525330

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

Properties

• 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

Description

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable