BSO

製品コードS9728 バッチS972801

印刷

化学情報

 Chemical Structure Synonyms L-Buthionine sulfoximine, l-BSO Storage
(From the date of receipt)
3 years -20°C powder
化学式

C8H18N2O3S

分子量 222.31 CAS No. 83730-53-4
Solubility (25°C)* 体外 Water 40 mg/mL (179.92 mM)
DMSO Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 BSO is a cell-permeable, potent, fast acting and irreversible inhibitor of g-glutamylcysteine synthetase (γ-glutamylcysteine synthetase, γ-GCS) and depletes cellular glutathione levels. The IC50 of BSO on melanoma, breast and ovarian tumor specimens are 1.9 μM, 8.6 μM, and 29 μM, respectively.
in vitro

BSO (L-Buthionine-(S,R)-sulfoximine) synergistically enhanced BCNU activity against melanoma cell lines and human tumors. This compound (50 μM) treatment for 48 hr results in a 95% decrease in ZAZ and M14 melanoma cell line GSH levels, and a 60% decrease in GST enzyme activity. GST-μ protein and mRNA levels are significantly reduced in both cell lines. GST-π expression is unaffected. This chemical enhancement of alkylator action may be related in part to down regulation of GST.[1]

in vivo

LButhionine-S,R-sulfoximine (L-S,R-BSO) substantially inhibits GSH production at a greater degree and causes a higher toxicity to guinea pigs than mice, implying that mice may have an additional protective mechanism against oxidative stress injury. Indeed, administration of this compound to mice inhibits tissue GSH production while increasing ascorbate levels. This chemical also increases tissue ascorbate levels in mice fed a ascorbate and dehydroascorbatefree diet suggesting activation of ascorbate synthesis, which is further confirmed by increased urinary ascorbate excretion.[2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 ZAZ, M14 melanoma cell line
濃度 50 μM
反応時間 6 h, 24 h, 48 h, 72 h
実験の流れ

The effect of BSO treatment on glutathione content (GSH + GSSG) is determined on cells plated in 24-well plates at the same density as in the thymidine incorporation assay. GSH is measured at time zero, and at 6, 24, 48, and 72 hr by a modified Tietze method. GSH standard curves are obtained by dissolving 5 mg GSH in 25 ml 0.01 N HCl and running determinations on serial dilutions. Cell supernatants are prepared by freezethawing cells resuspended to 107 cells per ml in 0.01 M NaP04 + 0.005 M EDTA buffer (pH 7.5) three times, and centrifuging for 30 min at 30,000g at 4℃. GSH levels are determined from the rate of change in optical density at 412 nm, 25℃.

動物実験 動物モデル Swiss-Webster mice, guinea pigs
投薬量 2.5 mM/kg, 1.25 mM/kg, 0.625 mM/kg
投与方法 SC

参考

  • https://pubmed.ncbi.nlm.nih.gov/9263331/
  • https://pubmed.ncbi.nlm.nih.gov/28115164/

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人間や獣医の診断であるか治療的な使用のためにでない。

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