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

A cell-permeable, potent and competitive inhibitor of fructose-2,6-bisphosphatase 3 (PFKFB3; IC₅₀ = 670 nM).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 7,8-Dihydroxy-3-(4-hydroxyphenyl)-4H-chromen-4-one, 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 Inhibitor, YN1

Primary Target: PFKFB3
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531050
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
75187-63-2C₁₅H₁₀O₅

Products

Catalog NumberPackaging Qty/Pack
5.31050.0001 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
Applications
Biological Information
Primary TargetPFKFB3
Primary Target IC<sub>50</sub>670 nM & Ki
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
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
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalog Number GTIN
5.31050.0001 04055977242522

Documentation

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

Title

Safety Data Sheet (SDS) 

References

Reference overview
Klarer, A. C., et al. 2014. Cancer Metab. 2, 2.
Seo, M., et al. 2011. PLoS ONE 6, e24179.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision31-July-2014 JSW
Synonyms7,8-Dihydroxy-3-(4-hydroxyphenyl)-4H-chromen-4-one, 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 Inhibitor, YN1
DescriptionA 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
FormOff-white powder
Intert gas (Yes/No) Packaged under inert gas
CAS number75187-63-2
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
+2°C to +8°C
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.
Toxicity Regulatory Review
ReferencesKlarer, A. C., et al. 2014. Cancer Metab. 2, 2.
Seo, M., et al. 2011. PLoS ONE 6, e24179.