推荐产品
方案
≥94% (HPLC)
质量水平
表单
powder
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
yellow
溶解性
DMSO: 50 mg/mL
储存温度
−20°C
SMILES字符串
[s]1c(nnc1CCSCCc3[s]c(nn3)NC(=O)Cc4ccccc4)NC(=O)Cc2ccccc2
InChI
1S/C24H24N6O2S3/c31-19(15-17-7-3-1-4-8-17)25-23-29-27-21(34-23)11-13-33-14-12-22-28-30-24(35-22)26-20(32)16-18-9-5-2-6-10-18/h1-10H,11-16H2,(H,25,29,31)(H,26,30,32)
InChI key
MDJIPXYRSZHCFS-UHFFFAOYSA-N
一般描述
Glutaminase Inhibitor II,Bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide (BPTES)is a cell-permeable bis-thiadiazole compound that selectivelyinhibits glutaminase-1(GLS1). It does not inhibit the liver-type GLS-2 mitochondrialglutaminase activity. It exerts its effect by inducing an inactive GLS1tetrameric conformation via a 2:1 inhibitor-to-tetramer stoichiometric binding.BPTES blocks the growth under aerobic/ normoxic conditions, and promotes celldeath under hypoxic conditions in P493 B-cell lymphoma cultures invitro, and effectively suppresses P493 tumor expansion in mice invivo.BPTES has been observedto be active in several cancer cells as it prevents cancer cellproliferation.
应用
Glutaminase Inhibitor II, BPTES has been used asa glutaminase inhibitor to study its effects on the release of extracellularvesicles (EVs) in human immunodeficiency virus (HIV-1) infected macrophages.
生化/生理作用
主要靶标
肾型谷氨酰胺酶
肾型谷氨酰胺酶
可逆性：是
细胞可渗透性：具有
靶标IC50：在表达wt-KGA和F318Y-cKGA的HEK293细胞中分别为140和210 nM
包装
用惰性气体包装
警告
毒性：标准处理（A）
重悬
复溶后，等分并冷冻保存（-20°C）。贮备液在-20°C下可稳定保存至多6个月。
其他说明
Shukla, K., et al. 2012.J. Med. Chem.55, 10551.
Thangavelu, K., et al. 2012.Proc.Natl.Acad.Sci. USA109, 7705.
Le, A., et al. 2012.Cell Metab.15, 110.
DeLaBarre, B., et al. 2011.Biochemistry 50, 10764.
Seltzer, M.J., et al. 2010.Cancer Res.70, 8981.
Robinson, M.M., et al. 2007.Biochem.J.406, 407.
Thangavelu, K., et al. 2012.Proc.Natl.Acad.Sci. USA109, 7705.
Le, A., et al. 2012.Cell Metab.15, 110.
DeLaBarre, B., et al. 2011.Biochemistry 50, 10764.
Seltzer, M.J., et al. 2010.Cancer Res.70, 8981.
Robinson, M.M., et al. 2007.Biochem.J.406, 407.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
警示用语：
Warning
危险分类
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
靶器官
Respiratory system
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Glutaminase 1 regulates the release of extracellular vesicles during neuroinflammation through key metabolic intermediate alpha-ketoglutarate
Beiqing W, et al.
Journal of Neuroinflammation (2018)
Charles J McDonald et al.
Neurochemistry international, 88, 10-14 (2014-12-17)
The GLS1 gene encodes a mitochondrial glutaminase that is highly expressed in brain, kidney, small intestine and many transformed cells. Recent studies have identified multiple lysine residues in glutaminase that are sites of N-acetylation. Interestingly, these sites are located within
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