PFKFB3 Inhibitor II, PFK15-Calbiochem

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一般描述

A cell-permeable, bioavailable and more potent quinolinyl analog of PFKFB3 Inhibitor, 3PO (Cat. No. 525330) that inhibits the activity of 6-Phosphofructo-2-kinase (PFKFB3) by reversibly docking to its substrate binding domain (IC₅₀= 207 nM compared to 22.9 ?M for 3PO). Shown to effectively reduce fructose 2,6-bisphosphate, glucose uptake, and intracellular ATP levels. Does neither affect the activity of 96 other kinases in any significant manner (at ~10 ?M) nor PFK-1, hexokinase, phosphoglucoisomerase, or PFKFB4 even at 100 ?M. Induces apoptosis and reduces proliferation in transformed cells (mean GI₅₀of ~3 ?M in the NCI-60 cancer cell panel). Displays adequate pharmacokinetic properties to suppress glucose uptake and the growth of Lewis lung carcinoma is syngenic mice and block the growth of human tumor xenografts in athymic mice (~25 mg/kg, i.p. administered every 3rd day).
A cell-permeable, bioavailable and more potent quinolinyl analog of PFKFB3 Inhibitor, 3PO (Cat. No. 525330) that inhibits the activity of 6-Phosphofructo-2-kinase (PFKFB3) by reversibly docking to its substrate binding domain (IC ₅₀= 207 nM compared to 22.9 ?M for 3PO). Shown to effectively reduce fructose 2,6-bisphosphate, glucose uptake, and intracellular ATP levels. Does neither affect the activity of 96 other kinases in any significant manner (at ~10 ?M) nor PFK-1, hexokinase, phosphoglucoisomerase, or PFKFB4 even at 100 ?M. Induces apoptosis and reduces proliferation in transformed cells (mean GI ₅₀of ~3 ?M in the NCI-60 cancer cell panel). Displays adequate pharmacokinetic properties to suppress glucose uptake and the growth of Lewis lung carcinoma is syngenic mice and block the growth of human tumor xenografts in athymic mice (~25 mg/kg, i.p. administered every 3rd day).

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
Primary Target
PFKFB3
Reversible: yes
Target IC₅₀: 207 nM for hrPFKFP3

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
Use only fresh DMSO for reconstitution.

其他说明

Clem, B. F., et al. 2013.Mol. Cancer Ther.12,1461.

法律信息

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

基本信息

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