A cell-permeable pyrrolyl-hydroxybenzoate compound that inhibits fructose-1,6-bisphosphate- (FBP-) dependent activation of pyruvate kinases PKM2 and PKL (IC50 10 to 50 µM), while exhibiting reduced potency against non-FBP-dependent PKM1 activity (81% inhibition of PKM2 vs. 34% inhibition of PKM1 at 30 µM). Lysates from inhibitor-treated (250 µM inhibitor treatment for 6 h) human lung cancer H1299 cells are shown to exhibit significantly reduced PKM2 activity (by 84%) even upon exogenous FBP addition. Inhibitor treatment (Effective conc. 50 to 100 µM) is also demonstrated to enhance cell death of IL-3-dependent murine pro-B lymphocytic FL5.12 and EGFR-signaling-dependent human lung adenocarcinoma HCC827 cultures upon IL-3 withdrawal and EGFR inhibitor treatment, respectively.
A cell-permeable pyrrolyl-hydroxybenzoate compound that inhibits fructose-1,6-bisphosphate- (FBP-) dependent activation of pyruvate kinases PKM2 and PKL (IC50 10 to 50 µM), while exhibiting reduced potency against non-FBP-dependent PKM1 activity (81% inhibition of PKM2 vs. 34% inhibition of PKM1 at 30 µM). Lysates from inhibitor-treated (250 µM inhibitor treatment for 6 h) human lung cancer H1299 cells are shown to exhibit significantly reduced PKM2 activity (by 84%) even upon exogenous FBP addition. Inhibitor treatment (Effective conc. 50 to 100 µM) is also demonstrated to enhance cell death of IL-3-dependent murine pro-B lymphocytic FL5.12 and EGFR-signaling-dependent human lung adenocarcinoma HCC827 cultures upon IL-3 withdrawal and EGFR inhibitor treatment, respectively.
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Biochem/physiol Actions
Cell permeable: yes
Primary Target pyruvate kinases
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 weeks at -20°C.
Other Notes
Vander Heiden, M.G., et al. 2010. Biochem. Pharmacol.79, 1118.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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