In vitro: WZB117 inhibits glucose transport in human red blood cells. Cancer cell treatment with WZB117 leads to decreases in levels of Glut1 protein, intracellular ATP, and glycolytic enzymes. All these changes are followed by increase in ATP-sensing enzyme AMP-activated protein kinase (AMPK) and declines in cyclin E2 as well as phosphorylated retinoblastoma, resulting in cell-cycle arrest, senescence, and necrosis.
In vivo: Daily intraperitoneal injection of WZB117 at 10mg/kg resultes in 70% reduction in tumor volume of human A549 lung cancer grafted on nude mice.
|Cell lines||Human non–small cell lung cancer (NSCLC) cell|
|Preparation method||Cells were treated with compound WZB117 for 24 or 48 hours. WZB117 (10 μmol/L) was used in the experiments unless otherwise noted.|
|Incubation time||24 or 48 h|
|Animal models||BALB/cAJcl-nu/nu mice|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||73 mg/mL in DMSO|
Targeting the facilitative glucose transporter GLUT1 inhibits the self-renewal and tumor-initiating capacity of cancer stem cells.
Shibuya K, et al. Oncotarget. 2015 Jan 20;6(2):651-61. PMID: 25528771.
A small-molecule inhibitor of glucose transporter 1 downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo.
Liu Y, et al. Mol Cancer Ther. 2012 Aug;11(8):1672-82. PMID: 22689530.
7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for inhibition of [14C]-lactate influx; new antitumor treatment targeting lactate transport in cancer cells. IC50 value: 11 nM ([14C]-lactate influx).
7ACC1(DEAC; Coumarin D 1421; D 1421) selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.
Avibactam sodium is a covalent, reversible β-lactamase inhibitor, inhibits β-lactamase TEM-1 and CTX-M-15 with IC50 of 8 nM and 5 nM, respectively.
|AHU-377 hemicalcium salt
AHU-377 hemicalcium salt is a potent NEP inhibitor with an IC50 of 5 nM. AHU-377 is a component of the heart failure medicine LCZ696.
Isavuconazole is a moderate inhibitor of CYP3A4 and a water-soluble triazole with broad-spectrum antifungal activity.
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