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533660 Lactate Dehydrogenase Inhibitor II, GSK2837808A

A cell-permeable, NADH-competitive LDHA selective inhibitor (IC₅₀ = 2.6 & 43 nM for LDHA & LDHB). Blocks cytosolic glycolysis, activates PKM2 and induces apoptosis.

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Synonyme: LDH Inhibitor II, Compound 1, 3-((3-(N-Cyclopropylsulfamoyl)-7-(2,4-dimethoxypyrimidin-5-yl)quinolin-4-yl)amino)-5-(3,5-difluorophenoxy)benzoic acid

Primary Target: lactate dehydrogenase A
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533660
Preis & Verfügbarkeit

Übersicht

Replacement Information

Key Spec Table

Empirical Formula
C₃₁H₂₅F₂N₅O₇S

Preis & Verfügbarkeit

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      Description
      OverviewA cell-permeable quinolinesulfonamide compound that acts as potent and reversible inhibitor of lactate dehydrogenase A (IC50 = 2.6 nM for human LDH-A). The inhibition appears to be competitive with respect to NADH and non-competitive with respect to pyruvate. Exhibits high selectivity over LDH-B (IC50 = 43 nM) and does not affect the activity of 32 other enzymes, receptors, and ion-channels even at high concentration (~ 10 µM). Rapidly reduces lactate production in hepatocellular (EC50 = 400 and 588 nM in Snu398 and HepG2 cells, respectively) and breast carcinoma cell lines, and induces PKM2 activation (EC50 = 600 nM in Snu398 cells). Shown to increase mitochondrial oxygen consumption rate (EC50 = 500 and 900 nM in Snu398 and HepG2 cells, respectively) and causes a diminution in extracellular acidification rates (EC50 = 600 nM in both cell lines). Shown to downregulate the ability of A549 cells to form tumorspheres and diminishes the number of CD24/CD44-positive cells in HMLER system and in stem cells isolated from HMLER. Blocks the proliferation of Snu398 cells and induces apoptosis within 24 h of incubation.
      Catalogue Number533660
      Brand Family Calbiochem®
      SynonymsLDH Inhibitor II, Compound 1, 3-((3-(N-Cyclopropylsulfamoyl)-7-(2,4-dimethoxypyrimidin-5-yl)quinolin-4-yl)amino)-5-(3,5-difluorophenoxy)benzoic acid
      References
      ReferencesXie, H. 2014. Cell Metab. 19, 795.
      Billiard, J. 2013. Cancer Metab. 1, 19.
      Product Information
      FormYellow solid
      Hill FormulaC₃₁H₂₅F₂N₅O₇S
      Chemical formulaC₃₁H₂₅F₂N₅O₇S
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Targetlactate dehydrogenase A
      Primary Target IC<sub>50</sub>2.6 nM for human LDH-A
      Purity≥95% 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 Standard Handling
      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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Bestellnummer GTIN
      5.33660.0001 04055977286601

      Documentation

      Lactate Dehydrogenase Inhibitor II, GSK2837808A SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Xie, H. 2014. Cell Metab. 19, 795.
      Billiard, J. 2013. Cancer Metab. 1, 19.
      Datenblatt

      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.

      Revision23-July-2016 JSW
      SynonymsLDH Inhibitor II, Compound 1, 3-((3-(N-Cyclopropylsulfamoyl)-7-(2,4-dimethoxypyrimidin-5-yl)quinolin-4-yl)amino)-5-(3,5-difluorophenoxy)benzoic acid
      DescriptionA cell-permeable quinolinesulfonamide compound that acts as potent and reversible inhibitor of lactate dehydrogenase A (IC50 = 2.6 nM for human LDH-A). The inhibition appears to be competitive with respect to NADH and non-competitive with respect to pyruvate. Exhibits high selectivity over LDH-B (IC50 = 43 nM) and does not affect the activity of 32 other enzymes, receptors, and ion-channels even at high concentration (~ 10 µM). Rapidly reduces lactate production in hepatocellular (EC50 = 400 and 588 nM in Snu398 and HepG2 cells, respectively) and breast carcinoma cell lines, and induces PKM2 activation (EC50 = 600 nM in Snu398 cells). Shown to increase mitochondrial oxygen consumption rate (EC50 = 500 and 900 nM in Snu398 and HepG2 cells, respectively) and causes a diminution in extracellular acidification rates (EC50 = 600 nM in both cell lines). Shown to downregulate the ability of A549 cells to form tumorspheres and diminishes the number of CD24/CD44-positive cells in HMLER system and in stem cells isolated from HMLER. Blocks the proliferation of Snu398 cells and induces apoptosis within 24 h of incubation.
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₃₁H₂₅F₂N₅O₇S
      Purity≥95% by HPLC
      SolubilityDMSO (50 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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesXie, H. 2014. Cell Metab. 19, 795.
      Billiard, J. 2013. Cancer Metab. 1, 19.