L-Buthionine-(S,R)-sulfoximine 是一种细胞渗透性和不可逆的 γ-谷氨酰半胱氨酸合成酶抑制剂,通过消耗 GSH 诱导细胞中的氧化应激,可降低细胞内谷胱甘肽的水平,其对黑色素瘤、乳腺卵巢癌标本的IC50值分别为1.9 μM、8.6 μM 和29 μM。
产品描述
L-Buthionine-(S,R)-sulfoximine is a cell-permeable and irreversible inhibitor of γ-glutamylcysteine synthetase (Ki<100 μM) that induces oxidative stress in cells by depleting GSH.
体外活性
IC50 values (microM) for L-buthionine-S,R-sulfoximine (BSO) on melanoma, breast and ovarian tumor specimens were 1.9, 8.6, and 29, respectively. The IC90 for melanoma was 25.5 microM, a level 20-fold lower than steady-state levels achieved clinically [1]. GSH loss induced by L-buthionine-S,R-sulfoximine (BSO) leads to overproduction of reactive oxygen species (ROS) and triggers apoptosis of MYCN-amplified neuroblastoma cells [2].
体内活性
Systemic BSO administration selectively altered GSH homeostasis and EAAT3 levels in the mice cerebellum. Intraperitoneal treatment of mice with 6?mmol/kg of BSO depleted GSH and GSSG in the liver at 2?h of treatment [3].
Cas No.
83730-53-4
分子式
C8H18N2O3S
分子量
222.31
别名
丁硫氨酸-亚砜亚胺;L-Butionine sulfoximine
储存和溶解度
DMSO:Insoluble
H2O:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years