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48-602MAG
Buffer Detection Kit for Magnetic Beads
1 Kit
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531050
Sigma-AldrichPFKFB3 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).
More>>A cell-permeable, potent and competitive inhibitor of fructose-2,6-bisphosphatase 3 (PFKFB3; IC₅₀ = 670 nM). Less<<
MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
A 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.
Klarer, A. C., et al. 2014. Cancer Metab.2, 2. Seo, M., et al. 2011. PLoS ONE6, 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.
A 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
Form
Off-white powder
Intert gas (Yes/No)
Packaged under inert gas
CAS number
75187-63-2
Purity
≥98% by HPLC
Solubility
DMSO (100 mg/ml)
Storage
Protect from light +2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity
Regulatory Review
References
Klarer, A. C., et al. 2014. Cancer Metab.2, 2. Seo, M., et al. 2011. PLoS ONE6, e24179.