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- CAS号：
314045-39-1
- 规格：
1mg/1mLx10mM(inDMSO)/2mg/5mg/10mg/25mg/50mg/100mg/200mg/500mg
| 规格： | 1mg | 产品价格： | ￥188.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥545.0 |
| 规格： | 2mg | 产品价格： | ￥253.0 |
| 规格： | 5mg | 产品价格： | ￥428.0 |
| 规格： | 10mg | 产品价格： | ￥545.0 |
| 规格： | 25mg | 产品价格： | ￥1000.0 |
| 规格： | 50mg | 产品价格： | ￥1568.0 |
| 规格： | 100mg | 产品价格： | ￥2336.0 |
| 规格： | 200mg | 产品价格： | ￥3384.0 |
| 规格： | 500mg | 产品价格： | ￥5272.0 |
Product Introduction
Bioactivity
| 名称 | BPTES |
| 描述 | BPTES(IC50 of 0.16 μM) is an effective and specific GlutamiN/Ase GLS1 (KGA) inhibitor. |
| 细胞实验 | BPTES is dissolved in DMSO. Cells are plated at a density of 500 cells/well in a 96-well black clear bottom plate. At 24 hrs, media is changed to the appropriate media (DMEM with 4.5 g/L, 1.5 g/L or 0.1 g/L glucose, 10% FBS, pencillin/streptomycin, and 4 mM glutamine with or without doxycyline). 48 hours after plating, compounds or DMSO are added. Media and alamarBlue is added to a volume of 200 μL in each well. Fluorescence is measured at 48 hrs or 72 hrs (EGCG) using a Victor3 plate-reader. |
| 激酶实验 | Glutaminase Inhibition: Cell Free Assay: Assay plates are prepared containing 2 μL test compound in DMSO/well. The enzyme is diluted to 1 unit (liver) or 0.8 unit (kidney)/100 μL in glutaminase assay buffer, and 100 μL diluted enzyme is added to each well of the assay plate by Multidrop. The contents are mixed by shaking at full speed for 1 min on TiterMix 100. The plates are preincubated at room temperature (RT) for 20 min to allow binding of test compounds to glutaminase, and 50 μL glutamine solution (7 mM in assay buffer) is added to each well by Multidrop. The contents are shaken at full speed for 30 sec on TiterMix 100, and the plates are then incubated at RT for 60 min (liver) or 90 min (kidney). To stop the reactions, 20 μL HCl (0.3 N) is added to each well by Multidrop and mixed immediately by shaking for 30 sec on TiterMix 100. For quantification, glutamate (formed by glutaminase-catalyzed hydrolysis of glutamine) is oxidized to 2-oxoglutarate by a second enzyme, glutamate dehydrogenase (GDH), with the concomitant production of the reduced form of nicotinamide adenine dinucleotide (NADH). Reduction of nitro blue tetrazolium (NBT) in the assay solution by NADH, catalyzed by phenazine methosulphate (PMS), results in the formation of a blue-purple formazan. The absorption of formazan at 540 nm is linearly proportional to the concentration of glutamate up to 200 μM. NBT/GDH reagent (50 μL) is added to each well by Multidrop and mixed by shaking for 30 sec on TiterMix 100, and the plates are incubated at RT for 20 min to allow color formation by the GDH reaction. Glutamate concentration is determined from formazan concentration as determined by reading OD540 nm on a SpectraMax 340. |
| 体外活性 | BI-9564 with EC50 of 800 nM.BRD7 implied as a tumor suppressor and is down-regulated in cancer cells, BI-9564 shows Kd of 73 nM for it, and is >10-fold more selective for BRD9 over the high homologues bromodomain. BI-9564 (<5 μM) shows no activity against 324 kinases, when BI-9564 at 10 μM, an inhibition >40% is observed for only 2 out of 55 GPCRs. |
| 体内活性 | In LAP/MYC mice, BPTES (12.5 mg/kg, i.p.) prolongs survival with no significant effects on MYC, GLS, or GLS2 levels. BPTES (200 μg/mouse, i.p.) also inhibits tumor cell growth in mice harboring P493 tumor xenografts. [3] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 35.71 mg/mL (68.06 mM), Sonication is recommended. |
| 关键字 | Inhibitor | inhibit | Glutaminase GLS1 (KGA) | Glutaminase | BPTES |
| 相关产品 | Evans blue | Allyl Methyl Sulfide | Brilliant Yellow | Phloretin | N-Phenylacrylamide | GK921 | Telaglenastat | TG2-IN-3h | Cystamine dihydrochloride | Decanoic Acid | SLC26A3-IN-1 | BAY-876 |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Bioactive Compounds Library Max | Anti-Cancer Metabolism Compound Library | Metabolism Compound Library | Highly Selective Inhibitor Library | NO PAINS Compound Library | Glutamine Metabolism Compound Library | Multi-Target Compound Library | Membrane Protein-targeted Compound Library | Anti-Metabolism Disease Compound Library |
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网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 BPTES【314045-39-1】
￥188 - 5272
