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525330

Sigma-Aldrich

PFKFB3 Inhibitor, 3PO

PFKFB3 Inhibitor, 3PO, is a cell-permeable, selective inhibitor of PFK-2 (6-phosphofructo-2-Kinase) activity.

Sinónimos:

PFKFB3 Inhibitor, 3PO, (2 E)-3-Pyridin-3-yl-1-pyridin-4-ylprop-2-en-1-one, 3-(3-Pyridinyl)-1-(4-pyridinyl)-2-propen-1-one, 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 Inhibitor, 3PO

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About This Item

Fórmula empírica (notación de Hill):
C13H10N2O
Peso molecular:
210.23
Número MDL:
MFCD00224002
Código UNSPSC:
12352200
NACRES:
NA.28

Nivel de calidad

100

Ensayo

≥99% (HPLC)

Formulario

solid

fabricante / nombre comercial

Calbiochem®

condiciones de almacenamiento

OK to freeze
protect from light

color

pale yellow

solubilidad

DMSO: 50 mg/mL

Condiciones de envío

ambient

temp. de almacenamiento

2-8°C

cadena SMILES

n1cc(ccc1)\C=C\C(=O)c2ccncc2

InChI

1S/C13H10N2O/c16-13(12-5-8-14-9-6-12)4-3-11-2-1-7-15-10-11/h1-10H/b4-3+

Clave InChI

UOWGYMNWMDNSTL-ONEGZZNKSA-N

Descripción general

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.

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.

Otras notas

Clem, B., et al. 2008. Mol. Cancer Ther.7, 110.

Información legal

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

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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Brian Clem et al.
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
Juliana Escher Toller-Kawahisa et al.
Nature communications, 14(1), 4280-4280 (2023-07-18)
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
Gangqi Wang et al.
Arteriosclerosis, thrombosis, and vascular biology, 40(2), 350-364 (2019-12-13)
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

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