Brusatol

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Brusatol 是从鸦胆子植物中分离出来的天然产物。它抑制 Nrf2。

Brusatol is a natural product isolated from the Brucea javanica plant. It inhibits Nrf2.

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.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. Cell Viability Assay 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 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.

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.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.?" Animal Model:Athymic nude mice 4-6 wk old bearing A549 xenografts 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.?"

NSC 172924 | (+)-Brusatol

Nuclear Receptor/Transcription Factor

Keap1-Nrf2

Nrf2

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14907-98-3

520.53

C26H32O11

>98% (HPLC)

DMSO: 90 mg/mL (172.9 mM);Water: Insoluble

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

(11beta12alpha15beta)-1320-Epoxy-31112-trihydroxy-15-((3-methyl-1-oxo-2-butenyl)oxy)-216-dioxopicras-3-en-21-oic acid methyl ester

(-20℃)

With Ice Pack

≥ 2 years