PEPCK Inhibitor

SKF-34288 (3-Mercaptopicolinic acid) hydrochloride is an orally active phosphoenolpyruvate carboxykinase (PEPCK) inhibitor (K_i: 2-9 μM). SKF-34288 hydrochloride is a potent hypoglycemic agent by inhibiting glucose synthesis. SKF-34288 hydrochloride also inhibits Asn metabolism and increases amino acids and amides.

Hydrazine sulfate is an orally active PEPCK inhibitor. Hydrazine sulfate inhibits PEPCK and low-K_m ALDH. Hydrazine sulfate impairs gluconeogenesis and enhances the protective effect of energy substrates against MPP⁺ toxicity. Hydrazine sulfate exacerbates liver damage in rats when combined with Ethanol. Hydrazine sulfate can be used in the research of shock, non-small cell lung cancer, colorectal cancer and Parkinson's disease.

Demethoxycapillarisin (6-Demethoxycapillarisin) inhibits PEPCK mRNA levels (IC₅₀: 43 μM) by activation of the PI3K pathway. Demethoxycapillarisin decreases glucose production.

7-Methoxyrosmanol (7-O-Methoxyrosmanol), a phenolic diterpene isolated from rosemary, suppresses the cAMP responsiveness of PEPCK and G6Pase promoters.

Pterosin A ((2S)-Pterosin A) is a sesquiterpene compound. Pterosin A is an orally active AMPK activator with anti-diabetic effect. Pterosin A can promote glucose uptake, increase serum insulin, and improve hyperglycemia and glucose intolerance. Pterosin A can prevent insulin-secreting cells death and reduce ROS production. Pterosin A can be used for the research of metabolic disease, such as diabetes.

cis-THSG is a selective and orally active DNA topoisomerase II inhibitor with no activity against DNA topoisomerase I. cis-THSG suppresses transcription of PEPCK. cis-THSG reduces blood glucose levels, ameliorates glucose intolerance, and alleviates insulin resistance in high fat diet-induced diabetic male CF-1 mice. cis-THSG can be used for the research of type 2 diabetes mellitus.