PFKFB3 Inhibitor III, YN1-CAS 75187-63-2-Calbiochem

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一般描述

A cell-permeable isoflavone compound that acts as a potent and competitive inhibitor of fructose-2,6-bisphosphatase 3 (PFKFB3; IC₅₀= 670 nM; K_i= 240 nM). Directly docks into the Fru-6-P binding pocket of PFKFB3 and down-regulates Fru-2,6-BP levels (40% decrease in 48 h in HeLa cells) resulting in reduced glycolysis and lactate production. Shown to diminish the proliferation of HCT-116 human adenocarcinoma cells (GI₅₀= 8.2 ?M) and inhibit HeLa cells colony formation on soft agar (~79% reduction at 25 ?M). Induces apoptotic (~25 ?M) and necrotic (~50 ?M) cell death depending on the level of ATP depletion. Also reported to increase autophagy in HCT-116 cells as evidenced by an increase in LC3-II levels and a decrease in p62 levels
A cell-permeable isoflavone compound that acts as a potent and competitive inhibitor of fructose-2,6-bisphosphatase 3 (PFKFB3; IC₅₀= 670 nM; K_i= 240 nM). Directly docks into the Fru-6-P binding pocket of PFKFB3 and down-regulates Fru-2,6-BP levels (40% decrease in 48 h in HeLa cells) resulting in reduced glycolysis and lactate production. Shown to diminish the proliferation of HCT-116 human adenocarcinoma cells (GI₅₀= 8.2 ?M) and inhibit HeLa cells colony formation on soft agar (~79% reduction at 25 ?M). Induces apoptotic (~25 ?M) and necrotic (~50 ?M) cell death depending on the level of ATP depletion. Also reported to increase autophagy in HCT-116 cells as evidenced by an increase in LC3-II levels and a decrease in p62 levels.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

生化/生理作用

Cell permeable: yes
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Regulatory Review (Z)

其他说明

Klarer, A. C., et al. 2014.Cancer Metab.2,2.
Seo, M., et al. 2011.PLoS ONE6,e24179.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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