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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Glutaminase-BPTES
BPTES

Chemical Structure : BPTES

CAS No.: 314045-39-1

BPTES

货号: PC-43147Not For Human Use, Lab Use Only.

BPTES is a potent, selective kidney-type glutaminase 1 (GLS1) inhibitor with Ki of 3 uM (rat KGA), selective for GLS1 over GLS2, glutamate dehydrogenase, and γ-glutamyl transpeptidase.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BPTES is a potent, selective kidney-type glutaminase 1 (GLS1) inhibitor with Ki of 3 uM (rat KGA), selective for GLS1 over GLS2, glutamate dehydrogenase, and γ-glutamyl transpeptidase.
BPTES inhibits the allosteric activation caused by phosphate binding and promotes the formation of an inactive complex.
BPTES slows growth of glioblastoma cells expressing mutant IDH1 compared with those expressing wild-type IDH1, lowers glutamate and α-KG levels, and increases glycolytic intermediates while leaving total 2-HG levels unaffected.
BPTES nanoparticles significantly reduces pancreatic tumor combined with metformin in vivo.

物理化学性质&存储条件

分子量 524.6813
分子式 C24H24N6O2S3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: < 41 mg/mL

Chemical Name/SMILES

Benzeneacetamide, N,N'-[thiobis(2,1-ethanediyl-1,3,4-thiadiazole-5,2-diyl)]bis-

参考文献

1. Robinson MM, et al. Biochem J. 2007 Sep 15;406(3):407-14.

2. Seltzer MJ, et al. Cancer Res. 2010 Nov 15;70(22):8981-7.

3. Elgogary A, et al. Proc Natl Acad Sci U S A. 2016 Sep 6;113(36):E5328-36.

4. Shukla K, et al. J Med Chem. 2012 Dec 13;55(23):10551-63.

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