FX11

A cell permeable, gossypol analog that acts as a selective, reversible, and NADH competitive inhibitor of lactate dehhydrogenase A (LDHA; K_i = 8 µM for human liver LDHA). Does not affect the activities of LDHB and glyceraldehyde-3-phosphate dehydrogenase even at higher concentrations. Shown to increase oxygen consumption, reactive oxygen species production, and cell death in P493 human lymphoma B cells. Also shown to reduce mitochondrial transmembrane potential and ATP levels and increase AMP kinase activity. Exhibits synergistic toxicity in P493 cells when combined with FK866 (Cat. No. 481908). Blocks the progression of human lymphoma and pancreatic cancer xenografts and when used in combination with FK866 it induces lymphoma regression.

Lactate Dehydrogenase A Inhibitor, FX11, CAS 213971-34-7, is a cell permeable, selective, reversible, NADH competitive inhibitor of lactate dehhydrogenase A (LDHA; Ki = 8 µM for human liver LDHA).

Cell permeable: yes

Primary Target
LDHA

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Le, A., et al. 2011. Proc Natl Acad Sci USA.107, 2037.
Deck, L. M., et al. 1998. J Med Chem.41, 3879.

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

Toxicity: Standard Handling (A)