1. Brusatol

Brusatol  (Synonyms: NSC 172924)

Cat. No.: HY-19543 Purity: 99.89%
COA 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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 134 In-stock
Solution
10 mM * 1 mL in DMSO USD 134 In-stock
Solid
1 mg USD 42 In-stock
5 mg USD 117 In-stock
10 mg USD 200 In-stock
25 mg USD 400 In-stock
50 mg USD 640 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 23 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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 MedChemExpress. Usage Cited in: Invest Ophthalmol Vis Sci. 2020 Jun 3;61(6):51.  [Abstract]

    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.
    • Biological Activity

    • Purity & Documentation

    • Customer Review

    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[3].

    MedChemExpress (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].?"

    MedChemExpress (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.
    Appearance

    Solid

    Color

    White to off-white

    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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light, stored under nitrogen

    *In solvent : -80°C, 1 year; -20°C, 6 months (protect from light, stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (48.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light, stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 1 year; -20°C, 6 months (protect from light, stored under nitrogen)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.89%

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light, stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9211 mL 9.6056 mL 19.2112 mL 48.0280 mL
    5 mM 0.3842 mL 1.9211 mL 3.8422 mL 9.6056 mL
    10 mM 0.1921 mL 0.9606 mL 1.9211 mL 4.8028 mL
    15 mM 0.1281 mL 0.6404 mL 1.2807 mL 3.2019 mL
    20 mM 0.0961 mL 0.4803 mL 0.9606 mL 2.4014 mL
    25 mM 0.0768 mL 0.3842 mL 0.7684 mL 1.9211 mL
    30 mM 0.0640 mL 0.3202 mL 0.6404 mL 1.6009 mL
    40 mM 0.0480 mL 0.2401 mL 0.4803 mL 1.2007 mL
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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