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Brusatol Nrf2 inhibitor

Cat.No.S7956

Brusatol (NSC 172924), isolated from the fruit of B. javanica, is a NRF2 inhibitor.
Brusatol Nrf2 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 520.53

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 520.53 Formula

C26H32O11

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 14907-98-3 -- Storage of Stock Solutions

Synonyms NSC 172924 Smiles CC1=C(C(=O)CC2(C1CC3C45C2C(C(C(C4C(C(=O)O3)OC(=O)C=C(C)C)(OC5)C(=O)OC)O)O)C)O

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (192.11 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
Nrf2 [1]
In vitro

Brusatol provokes a rapid and transient depletion of Nrf2 protein, through a posttranscriptional mechanism, in mouse Hepa-1c1c7 hepatoma cells and freshly isolated primary human hepatocytes [1].

In vivo

Brusatol inhibits Nrf2 signaling, reduces tumor burden, and ameliorates chemoresistance in both in vitro and in vivo cancer models[1].

References

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