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. BSO (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. BSO 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 L-S,R-BSO to mice inhibits tissue GSH production while increasing ascorbate levels. L-S,R-BSO 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

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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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