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编 号:F473887
分子式:C8H18N2O3S
分子量:222.31
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50mg
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100mg
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生物活性:
L-Buthionine-(S,R)-sulfoximine is a cell-permeable, potent, fast acting and irreversible inhibitor of g-glutamylcysteine synthetase and depletes cellular glutathione levels. The IC50 value of L-Buthionine-(S,R)-sulfoximine on melanoma, breast and ovarian tumor specimens are 1.9 μM, 8.6 μM, and 29 μM, respectively.

体内研究:
BSO 导致小鼠发育过程中 DNA 缺失的频率升高。与未处理的小鼠相比,BSO 处理在 2 mM 和 20 mM BSO 剂量下分别将小鼠胎儿中的 GSH 浓度降低了 55% 和 70%。与 2 mM BSO 和 20 mM NAC 共同处理耗尽 GSH 的程度与 2 mM BSO 相似,这与 BSO 抑制 GSH 合成不可或缺的 g-GCS 酶的功能一致。与 GSH 一样,BSO 处理后半胱氨酸水平下降。Animal Model:C57BL/6J pun/pun mice.
Dosage:2 mM L-Buthionine-(S,R)-sulfoximine (BSO), 20 mM BSO, 2 mM BSO and 20 mM NAC, 20 mM NAC or unsupplemented water for 18 days from 0.5 to 18.5 d.p.c. The pH of supplemented water is as follows: 6.88, 20 mM BSO; 3.37, 2 mM BSO; 2.65, 2 mM BSO plus 20 mM NAC; and 2.58, 20 mM NAC. The pH of regular water used in our facility is ~4.
Administration:Drinking water.
Result:The average number of eye-spots (mean±SEM) is 5.36±0.29 (n=46), 7.79±0.45 (n=34) and 8.78±0.61 (n=32) in untreated controls, 2 mM L-Buthionine-(S,R)-sulfoximine (BSO) and 20 mM BSO treated mice, respectively. The 2 mM BSO treatment results in ~30% more eye-spots, and the 20 mM treatment results in 40% more eye-spots compared with untreated mice.

体外研究:
L-Buthionine-(S,R)-suLfoximine (BSO:50 μM) 处理 48 小时导致 ZAZ 和 M14 黑色素瘤细胞系 GSH 水平降低 95%,GST 酶活性降低 60%。两种细胞系中的 GST-π 蛋白和 mRNA 水平均显著降低。 L-Buthionine-(S,R)-suLfoximine (BSO) 通过不可逆地抑制 g-谷氨酰半胱氨酸合成酶诱导细胞氧化应激,g-谷氨酰半胱氨酸合成酶是合成谷胱甘肽 (GSH) 的必需酶。 L-Buthionine-(S,R)-suLfoximine (BSO) 诱导癌细胞铁死亡。
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