3PO

SKU: orb1306064

Description

3PO is a small-molecule PFKFB3 inhibitor (IC50: 22.9 μM) that impedes cancer cell proliferation by disrupting glycolysis. It reduces glucose uptake and lowers levels of Fru-2,6-BP, lactate, and ATP, making it a useful tool for studying cancer metabolism in both in vitro and in vivo models.

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 18550-98-6
• MW: 210.23
• Purity: 99.67% (May vary between batches)
• Formula: C₁₃H₁₀N₂O
• SMILES: O=C(\C=C\c1cccnc1)c1ccncc1
• Target: Glucokinase,Autophagy
• Solubility: DMSO:40 mg/mL (190.27 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2.5 mg/mL (11.89 mM);H2O:Insoluble;Ethanol:11 mg/mL (52.32 mM)

Bioactivity

• Target IC50:
  PFKFB3:22.9 μM
• In Vivo:
  Compared with vehicle control, compound 3PO treatment significantly reduced Fru-2,6-BP in tumor xenografts (vehicle: 13.1 ± 1.9 pmol/mg, 3PO: 8.5 ± 1.7 pmol/mg). 3PO also impairs (pathological) angiogenesis.
• In Vitro:
  3PO markedly attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50, 1.4-24 μM) and is selectively cytostatic to ras-transformed human bronchial epithelial cells relative to normal human bronchial epithelial cells. Compared with the wild-type PFKFB3+/+transformed cells (IC50, 49 μM), the PFKFB3+/- fibroblasts were more sensitive to compound 3PO treatment (IC50, 26 μM). 3PO Causes G2-M phase arrest, which Is preceded by decreased Fru-2,6-BP and glucose uptake. 3PO slows growth through inhibition of PFK-2 activity, then ectopic expression of the PFKFB3 isozyme may thwart the cytostatic activity of 3PO. 3PO inhibits the glycolytic regulator PFKFB3 in endothelial cells (ECs). 3PO decreases glycolysis in ECs and impairs vessel sprouting. 3PO also suppresses vascular hyperbranching induced by inhibition of Notch or VEGF receptor 1 (VEGFR1) and amplified the antiangiogenic effect of VEGF blockade.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

small-molecule, PFKFB3, chemotherapeutic agents, Autophagy, 3PO, adenocarcinoma cell, inhibit, isozyme, Inhibitor, human malignant hematopoietic

Compound Identifiers

PubChem CID

5720233