5.33660

Lactate Dehydrogenase Inhibitor II, GSK2837808A

• Sinonimo/i: Lactate Dehydrogenase Inhibitor II, GSK2837808A, 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
• Formula empirica (notazione di Hill): C₃₁H₂₅F₂N₅O₇S
• Peso molecolare: 649.62
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Saggio: ≥95% (HPLC)
• Livello qualitativo: 100
• Stato: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: yellow
• Solubilità: DMSO: 50 mg/mL
• Temperatura di conservazione: 2-8°C

Descrizione

Descrizione generale

A 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.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
lactate dehydrogenase A

Reversible: yes

Target IC₅₀: 2.6 nM for human LDH-A

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Altre note

Xie, H. 2014. Cell Metab.19, 795.

Billiard, J. 2013. Cancer Metab.1, 19.

Note legali

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable