LDHB Inhibitor

(R)-GNE-140 is a potent inhibitor of lactate dehydrogenase (LDH) A, B and C, with IC₅₀ values of 3, 5 and 5 nM against LDHA, LDHB, LDHC, respectively. (R)-GNE-140 blocks the conversion of pyruvate to lactate, reduces lactate production and histone lysine lactylation, and inhibits glycolysis. (R)-GNE-140 attenuates cardiac hypertrophy, alleviates PM_2.5-induced pulmonary inflammation and fibrosis, blocks MRSA-induced Arg1 expression. (R)-GNE-140 is applicable to research related to pathological cardiac hypertrophy, pulmonary fibrosis, MRSA infection and pancreatic cancer.

AXKO-0046, indole derivative, is an uncompetitive Lactate dehydrogenase B (LDHB) selective inhibitor.AXKO-0046 has LDHB inhibitory activity with an EC₅₀ value of 42 nM.AXKO-0046 can be used for the research of cancer metabolism.

GNE-140 racemate is a racemic mixture of (R)-GNE-140 (HY-100742A) and (S)-GNE-140 (HY-100742B), and also a tautomer of GNE-140 (HY-118241). GNE-140 racemate is an orally active lactate dehydrogenase inhibitor, with an IC₅₀ of 3 nM against human LDHA and an IC₅₀ of 5 nM against LDHB. GNE-140 racemate reduces the phosphorylation level and total protein expression of p38 MAPK, and inhibits EGF-induced AKT phosphorylation. GNE-140 racemate decreases lactate production, regulates glycolysis, the pentose phosphate pathway and nucleotide biosynthesis, increases extracellular pH, inhibits cell proliferation, migration and invasion, and induces caspase-3 activation and ROS accumulation. GNE-140 racemate can be used in research related to breast cancer, cystic fibrosis and pancreatic cancer.

(S)-GNE-140 (Compound 30-S) is the S-enantiomer of GNE-140 (HY-118241). (S)-GNE-140 is an effective lactate dehydrogenase (LDH) inhibitor, with IC₅₀ values of 55 nM for LDHA and 140 nM for LDHB. (S)-GNE-140 can be used in cancer research.

GNE-140 (Compound 28) is an external racemic mixture of (R)-GNE-140 (HY-100742A) and (S)-GNE-140 (HY-100742B). GNE-140 is an effective lactate dehydrogenase (LDH) inhibitor, with the IC₅₀ values for LDHA and LDHB being 9 nM and 30 nM respectively. GNE-140 can be used in cancer research.

NCATS-SM1440 is a glycolysis inhibitor and metabolic regulator that targets LDHA and LDHB (IC₅₀=0.06 μM and 0.03 μM, respectively). Upon binding to LDHA, NCATS-SM1440 blocks the glycolysis pathway and reduces lactate production. NCATS-SM1440 drives the shift of pyruvate metabolism toward mitochondrial metabolism, effectively disrupting the dependence of cancer cells on aerobic glycolysis. NCATS-SM1440 can be widely used in research related to cancer, Ewing's sarcoma, and other related conditions.

LDH-IN-4 is a LDHA and LDHB inhibitor, as well as a ligand for target protein for PROTACs. LDH-IN-4 can be used to synthesize proteolysis-targeting chimeras (PROTAC), such as MS6105 (HY-152261). LDH-IN-4 is applicable to pancreatic cancer-related research.

GNE-140 racemate (Standard) is the analytical standard of GNE-140 racemate (HY-100742). This product is intended for research and analytical applications. GNE-140 racemate is a racemic mixture of (R)-GNE-140 (HY-100742A) and (S)-GNE-140 (HY-100742B), and also a tautomer of GNE-140 (HY-118241). GNE-140 racemate is an orally active lactate dehydrogenase inhibitor, with an IC₅₀ of 3 nM against human LDHA and an IC₅₀ of 5 nM against LDHB. GNE-140 racemate reduces the phosphorylation level and total protein expression of p38 MAPK, and inhibits EGF-induced AKT phosphorylation. GNE-140 racemate decreases lactate production, regulates glycolysis, the pentose phosphate pathway and nucleotide biosynthesis, increases extracellular pH, inhibits cell proliferation, migration and invasion, and induces caspase-3 activation and ROS accumulation. GNE-140 racemate can be used in research related to breast cancer, cystic fibrosis and pancreatic cancer.