Brusatol (Synonyms: NSC 172924)

Name: Brusatol
Brand: MedChemExpress
SKU: HY-19543
Rating: 5.0 (40 reviews)

Cat. No.: HY-19543 Pureza: 99.94%: Ficha de datos
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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.

Para uso exclusivo en investigación. No vendemos a pacientes.

No. CAS : 14907-98-3

Tamaño	Stock	Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
1 mg	En stock	Estimated Time of Arrival: December 31
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
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Revisión del cliente

Based on 40 publication(s) in Google Scholar

40 Publications Citing Use of MCE Brusatol

Cell Proliferation/Viability Assay

Bio/Physico-chemical Assay

RT-PCR

: Brusatol purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Aug 3;15(1):6587. [Abstract]; NIC cells were treated with the Nrf2 inhibitors, Brusatol (100 nM), ML385 (2μM)), or vehicle (DMSO). Proliferation was assessed by Incucyte after 72 h.

: Brusatol purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Aug 3;15(1):6587. [Abstract]; Glucose consumption in NIC cells treated with the Nrf2 inhibitors, Brusatol (100 nM), ML385 (2μM)), or vehicle (DMSO) for 72h.

: Brusatol purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Aug 3;15(1):6587. [Abstract]; QRT-PCR analysis of Glut1 gene expression in NIC cells treated with the Nrf2 inhibitors, Brusatol (100 nM), ML385 (2μM)), or vehicle (DMSO) for 72h.

: Brusatol purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Aug 3;15(1):6587. [Abstract]; Basal, maximal (Carbonyl cyanide 4-(trifluoromethoxy)phenylhydrazone – FCCP), ATP-synthesis coupled (Oligomycin A), and non-mitochondrial (rotenone/ antimycin A) oxygen consumption rates (OCRs) of NIC cells treated with DMSO or Nrf2 inhibitor Brusatol (100 nM).

: Brusatol purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Aug 3;15(1):6587. [Abstract]; Quantification of basal OCR and extracellular acidification rates (ECAR) of NIC cells treated with the Nrf2 inhibitors, Brusatol (100 nM), ML385 (2μM)), or vehicle (DMSO) for 72h.

: 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.

