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BPTES Sale

目录号 : GC13958

An allosteric inhibitor of GLS1

BPTES Chemical Structure

Cas No.:314045-39-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥494.00
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1mg
¥220.00
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10mg
¥567.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

AML cells

Preparation method

The solubility of this compound in DMSO is > 18 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

20 or 40 μM

Applications

After being exposed to 20 μM BPTES for 4 days, all IDH1-mutant AML cells were reduced approximately by 50%. The doses of 20 μM and 40 μM exhibited similar effects. However, BPTES did not significantly affect the growth of wild type AML cells. According to the mass spectrometry analysis, BPTES did not significantly change α-KG or 2-HG levels in IDH-mutant or wild type AML cells.

Animal experiment [2]:

Animal models

Mice harboring P493 tumor xenografts

Dosage form

200 μg; i.p.; every 3 days for 10 days

Applications

In mice harboring P493 tumor xenografts, BPTES reduced tumor growth by approximately 50% over a 10-day treatment period. However, BPTES did not inhibit the growth of P493 xenografts expressing wild type GLS or BPTES-resistant mutant GLS K325A. According to the metabolic analysis of P493 xenografts, BPTES treatment increased tumor glutamine levels and decreased glutamate levels.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Emadi A, Jun SA, Tsukamoto T, et al. Inhibition of glutaminase selectively suppresses the growth of primary acute myeloid leukemia cells with IDH mutations. Experimental hematology, 2014, 42(4): 247-251.

[2]. Xiang Y, Stine ZE, Xia J, Lu Y, O'Connor RS, Altman BJ, Hsieh AL, Gouw AM, Thomas AG, Gao P, Sun L, Song L, Yan B, Slusher BS, Zhuo J, Ooi LL, Lee CG, Mancuso A, McCallion AS, Le A, Milone MC, Rayport S, Felsher DW, Dang CV. Targeted inhibition of tumor-specific glutaminase diminishes cell-autonomous tumorigenesis. J Clin Invest. 2015 Jun;125(6):2293-306.

产品描述

BPTES is a potent and selective kidney-type glutaminase (GLS) inhibitor [1], with a Ki value of approx. 3 μM [2].

Glutaminase hydrolyzes glutamine into ammonia and glutamate. In mammalian tissues, two glutaminase isoforms derived from structurally related but distinct genes, are expressed. GLS is widely distributed in extra-hepatic tissues. Liver-type glutaminase (GLS2) is primarily found in adult liver. GLS is critical in glutaminolysis for many proliferating cells, especially malignant cells with rapid growth [1].

Cell lines with mutations in isocitrate dehydrogenase 1 and 2 (IDH1/2) were used. In all IDH1-mutant AML cells, compared with DMSO, exposure to 20 µmol/L BPTES reduced the cell growth by approximately 50% on day 4. 20 µmol/L BPTES was not significantly different from 40 µmol/L BPTES in the reduction effect. Treatment without drug was not significantly different from treatment with DMSO in the growth of cells. BPTES did not significantly affect the cell growth of wild type AML cells [3]. In tumor cells, BPTES inhibited the conversion of glutamine into glutamate [4].

Glutamate is a substrate of GPT in the transamination of pyruvate to alanine. Compared with controls, BPTES treatment reduced the pyruvate-to-alanine conversion in animals. In replicated experiments, BPTES significantly reduce the alanine-to-pyruvate (Ala/Pyr) flux ratio [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. Journal of medicinal chemistry, 2012, 55(23): 10551-10563.
[2].  Robinson MM, Mcbryant SJ, Tsukamoto T, et al. Novel mechanism of inhibition of rat kidney-type glutaminase by bis-2-(5-phenylacetamido-1, 2, 4-thiadiazol-2-yl) ethyl sulfide (BPTES). Biochemical Journal, 2007, 406(3): 407-414.
[3].  Emadi A, Jun SA, Tsukamoto T, et al. Inhibition of glutaminase selectively suppresses the growth of primary acute myeloid leukemia cells with IDH mutations. Experimental hematology, 2014, 42(4): 247-251.
[4].  Dutta P, Le A, Vander Jagt DL, et al. Evaluation of LDH-A and glutaminase inhibition in vivo by hyperpolarized 13C-pyruvate magnetic resonance spectroscopy of tumors. Cancer research, 2013, 73(14): 4190-4195.

Chemical Properties

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。
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。

溶解性数据

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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
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