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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.

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: 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
533660
Purchase on Sigma-Aldrich

Aperçu

Replacement Information

Tableau de caractéristiques principal

Empirical Formula
C₃₁H₂₅F₂N₅O₇S

Products

RéférenceConditionnement Qté
5336600001 Flacon en verre 5 mg
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
Référence GTIN
5336600001 04055977286601

Documentation

Lactate Dehydrogenase Inhibitor II, GSK2837808A FDS

Titre

Fiche de données de sécurité des matériaux (FDS) 

Références bibliographiques

Aperçu de la référence bibliographique
Xie, H. 2014. Cell Metab. 19, 795.
Billiard, J. 2013. Cancer Metab. 1, 19.
Fiche technique

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.