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PFK-158

Chemical Structure : PFK-158

CAS No.: 1462249-75-7

PFK-158 (PFK 158;PFK158)

Catalog No.: PC-42914Not For Human Use, Lab Use Only.

PFK-158 is the first potent, selective and competitive small molecule inhibitor of PFKFB3 with IC50 of 137 nM, inhibits glycolysis, induces apoptosis and autophagy.

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Biological Activity

PFK-158 is the first potent, selective and competitive small molecule inhibitor of PFKFB3 with IC50 of 137 nM, inhibits glycolysis, induces apoptosis and autophagy.
PFK-158 reduces glucose uptake, ATP production, lactate release, and induces apoptosis and autophagy in cancer cells.
PFK-158 has synergistic anti-proliferative effects in vitro when combined with Cisplatin in C13 and HeyA8MDR cells.
PFK-158 shows a dose-dependent downregulation of p62/SQSTM1 and upregulation of LC3BII, two markers of autophagy induction, in both C13 and HeyA8MDR cells.
PFK-158 combined with CBPt treatment leads to significantly enhanced antitumor activity in a gynecologic cancer mouse model.
PFK-158 is more potent than 3PO with improved PK properties.

Physicochemical Properties

M.Wt 328.288
Formula C18H11F3N2O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 30 mg/mL

Chemical Name/SMILES

2-Propen-1-one, 1-(4-pyridinyl)-3-[7-(trifluoromethyl)-2-quinolinyl]-, (2E)-

References

1. Sucheta Telang, et al. Cancer Metab. 2014; 2(Suppl 1): P14.

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