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531050 PFKFB3 Inhibitor III, YN1 - CAS 75187-63-2 - Calbiochem

531050
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Overview

Key Spec Table

CAS #Empirical Formula
75187-63-2C₁₅H₁₀O₅

Products

Catalogue NumberPackaging Qty/Pack
5310500001 Glass bottle 25 mg
Description
OverviewA cell-permeable isoflavone compound that acts as a potent and competitive inhibitor of fructose-2,6-bisphosphatase 3 (PFKFB3; IC50 = 670 nM; Ki = 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 µM) and inhibit HeLa cells colony formation on soft agar (~79% reduction at 25 µM). Induces apoptotic (~25 µM) and necrotic (~50 µM) 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.
Catalogue Number531050
Brand Family Calbiochem®
Synonyms7,8-Dihydroxy-3-(4-hydroxyphenyl)-4H-chromen-4-one, 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 Inhibitor, YN1
References
ReferencesKlarer, A. C., et al. 2014. Cancer Metab. 2, 2.
Seo, M., et al. 2011. PLoS ONE 6, e24179.
Product Information
CAS number75187-63-2
FormOff-white powder
Hill FormulaC₁₅H₁₀O₅
ReversibleY
Quality LevelMQ100
Biological Information
Primary TargetPFKFB3
Primary Target IC<sub>50</sub>670 nM & Ki
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Regulatory Review
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Global Trade Item Number
Catalogue Number GTIN
5310500001 04055977242522