A selective inhibitor of PFKFB3 (IC50 = 207 nM); rapidly induces apoptosis in transformed cells

PFK15 – 5 mg

Brand:
Cayman
CAS:
4382-63-2
Storage:
-20
UN-No:
Non-Hazardous - /

6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) is a bifunctional enzyme that contains distinct domains for the phosphorylation of fructose 6-phosphate and the dephosphorylation of fructose 2,6-bisphosphate. PFKFB3 protein expression is elevated in most tumor types.{30751,27006} PFK15 is a selective inhibitor of PFKFB3 (IC50 = 207 nM).{30752} It has no significant inhibitory effect on any member of a panel of 96 other kinases, and does not inhibit purified 6-phosphofructo-1-kinase, hexokinase, phosphoglucose isomerase, or PFKFB4. PFK15 rapidly induces apoptosis in transformed cells, suppresses glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and yields antitumor effects in human xenograft models of cancer in athymic mice.{30752}  

 

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Description

A selective inhibitor of PFKFB3 (IC50 = 207 nM); rapidly induces apoptosis in transformed cells, suppresses glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and yields antitumor effects in human xenograft models of cancer in athymic mice

Formal name: 1-(4-pyridinyl)-3-(2-quinolinyl)-2-propen-1-one

Synonyms: 

Molecular weight: 260.3

CAS: 4382-63-2

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Phosphatases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling||Research Area|Cancer|Metabolism

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