BPTES
目录号 : GC13958
BPTES是一种高效且选择性的肾型谷氨酰胺酶（GLS）变构抑制剂，已被用作分子探针以确定GLS抑制的治疗潜力。
Cas No.:314045-39-1
Sample solution is provided at 25 µL, 10mM.
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BPTES is a potent and selective allosteric inhibitor of kidney-type glutaminase (GLS) that has served as a molecular probe to determine the therapeutic potential of GLS inhibition[1].
In vitro, BPTES (2, 5 and 10μM) could effectively and specifically suppress NLRP1b inflammasome activation in macrophages[2]. BPTES (10μM; 6h) pretreatments increased the toxic effects of cisplatin and etoposide on HCC1937 and BT-549 cells[3]. BPTES (0, 0.05, 0.5, 1, 2.5 and 5μM; 72h) selectively eliminates human skin senescent fibroblasts[4]. BPTES (10μM; 24h) reduces Extracellular vesicle (EV) release in HIV-1-infected macrophages and immune-activated microglia[5].
In vivo, BPTES (1mg/kg; 1h; i.p.) can block the anthrax lethal toxin-induced mortality and tissue injury in mice by preventing injury to lungs, adrenal glands and intestine[2]. BPTES (0.25mg/20g/200μL; 2-3 times a week for 1 month; i.p.) can eliminate SA-β-Gal-positive cells in a human skin graft chimera model in mice[4].
References:
[1] Shukla K, Ferraris DV, Thomas AG, et al. Design, synthesis, and pharmacological evaluation of bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide 3 (BPTES) analogs as glutaminase inhibitors. J Med Chem. 2012 Dec 13;55(23):10551-63.
[2] Wang J, Yang D, Shen X, et al. BPTES inhibits anthrax lethal toxin-induced inflammatory response. Int Immunopharmacol. 2020 Aug;85:106664.
[3] Chen L, Cui H, Fang J, et al. Glutamine deprivation plus BPTES alters etoposide- and cisplatin-induced apoptosis in triple negative breast cancer cells. Oncotarget. 2016 Aug 23;7(34):54691-54701.
[4] Takaya K, Ishii T, Asou T, et al. Glutaminase inhibitors rejuvenate human skin via clearance of senescent cells: a study using a mouse/human chimeric model. Aging (Albany NY). 2022 Nov 21;14(22):8914-8926.
[5] Wu B, Liu J, Zhao R, et al. Glutaminase 1 regulates the release of extracellular vesicles during neuroinflammation through key metabolic intermediate alpha-ketoglutarate. J Neuroinflammation. 2018 Mar 14;15(1):79.
BPTES是一种高效且选择性的肾型谷氨酰胺酶（GLS）变构抑制剂，已被用作分子探针以确定GLS抑制的治疗潜力[1]。
在体外实验中，体外实验中，BPTES（2, 5和10μM）能够有效且特异性地抑制巨噬细胞中NLRP1b炎症体的激活[2]。BPTES（10μM; 6小时）预处理可增强顺铂和依托泊苷对HCC1937和BT-549细胞的毒性作用[3]。BPTES（0, 0.05, 0.5, 1, 2.5和5μM; 72小时）选择性地清除人皮肤衰老成纤维细胞[4]。BPTES（10μM; 24小时）减少HIV-1感染巨噬细胞和免疫激活小胶质细胞中外泌体（EV）的释放[5]。
在体内实验中，BPTES（1mg/kg; 1小时; 腹腔注射）可以通过防止肺部、肾上腺和肠道损伤，阻断炭疽致死毒素诱导的小鼠死亡和组织损伤[2]。BPTES（0.25mg/20g/200μL; 每周2-3次，持续 1 个月; 腹腔注射）可以在小鼠的人类皮肤移植嵌合体模型中清除SA-β-Gal阳性细胞[4]。
| Cell experiment [1]: | |
Cell lines | HCC1937 and BT-549 cells |
Preparation Method | HCC1937 and BT-549 cells were pretreated with 10μM BPTES for 6h and then treated with 5μM etoposide or cisplatin for 48h. The expressions of cleaved-PARP, cleaved-caspase 3, cleaved-caspase 9, Bcl-2, and BAX in HCC1937 and BT-549 cells were measured by immunoblotting. Cell apoptosis was measured by flow cytometry in BT-549 and HCC1937 cells. |
Reaction Conditions | 10μM; 6h |
Applications | BPTES pretreatments increased the toxic effects of cisplatin and etoposide on HCC1937 and BT-549 cells. |
| Animal experiment [2]: | |
Animal models | 4-week-old female Balb/c mice |
Preparation Method | Four-week-old female Balb/c mice were pretreated with vehicle or 1mg/kg BPTES via intraperitoneal injection for 1h, and then subjected to intravenous injection of 500mg/kg lethal factor (LF) and protective antigen (PA). Mouse survival was measured up to 150h. |
Dosage form | 1mg/kg; 1h; i.p. |
Applications | BPTES can block the anthrax lethal toxin-induced mortality and tissue injury in mice by preventing injury to lungs, adrenal glands and intestine. |
References: | |
| Cas No. | 314045-39-1 | SDF | |
| 化学名 | (1Z,1'Z)-N',N''-(5,5'-(thiobis(ethane-2,1-diyl))bis(1,3,4-thiadiazole-5,2-diyl))bis(2-phenylacetimidic acid) | ||
| Canonical SMILES | O/C(CC1=CC=CC=C1)=N\C2=NN=C(S2)CCSCCC(S3)=NN=C3/N=C(O)/CC4=CC=CC=C4 | ||
| 分子式 | C24H24N6O2S3 | 分子量 | 524.68 |
| 溶解度 | ≥ 18 mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9059 mL | 9.5296 mL | 19.0592 mL |
| 5 mM | 0.3812 mL | 1.9059 mL | 3.8118 mL |
| 10 mM | 0.1906 mL | 0.953 mL | 1.9059 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet