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PFK-015

Catalog No. T2455   CAS 4382-63-2
Synonyms: PFK15, PFK 015

PFK-015 (PFK15) is an effective inhibitor of PFKFB3 (IC50: 110 nM) and inhibits PFKFB3 activity in Y cells (IC50: 20 nM).

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PFK-015 Chemical Structure
PFK-015, CAS 4382-63-2
Pack Size Availability Price/USD Quantity
5 mg In stock $ 52.00
10 mg In stock $ 81.00
25 mg In stock $ 162.00
50 mg In stock $ 297.00
100 mg In stock $ 441.00
200 mg In stock $ 612.00
500 mg In stock $ 976.00
1 mL * 10 mM (in DMSO) In stock $ 52.00
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Purity: 99.7%
Purity: 98.94%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PFK-015 (PFK15) is an effective inhibitor of PFKFB3 (IC50: 110 nM) and inhibits PFKFB3 activity in Y cells (IC50: 20 nM).
Targets&IC50 PFKFB3:110 nM, PFKFB3:20 nM
In vitro PFK-015 (25 mg/kg, i.p.) inhibits the growth, metastatic spread, and glucose metabolism of LLC tumors in syngeneic mice. In three distinct athymic mouse models of xenografted human cancers, the anticancer efficacy of PFK-015 is comparable to that of established chemotherapy drugs. PFK-015 exhibits favorable pharmacokinetic properties in vivo.
In vivo PFK-015 effectively reduces levels of F26BP, glucose uptake, and intracellular adenosine triphosphate (ATP) in Jurkat T-cell leukemia cells and H522 lung adenocarcinoma cells. Additionally, PFK-015 exhibits significant inhibitory effects on the growth of a variety of cancer cells.
Kinase Assay Recombinant PFKFB3 assay: Kinase reactions are conducted by incubating 13 ng of recombinant human PFKFB3 protein in a reaction mix containing 10 μmol/L ATP, 10 μmol/L F6P, and either dimethyl sulfoxide (DMSO) vehicle control, 3PO, or PFK15 for 1 hour at room temperature. Kinase activity is measured with the Adapta Universal Kinase Assay per manufacturer
Cell Research Viability is determined using trypan blue exclusion. Cells were incubated in 20% trypan blue for 5 minutes. Cells excluding trypan blue are counted using a standard hemocytometer to determine the total number of viable cells. Experiments are conducted in triplicate. (Only for Reference)
Synonyms PFK15, PFK 015
Molecular Weight 260.29
Formula C17H12N2O
CAS No. 4382-63-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 26 mg/mL (100 mM)

TargetMolReferences and Literature

1. Clem BF, et al. Mol Cancer Ther. 2013, 12(8), 1461-1470. 2. Zhang Y, Wang X, Li X, et al. Synergistic effect of colistin combined with PFK-158 against colistin-resistant Enterobacteriaceae[J]. Antimicrobial agents and chemotherapy. 2019, 63(7): e00271-19.

TargetMolCitations

1. Zhang Y, Wang X, Li X, et al. Synergistic effect of colistin combined with PFK-158 against colistin-resistant Enterobacteriaceae. Antimicrobial Agents and Chemotherapy. 2019, 63(7): e00271-19

Related compound libraries

This product is contained In the following compound libraries:
Kinase Inhibitor Library Inhibitor Library Target-Focused Phenotypic Screening Library Metabolism Compound Library Bioactive Compound Library Autophagy Compound Library Apoptosis Compound Library ReFRAME Related Library Bioactive Compounds Library Max Glycometabolism Compound Library

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Keywords

PFK-015 4382-63-2 Autophagy Metabolism Glucokinase PFK-15 PFK15 3PO stomach cancer PFK 015 cancers inhibit PFK 15 PFKFB3 esophageal squamous cell carcinoma (ESCC) PFK015 lung cancer colon cancer Inhibitor inhibitor

 

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