2[H])3[H])=C(O)C(C[C@]3(C)[C@]4([H])[C@]2(CO[C@@]5([C@@H](O)[C@@H]4O)C(OC)=O)[C@@]5([H])[C@@H](OC(/C=C(C)/C)=O)C1=O)=O
• CAS Number: 14907-98-3
• Cell Research: CT-26 cells in logarithmic growth are seeded onto a 96-well plate at a density of 4x10^3cells/well. After 24 hours of incubation at 37 degree C, fresh medium containing a series of concentrations of Brusatol (0.05, 0.15, 0.45, 1.35, 4.05 and 12.15ug/mL) and CDDP (0.05, 0.15, 0.45, 1.35, 4.05 and 12.15ug/mL) is added at 100uL/well; each concentration is used to treat six replicate wells. After 48 h of incubation at 37 degree C, the cells are further incubated with MTT (10mg/mL) at 37 degree C for 4 hours. The supernatant is then removed and the precipitate is dissolved with 100uL DMSO. Absorbance is measured using a microplate reader at a wavelength of 490nM. Cytotoxicity is expressed as the concentration of Brusatol and CDDP that inhibit cell growth by 50% (IC50 value). The inhibitory rate is calculated. The possible synergistic effect of Brusatol combined with CDDP is investigated by exposing CT-26 cells to various concentrations of each agent alone or in combination for 48 h [2].
• In Vitro: Nude mice are injected with A549 cells to induce tumor growth, followed by a single i.p. injection of 2mg/kg Brusatol. Tumors are isolated 24 hours or 48 h postinjection. Nrf2 protein levels are significantly decreased at 24 hours or 48 h postinjection, indicating that Brusatol is able to reach the tumor tissue and inhibit the Nrf2 pathway. In the first experiment, once the tumor size reaches an average of 230mM3, DMSO, Brusatol (2mg/kg), Cisplatin (2mg/kg), or Cisplatin (2mg/kg) and Brusatol (2mg/kg) combined treatment,is i.p. injected every other day for a total of five times. Cisplatin or Brusatol alone does not inhibit tumor growth significantly, whereas, in the combination group, tumor size is significantly reduced [3].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Related Product Information for Brusatol, inhibitor

Brusatol is a natural product isolated from the Brucea javanica plant. It inhibits Nrf2.

Product Categories/Family for Brusatol, inhibitor

Immunology/Inflammation; Nrf2

References

Olayanju A, et al. Brusatol provokes a rapid and transient inhibition of Nrf2 signaling and sensitizes mammaliancells to chemical toxicity-implications for therapeutic targeting of Nrf2. Free Radic Biol Med. 2015 Jan;78:202-12.
Olayanju A, et al. Brusatol provokes a rapid and transient inhibition of Nrf2 signaling and sensitizes mammaliancells to chemical toxicity-implications for therapeutic targeting of Nrf2. Free Radic Biol Med. 2015 Jan;78:202-12.
Chen HM, et al. Synergistic antitumor effect of Brusatol combined with Cisplatin on colorectal cancer cells. Int J Mol Med. 2018 Mar;41(3):1447-1454.
Chen HM, et al. Synergistic antitumor effect of Brusatol combined with Cisplatin on colorectal cancer cells. Int J Mol Med. 2018 Mar;41(3):1447-1454.
Ren D, et al. Brusatol enhances the efficacy of chemotherapy by inhibiting the Nrf2-mediated defense mechanism. Proc Natl Acad Sci U S A. 2011 Jan 25;108(4):1433-8.
Ren D, et al. Brusatol enhances the efficacy of chemotherapy by inhibiting the Nrf2-mediated defense mechanism. Proc Natl Acad Sci U S A. 2011 Jan 25;108(4):1433-8.