5.33660
Lactate Dehydrogenase Inhibitor II, GSK2837808A
Synonym(s):
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
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25 MG
CA$190.00
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25 MG
CA$190.00
About This Item
Empirical Formula (Hill Notation):
C31H25F2N5O7S
Molecular Weight:
649.62
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
assay
≥95% (HPLC)
Quality Level
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
yellow
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
General description
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
lactate dehydrogenase A
lactate dehydrogenase A
Reversible: yes
Target IC50: 2.6 nM for human LDH-A
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Other Notes
Xie, H. 2014. Cell Metab.19, 795.
Billiard, J. 2013. Cancer Metab.1, 19.
Billiard, J. 2013. Cancer Metab.1, 19.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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