A cell-permeable dipyridinyl-propenone compound that selectively blocks PFK-2 (6-phosphofructo-2-kinase) activity of PFKFB3 isozyme over PFK-1(6-phosphofructo-1-kinase) in a mixed-mode manner. Rapidly decreases fructose-2,6-bisphosphate (F-2,6-P2) and 2-deoxyglucose uptake, and lactate secretion; efficiently arrests proliferation of transformed cells (IC50 ~ 1.4 µM in NHBE-ht/LT/ras) and suppresses tumor growth in several xenograft mouse models (70 mg/kg, i.p.). The cytostatic and cytotoxic effects of 3PO is shown to be highly sensitive to the intracellular levels of F-6-P (fructose-6-phosphate) and F-2,6-P2.
Conditionnement
Packaged under inert gas
Avertissement
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
Autres remarques
Clem, B., et al. 2008. Mol. Cancer Ther.7, 110.
Informations légales
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 3
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
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Molecular cancer therapeutics, 7(1), 110-120 (2008-01-19)
6-phosphofructo-1-kinase, a rate-limiting enzyme of glycolysis, is activated in neoplastic cells by fructose-2,6-bisphosphate (Fru-2,6-BP), a product of four 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase isozymes (PFKFB1-4). The inducible PFKFB3 isozyme is constitutively expressed by neoplastic cells and required for the high glycolytic rate and anchorage-independent
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Endothelial cells exposed to laminar shear stress express a thick glycocalyx on their surface that plays an important role in reducing vascular permeability and endothelial anti-inflammatory, antithrombotic, and antiangiogenic properties. Production and maintenance of this glycocalyx layer is dependent on
Neutrophils rely predominantly on glycolytic metabolism for their biological functions, including reactive oxygen species (ROS) production. Although pyruvate kinase M2 (PKM2) is a glycolytic enzyme known to be involved in metabolic reprogramming and gene transcription in many immune cell types
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