Sigma-Aldrich Lactate Dehydrogenase Inhi

Assay

≥95% (HPLC)

Quality Level

100

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: yesPrimary Target
lactate dehydrogenase AReversible: yesTarget 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.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany