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Glutaminase Inhibitor II, BPTES-CAS 314045-39-1-Calbiochem
| 产品编号： | 4083410 |
| 规格： | A cell-permeable, potent, selective, reversible, and uncompetitive allosteric inhibitor of kidney-type glutaminase (GLS1). Does not affect the activity of liver glutaminase. |
| CAS NO： | 314045-39-1 |
| 包装规格： | 10 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品价格查看更多规格...
| 产品编号 | 包装单位 | 单价(元) | 国内现货 | 国外库存 | 询价单 |
| 4083410 | 10 MG | 2940 |
产品别名
314045-39-1
Glutaminase Inhibitor II, BPTES-CAS 314045-39-1-Calbiochem
N,N'-(5,5'-(2,2'-Thio bis(ethane-2,1-diyl)) bis(1,3,4-thiadiazole-5,2-diyl)) bis(2-phenylacetamide), Kidney-Type Glutaminase Inhibitor II, GAC Inhibitor II, GLS1 Inhibitor II, KGA Inhibitor II
基本信息
| Empirical Formula【经验(实验)分子式】 | C24H24N6O2S3 |
| Molecular weight | 524.68 |
| MDL number | MFCD01079848 |
| General description【一般描述】 | A cell-permeable bis-thiadiazole compound that selectively inhibits GLS1 (IC50 = 60 and 80 nM, respectively, against hKGA and hGAC), but not the liver-type GLS2/LGA (IC50 = 88 µM using hLGA), mitochondrial glutaminase (GA) activity by inducing an inactive GLS1 tetrameric conformation via a 2:1 inhibitor-to-tetramer stoichiometric binding, non-competitive against glutamine or phosphate binding. B-cell lymphoma line P493 is shown to depend primarily on glutamine metabolism for survival under hypoxic condition and cellular GLS1 inhibtion by BPTES treatment results in cell death (2 µM BPTES & 3% O2 for 4 d), while under aerobic/normoxic condition (20% O2 and up to 10 µM BPTES for 4 d) only growth inhibition is observed. Likewise, intraperitoneal administration (12.5 mg/kg or 200 µg/animal; q.o.d.) is demonstrated to be efficacious in suppressing P493 tumor expansion in mice in vivo. A cell-permeable bis-thiadiazole compound that selectively inhibits GLS1 (IC50 = 60 and 80 nM, respectively, against hKGA and hGAC), but not the liver-type GLS2/LGA (IC50 = 88 µM using hLGA) mitochondrial glutaminase (GA) activity by inducing an inactive GLS1 tetrameric conformation via a 2:1 inhibitor-to-tetramer stoichiometric binding. Shown to induce growth inhibition under aerobic/normoxic (up to 10 µM; 20% O2) and cell death under hypoxic (2 µM; 3% O2) in P493 B-cell lymphoma cultures in vitro and effectively suppress P493 tumor expansion in mice in vivo (12.5 mg/kg or 200 µg/animal via i.p.; q.o.d.). |
| Biochem/physiol Actions【生化/生理作用】 | Cell permeable: yes Target IC50: 140 and 210 nM in HEK293 cells expressing wt-KGA and F318Y-cKGA, respectively Primary Target kidney-type glutaminase Reversible: yes |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. |
| Other Notes【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. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥94% (HPLC) |
| form【形式】 | powder |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze protect from light |
| color【颜色】 | yellow |
| solubility【溶解性】 | DMSO: 50 mg/mL |
| storage temp.【储存温度】 | −20℃ |
| packaging【包装】 | Packaged under inert gas |
安全信息
| Pictograms【象形图】 | GHS07 |
| Signal word【警示用语：】 | Warning |
| Hazard Statements | H315 - H319 - H335 |
| Precautionary Statements | P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338 |
| Hazard Classifications【危险分类】 | Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3 |
| Target Organs【靶器官】 | Respiratory system |
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
