Brusatol (Synonyms: (+)-Brusatol, NSC 172924) |
| Catalog No.GC34070 |
Brusatol is an Nrf2 inhibitor isolated from Brucea javanica and exhibits significant tumor inhibition in multiple cancers through decreased resistance to cancer oxidative stress injury.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 14907-98-3
Sample solution is provided at 25 µL, 10mM.
Brusatol is an Nrf2 inhibitor isolated from Brucea javanica and exhibits significant tumor inhibition in multiple cancers through decreased resistance to cancer oxidative stress injury[1,2,3]. Brusatol is confirmed to inhibit the Nrf2-Notch1 pathway, increse p-P38, LC3, Beclin 1 and p-JNK expression, downregulate BRF2, IGFBP-2, P62 and CD151[3].
In vitro, Brusatol (20, 50, 100, and 200nM; 0, 24, 48, 72, and 96h) treatment at the zygotic stage prevented the early embryo development in Kunming mice embryos[4]. Brusatol (1 and 100nM; 72h) shows an antitumor effect in an acute lymphoblastic leukemia (KOPN-8 cells) model triggered by reactive oxygen species accumulation[5]. Brusatol (0.31 to 10µM; 24 or 48h) results in breast cancer retardation via Nrf2 inhibition in breast cancer cell lines[6].
In vivo, Brusatol (2mg/kg; every 48h; 5 weeks; i.p.) hinders the progression of bladder cancer by Chac1/Nrf2/SLC7A11 pathway[7]. Brusatol (NSC 172924) sensitizes endometrial hyperplasia and cancer to progestin by suppressing NRF2-TET1-AKR1C1-mediated progestin metabolism in a Brusatol (NSC 172924)-treated (10nmol/l; 3 days) endometrial cancer cell (Ishikawa and ECC1) injected nude mice model[8].
References:
[1] Yu, Xiao-Qi et al. “Brusatol: A potential anti-tumor quassinoid from *Brucea javanica*.” *Chinese herbal medicines* vol. 12,4 359-366. 19 Aug. 2020, doi:10.1016/j.chmed.2020.05.007
[2] Sutiningsih, Dwi et al. “Larvicidal Activity of Brusatol Isolated from *Brucea javanica* (L) Merr on *Culex quinquefasciatus*.” *Iranian journal of public health* vol. 48,4 (2019): 688-696.
[3] Li, Kun-Wei et al. “Brucea javanica: A review on anticancer of its pharmacological properties and clinical researches.” *Phytomedicine : international journal of phytotherapy and phytopharmacology* vol. 86 (2021): 153560. doi:10.1016/j.phymed.2021.153560
[4] Lin, Ying et al. “Nrf2 inhibition affects cell cycle progression during early mouse embryo development.” *The Journal of reproduction and development*vol. 64,1 (2018): 49-55. doi:10.1262/jrd.2017-042
[5] Jorge, Joana et al. “Antitumor Effect of Brusatol in Acute Lymphoblastic Leukemia Models Is Triggered by Reactive Oxygen Species Accumulation.” *Biomedicines* vol. 10,9 2207. 6 Sep. 2022, doi:10.3390/biomedicines10092207
[6] Bovilla, Venugopal R et al. “Targeted Inhibition of Anti-Inflammatory Regulator Nrf2 Results in Breast Cancer Retardation In Vitro and In Vivo.” *Biomedicines* vol. 9,9 1119. 30 Aug. 2021, doi:10.3390/biomedicines9091119
[7] Yu, Xi et al. “Brusatol hinders the progression of bladder cancer by Chac1/Nrf2/SLC7A11 pathway.” *Experimental cell research* vol. 438,2 (2024): 114053. doi:10.1016/j.yexcr.2024.114053
[8] Hu, Meiyan et al. “Brusatol sensitizes endometrial hyperplasia and cancer to progestin by suppressing NRF2-TET1-AKR1C1-mediated progestin metabolism.” *Laboratory investigation; a journal of technical methods and pathology* vol. 102,12 (2022): 1335-1345. doi:10.1038/s41374-022-00816-5
| Cell experiment [1]: | |
Cell lines | MCF-7, MDA-MB-231, or MDA-MB-468 |
Preparation Method | Various BC cells (MCF-7, MDA-MB-231, or MDA-MB-468) (1.0 × 104cells in 100µL DMEM with 10% FBS) were seeded in 96-well plates and cultured in an incubator at 37 °C with 5% CO2 and 90% relative humidity. Following this, when cell confluence reached about 60 to 70% (36h later), the cells were exposed to gradual concentrations of brusatol (ranging from 0.31 to 10µM) for 24 or 48h. Following this treatment, cell viability was measured using sulforhodamine B (SRB) and MTT(3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide) assays. |
Reaction Conditions | 0.31 to 10µM; 24 or 48h |
Applications | The effect of two low/non-toxic concentrations (19.5 and 78nM) of brusatol did not demonstrate any significant effect on cell viability. Brusatol provoked a significant decrease in BC cell viability; however, this effect was not dose- or time-dependent. The highest cytotoxic effects of brusatol were observed at 24 and 48h of treatment. |
| Animal experiment [2]: | |
Animal models | male BALB/c-nude mice |
Preparation Method | T24 cells were injected subcutaneously into mice at a concentration of 1×106 cells per mouse. Three mice were randomly allocated into two groups, consisting of nude mice. The experimental groups were administered intraperitoneal injections of brusatol at a dosage of 2mg/kg every 48h, whereas the control groups were given injections of normal saline. Following a treatment duration of 5 weeks, the mice were administered anesthesia and subsequently euthanized to facilitate additional analysis. Sodium pentobarbital (30mg/kg) was administered as the anesthetic drug. |
Dosage form | 2mg/kg; every 48h; 5 weeks |
Applications | The tumor size of mice treated with brusatol was significantly reduced. |
References: | |
| Cas No. | 14907-98-3 | SDF | |
| Synonyms | (+)-Brusatol, NSC 172924 | ||
| Canonical 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 | ||
| Formula | C26H32O11 | M.Wt | 520.53 |
| Solubility | DMF: 1 mg/ml,DMSO: 1 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml | Storage | 4°C, protect from light, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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