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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.

Synonym(s):

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

Empirical Formula (Hill Notation):
C13H10N2O
Molecular Weight:
210.23
MDL number:
MFCD00224002
UNSPSC Code:
12352200
NACRES:
NA.28

Quality Level

100

Assay

≥99% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

pale yellow

solubility

DMSO: 50 mg/mL

shipped in

ambient

storage temp.

2-8°C

General description

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.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘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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