葡萄糖转运蛋白抑制剂 IV,WZB117-CAS 1223397-11-2-Calbiochem,25MG,400036-25MGCN,Sigma

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订货号 0BV5109
品牌型号 Sigma 400036-25MGCN
货期 询货期
最小订货量 1件
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产品介绍 Product Description

General description

A bis-hydroxybenzoate compound that acts as a fast-acting, irreversible blocker of glucose transport by GLUT1 in red blood cells. Shown to rapidly inhibit glucose transport in cancer cells (IC50 ~ 500 nM in A549 cells) and block proliferation. Its inhibitory effects are more pronounced in hypoxic cancer cells. It binds directly to GLUT1 involving three hydrogen bonds, one each with Asn34, Arg126, and Trp412. Also shown to reduce the levels of GLUT1 protein, intracellular ATP levels, and glycolytic enzymes and increase the level of AMPK in tumor cells. Preferentially induces cell cycle arrest and causes senescence and necrosis in red blood cells and tumor cells (IC50 = 10 µM) over non cancerous cells and synergizes the anti-tumor effects of cisplatin (Cat. No. 232120 ) and paclitaxel (Cat. No. 580555). Also, effectively suppresses tumor growth in human A549 lung cancer grafted nude mice model (10 mg/kg, i.p., daily).


Biochem/physiol Actions

Cell permeable: yes
Primary Target
Glut1
Reversible: no


Packaging

Packaged under inert gas


Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 weeks at -20°C. Unstable in DMSO.


Other Notes

Liu. Y., et al. 2012. Mol. Cancer Ther.11, 1672.


Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany


Disclaimer

Toxicity: Standard Handling (A)


技术参数 Specifications
Quality Segment100
assay≥98% (HPLC)
formpowder
manufacturer/tradenameCalbiochem®
storage conditionOK to freeze,desiccated,protect from light
color white
solubilityethanol: 100 mg/mL
shipped inambient
storage temp.−20°C
SMILES stringFc1c(c(ccc1)OC(=O)c3cc(ccc3)O)OC(=O)c2cc(ccc2)O
InChI keyFRSWCCBXIHFKKY-UHFFFAOYSA-N
长度(mm)
宽度(mm)
高度(mm)
重量(kg)
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