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BPTES

产品编号 T6791 CAS 314045-39-1

BPTES 是一种特异性 GlutamiN/Ase GLS1 (KGA) 抑制剂，IC50=0.16 μM。

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BPTES, CAS 314045-39-1

规格	价格/CNY	货期
1 mg	￥ 215	现货
2 mg	￥ 297	现货
5 mg	￥ 535	现货
10 mg	￥ 682	现货
25 mg	￥ 1,250	现货
50 mg	￥ 1,960	现货
100 mg	￥ 2,920	现货
200 mg	￥ 4,230	现货
500 mg	￥ 6,590	待询
1 mL * 10 mM (in DMSO)	￥ 682	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	BPTES(IC50 of 0.16 μM) is an effective and specific GlutamiN/Ase GLS1 (KGA) inhibitor.
靶点活性	Glutaminase GLS1:0.16 μM
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]
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.
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.

分子量	524.68
分子式	C24H24N6O2S3
CAS No.	314045-39-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 10.5 mg/mL (20 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9059 mL	9.5296 mL	19.0592 mL	47.6481 mL
	5 mM	0.3812 mL	1.9059 mL	3.8118 mL	9.5296 mL
	10 mM	0.1906 mL	0.953 mL	1.9059 mL	4.7648 mL
	20 mM	0.0953 mL	0.4765 mL	0.953 mL	2.3824 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Newcomb R. 2002. U.S. Pat. 6,451,828 B1. 2. Seltzer MJ, et al. Cancer Res. 2010, 70(22), 8981-81987. 3. Xiang Y, et al. J Clin Invest. 2015, 125(6), 2293-2306. 6. Lee JS, et al. Dual targeting of glutaminase 1 and thymidylate synthase elicits death synergistically in NSCLC. Cell Death Dis. 2016 Dec 8;7(12):e2511.

文献引用

1. Qi J, Gao X, Zhong X, et al. Selective inhibition of Aurora A and B kinases effectively induces cell cycle arrest in t(8;21) acute myeloid leukemia. Biomedicine & Pharmacotherapy. 2019, 117: 109113. 2. Zhu B, Wei X, Narasimhan H, et al.Inhibition of the mitochondrial pyruvate carrier simultaneously mitigates hyperinflammation and hyperglycemia in COVID-19.Science immunology.2023: eadf0348.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

BPTES 314045-39-1 Metabolism Proteases/Proteasome transporter Glutaminase inhibit Inhibitor inhibitor

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BPTES

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords