PFK-158

PFK-158 is a potent and selective PFKFB3 inhibitor with an IC50 value 137 nM. PFK-158 reduces glucose uptake, ATP production, lactate release, and induces apoptosis and autophagy in cancer cells. PFK-158 has broad anti-tumor activity. PFK-158 can also enhance Colistin's resistance to bacteria[1][2][3].

Product Specifications

CAS Number

[1462249-75-7]

UNSPSC

12352005

Hazard Statement

H315, H317, H318, H334, H335, H341, H361, H370, H413

Target

Apoptosis; Autophagy

Type

Reference compound

Related Pathways

Apoptosis; Autophagy

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/PFK-158.html

Concentration

10mM

Purity

98.88

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(C1=CC=NC=C1)/C=C/C2=NC3=CC(C(F)(F)F)=CC=C3C=C2

Molecular Formula

C18H11F3N2O

Molecular Weight

328.29

Precautions

H315, H317, H318, H334, H335, H341, H361, H370, H413

References & Citations

[1]Mondal S, et al. Therapeutic targeting of PFKFB3 with a novel glycolytic inhibitor PFK158 promotes lipophagy and chemosensitivity in gynecologic cancers. Int J Cancer. 2019 Jan 1;144 (1) :178-189.|[2]Zhang Y, et al. Synergistic Effect of Colistin Combined with PFK-158 against Colistin-Resistant Enterobacteriaceae. Antimicrob Agents Chemother. 2019 Jun 24;63 (7) . pii: e00271-19.|[3]Pooran Chand, et al. Pfkfb3 inhibitor and methods of use as an anti-cancer therapeutic. WO2013148228A1.