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Lactate Dehydrogenase Inhibitor II, GSK2837808A

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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
Empirical Formula (Hill Notation):
C31H25F2N5O7S
Molecular Weight:
649.62

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

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vibrant-m

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HMTase Inhibitor IV, UNC0638

form

solid

form

solid

form

solid

form

powder

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

color

yellow

color

brown

color

off-white

color

off-white

solubility

DMSO: 50 mg/mL

solubility

DMSO: 50 mg/mL

solubility

DMSO: 50 mg/mL

solubility

DMSO: 10 mg/mL

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°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
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.

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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