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

531050
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₅H₁₀O₅ 75187-63-2

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      5.31050.0001
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          Glass bottle 25 mg
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          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
          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

          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 +2°C to +8°C
          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.
          Toxicity Regulatory Review
          ReferencesKlarer, A. C., et al. 2014. Cancer Metab. 2, 2.
          Seo, M., et al. 2011. PLoS ONE 6, e24179.