化合物WZB117 T7018

Product Introduction
Bioactivity


英文名: WZB117

描述: WZB117 是葡萄糖转运蛋白 1 抑制剂，可下调糖酵解，诱导细胞周期停滞，有抗癌细胞生长的作用。

细胞实验: Human non–small cell lung cancer (NSCLC) cell lines H1299 and A549 are treated with compound WZB117（10 μM） for 24 or 48 hours.

激酶实验: Recombinant proteins expressed with Sf21 cells and baculovirus vectors are purified with affinity chromatography. JAK kinase assay is done by a homogeneous time-resolved fluorescence assay with the peptide substrate (-EQEDEPEGDYFEWLE). Each enzyme reaction is carried out with Ruxolitinib or control, JAK enzyme, 500 nM peptide, adenosine triphosphate (ATP; 1 mM), and 2% dimethyl sulfoxide (DMSO) for 1 hour. IC50 is the INCB018424 concentration required for inhibition of 50% of the fluorescent signal.

动物实验: Male NU/J nude mice were given intraperitoneal injection with WZB117 (10 mg/kg) daily for 10 weeks.

体外活性: WZB117 treats Cancer cell resulting in decreases in levels of Glut1 protein, intracellular ATP, and glycolytic enzymes. And WZB117 inhibits glucose transport in human red blood cells. The declines in cyclin E2 as well as phosphorylated retinoblastoma and increases in ATP-sensing enzyme AMP-activated protein kinase (AMPK), lead to the cell-cycle arrest, senescence, and necrosis.

体内活性: WZB117每日通过腹腔注射给予裸鼠10 mg/kg，这些裸鼠被移植了人类A549肺癌细胞，结果显示肿瘤体积减少了70%。

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

溶解度: DMSO : 36.8 mg/mL (100 mM)
Ethanol : 36.8 mg/mL (100 mM)


关键字: GLUT | Inhibitor | WZB-117 | inhibit | Glucose transporter | WZB 117 | WZB117

相关产品: DL-TBOA | Marein | Fasentin | STF-31 | 1-Hydroxy-2-oxopomolic acid | Phloretin | Jujuboside A | Brilliant Yellow | Homoeriodictyol | Sennidin B

相关库: Anti-Breast Cancer Compound Library | Glycometabolism Compound Library | Anti-Cancer Metabolism Compound Library | Anti-Metabolism Disease Compound Library | Anti-Lung Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Active Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library

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