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Descripciòn

IC₅₀ & Target

Nrf2^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	0.067 3 Compound: 9a	Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by WST-1 assay Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by WST-1 assay	[PMID: 33289552]
HCT-116	IC₅₀	0.067 3 Compound: 9a	Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by WST-1 assay Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by WST-1 assay	[PMID: 33289552]
HCT-116	IC₅₀	0.067 3 Compound: 9a	Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by WST-1 assay Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by WST-1 assay	[PMID: 33289552]
MCF7	IC₅₀	0.083 3 Compound: 9a	Cytotoxicity against human MCF-7 cells incubated for 72 hrs by MTT assay Cytotoxicity against human MCF-7 cells incubated for 72 hrs by MTT assay	[PMID: 33289552]
MDA-MB-231	IC₅₀	29.19 1 Compound: Brusatol	Inhibition of NRF2 in human MDA-MB-231 cells harboring ARE-GFP-Luc assessed as reduction in ARE-luciferase activity after 16 hrs by firefly luciferase reporter gene assay Inhibition of NRF2 in human MDA-MB-231 cells harboring ARE-GFP-Luc assessed as reduction in ARE-luciferase activity after 16 hrs by firefly luciferase reporter gene assay	[PMID: 31270017]
MCF7	IC₅₀	0.083 3 Compound: 9a	Cytotoxicity against human MCF-7 cells incubated for 72 hrs by MTT assay Cytotoxicity against human MCF-7 cells incubated for 72 hrs by MTT assay	[PMID: 33289552]
MDA-MB-231	IC₅₀	0.081 3 Compound: 9a	Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay	[PMID: 33289552]
MCF7	IC₅₀	0.083 3 Compound: 9a	Cytotoxicity against human MCF-7 cells incubated for 72 hrs by MTT assay Cytotoxicity against human MCF-7 cells incubated for 72 hrs by MTT assay	[PMID: 33289552]
MDA-MB-231	IC₅₀	0.081 3 Compound: 9a	Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay	[PMID: 33289552]
MDA-MB-231	IC₅₀	29.19 1 Compound: Brusatol	Inhibition of NRF2 in human MDA-MB-231 cells harboring ARE-GFP-Luc assessed as reduction in ARE-luciferase activity after 16 hrs by firefly luciferase reporter gene assay Inhibition of NRF2 in human MDA-MB-231 cells harboring ARE-GFP-Luc assessed as reduction in ARE-luciferase activity after 16 hrs by firefly luciferase reporter gene assay	[PMID: 31270017]
MDA-MB-231	IC₅₀	0.081 3 Compound: 9a	Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay	[PMID: 33289552]
MDA-MB-231	IC₅₀	29.19 1 Compound: Brusatol	Inhibition of NRF2 in human MDA-MB-231 cells harboring ARE-GFP-Luc assessed as reduction in ARE-luciferase activity after 16 hrs by firefly luciferase reporter gene assay Inhibition of NRF2 in human MDA-MB-231 cells harboring ARE-GFP-Luc assessed as reduction in ARE-luciferase activity after 16 hrs by firefly luciferase reporter gene assay	[PMID: 31270017]
PANC-1	IC₅₀	0.36 3 Compound: 9a	Cytotoxicity against human Panc-1 cells incubated for 72 hrs by sulphorhodamine B assay Cytotoxicity against human Panc-1 cells incubated for 72 hrs by sulphorhodamine B assay	[PMID: 33289552]
PANC-1	IC₅₀	0.36 3 Compound: 9a	Cytotoxicity against human Panc-1 cells incubated for 72 hrs by sulphorhodamine B assay Cytotoxicity against human Panc-1 cells incubated for 72 hrs by sulphorhodamine B assay	[PMID: 33289552]
PANC-1	IC₅₀	0.36 3 Compound: 9a	Cytotoxicity against human Panc-1 cells incubated for 72 hrs by sulphorhodamine B assay Cytotoxicity against human Panc-1 cells incubated for 72 hrs by sulphorhodamine B assay	[PMID: 33289552]
SW1990	IC₅₀	0.1 3 Compound: 9a	Antiproliferative activity against human SW1990 incubated for 72 hrs by sulphorhodamine B assay Antiproliferative activity against human SW1990 incubated for 72 hrs by sulphorhodamine B assay	[PMID: 33289552]
SW1990	IC₅₀	0.1 3 Compound: 9a	Antiproliferative activity against human SW1990 incubated for 72 hrs by sulphorhodamine B assay Antiproliferative activity against human SW1990 incubated for 72 hrs by sulphorhodamine B assay	[PMID: 33289552]
SW1990	IC₅₀	0.1 3 Compound: 9a	Antiproliferative activity against human SW1990 incubated for 72 hrs by sulphorhodamine B assay Antiproliferative activity against human SW1990 incubated for 72 hrs by sulphorhodamine B assay	[PMID: 33289552]

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. "

Peso molecular

520.53

Fòrmula

C₂₆H₃₂O₁₁

No. CAS

14907-98-3

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

Structure Classification

Initial Source

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

4°C, protect from light, stored under nitrogen

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

Solvente y solubilidad

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
10 mM	0.1921 mL	0.9606 mL	1.9211 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.

Calculadora de molaridad
Calculadora de dilución

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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.

Pureza y Documentación

Purity: 99.94%

Select Batch:

Ficha de datos (283 KB) SDS (396 KB)

COA (255 KB) HNMR (275 KB) RP-HPLC (224 KB) MS (71 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Dongmei Ren, 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. [Content Brief]

[2]. Hai-Ming Chen, et al. Synergistic antitumor effect of brusatol combined with cisplatin on colorectal cancer cells. Int J Mol Med. 2018 Mar;41(3):1447-1454. [Content Brief]

[3]. Adedamola Olayanju, et al. Brusatol provokes a rapid and transient inhibition of Nrf2 signaling and sensitizes mammalian cells to chemical toxicity-implications for therapeutic targeting of Nrf2. Free Radic Biol Med. 2015 Jan;78:202-12. [Content Brief]

Complete Stock Solution Preparation Table

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

Brusatol Related Classifications

Help & FAQs

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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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Observaciones

Brusatol (Synonyms: NSC 172924)

Revisión del cliente

40 Publications Citing Use of MCE Brusatol

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Brusatol (Synonyms: NSC 172924)

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40 Publications Citing Use of MCE Brusatol

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