LDHA 选择性抑制剂

Sodium oxamate

Sodium oxamate (SO, Aminooxoacetic acid, Oxamic acid) is an inhibitor of lactate dehydrogenase (LDH) that specificly inhibits LDH‑A. Sodium oxamate (SO) induces G2/M cell cycle arrest via downregulation of the CDK1/cyclin B1 pathway and promotes apoptosis through enhancement of mitochondrial ROS generation.

GSK 2837808A

GSK2837808A is a selective LDHA (lactate dehydrogenase A) inhibitor with IC50 of 2.6 nM and 43 nM for hLDHA and hLDHB, respectively.

AZ-33

AZ-33 (LDHA Inhibitor 33) is a potent inhibitor of lactate dehydrogenase A (LDHA) with IC50 of 0.5 μM. LDHA is the key enzyme involved in anaerobic glycolysis which is frequently deregulated in human malignancies.

FX11

FX-11(LDHA Inhibitor FX11) is a potent inhibitor of lactate dehydrogenase A (LDHA)) with IC50 of 49.27 μM in BxPc-3 cells.

(R)-GNE-140

(R)-GNE-140 is a selective inhibitor of the LDHA and LDHB with IC50s of 3 nM and 5 nM, respectively. The R enantiomer of GNE-140 is 18-fold more potent than S enantiomer.

Galloflavin

Galloflavin (NSC 107022) is a novel inhibitor of lactate dehydrogenasee (LDH) with Ki values of 5.46 μM and 15.06 μM for LDH-A and LDH-B, respectively.