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BPTES
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BPTES图片
CAS NO:314045-39-1
包装:10mg
规格:98%
市场价:680元
分子量:524.68

产品介绍
GLS inhibitor
CAS:314045-39-1
分子式:C24H24N6O2S3
分子量:524.68
纯度:98%
存储:Store at -20°C

Background:

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].


参考文献:
[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.