1. NF-κB
    Apoptosis
  2. Keap1-Nrf2
    Apoptosis
  3. Brusatol

Brusatol (Synonyms: NSC 172924)

Cat. No.: HY-19543 Purity: 99.89%
Handling Instructions

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. Brusatol increases cellular apoptosis.

For research use only. We do not sell to patients.

Brusatol Chemical Structure

Brusatol Chemical Structure

CAS No. : 14907-98-3

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 183 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 183 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 160 In-stock
Estimated Time of Arrival: December 31
10 mg USD 280 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 11 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Brusatol purchased from MCE. Usage Cited in: Invest Ophthalmol Vis Sci. 2020 Jun 3;61(6):51.

    After pretreatment HCECs with 20 nM Brusatol (BT) for 2 hours, add 0.6 mM PAE or DMSO for 4 hours, and then stimulated with A. fumigatus for 8 hours or 24 hours. The Nrf2 and HO-1 expression declined in normal HCECs pretreated with Brusatol (BT). BT partially inhibits PAE-induced Nrf2 and HO-1 expression in infected HCECs.

    Brusatol purchased from MCE. Usage Cited in: Invest Ophthalmol Vis Sci. 2020 Jun 3;61(6):51.

    PCR and ELISA results show the mRNA and protein levels of IL-6, IL-8, and TNF-α after blocking Nrf2 activity. Brusatol (BT) pretreatment partially reverses IL-6, TNF-α, and IL-8 expression levels, which are inhibited by PAE in infected HCECs.
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    Description

    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].

    IC50 & Target

    Nrf2[1]

    In Vitro

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Viability Assay[2]

    Cell Line: The murine CT-26 CRC cell line
    Concentration: 0.05, 0.15, 0.45, 1.35, 4.05 and 12.15 μg/mL
    Incubation Time: 48 hours
    Result: The viability of CT-26 cells was reduced in a dose-dependent manner, with IC50 value of 0.27±0.01 μg/mL.

    Western Blot Analysis[3]

    Cell Line: Mouse Hepa-1c1c7 hepatoma cells
    Concentration: 1, 3, 10, 30, 100, 300, and 1000 nM
    Incubation Time: 2 hours
    Result: Provoked the depletion of Nrf2, in a concentration-dependent manner within 2 h of exposure to cells.
    In Vivo

    "Brusatol is able to reach the tumor tissue and inhibit the Nrf2 pathway. Nude mice are injected with A549 cells to induce tumor growth, followed by a single i.p. injection of 2 mg/kg Brusatol. Nrf2 protein levels are significantly decreased at 24 h or 48 h postinjection[1]
    Cisplatin (2 mg/kg) or Brusatol (2 mg/kg) alone does not inhibit tumor growth significantly, whereas in the combination group, tumor size is significantly reduced[1]. "

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Athymic nude mice 4-6 wk old bearing A549 xenografts[1]
    Dosage: 2 mg/kg
    Administration: Treated i.p.; Cisplatin (2 mg/kg), Brusatol (2 mg/kg), or in combination every other day for a total of five times
    Result: Nrf2 protein levels were significantly decreased at 24 h or 48 h postinjection.
    Cisplatin or Brusatol alone did not inhibit tumor growth significantly, whereas in the combination group, tumor size was significantly reduced. "
    Molecular Weight

    520.53

    Formula

    C₂₆H₃₂O₁₁

    CAS No.
    Shipping

    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)

    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (48.03 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9211 mL 9.6056 mL 19.2112 mL
    5 mM 0.3842 mL 1.9211 mL 3.8422 mL
    10 mM 0.1921 mL 0.9606 mL 1.9211 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.89%

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    Product Name:
    Brusatol
    Cat. No.:
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