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FX11 is an inhibitor of lactate dehydrogenase-A (LDH-A; Ki = 8 µM).1 It is selective for LDH-A over GAPDH (Ki = >300 µM). FX11 increases oxygen consumption and the production of reactive oxygen species (ROS), as well as induces cell death in P493-6 lymphoblastoid cells. In vivo, FX11 (42 µg/animal, i.p.) reduces tumor volume in a P493-6 mouse xenograft model. It also reduces tumor weight in a BxPC-3 mouse xenograft model when administered at a dose of 2 mg/kg.2
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1. Inhibition of lactate dehydrogenase A induces oxidative stress and inhibits tumor progression. Proc. Nat. Acad. Sci. USA 107(5), 2037-2047 (2009).
2. Targeting pyruvate kinase M2 and lactate dehydrogenase A is an effective combination strategy for the treatment of pancreatic cancer. Cancers (Basel) 11(9), 1372 (2019).