disodium-r-2-hydroxyglutarate

Description: Disodium (R)-2-Hydroxyglutarate (also known as D-2-HGA, or 2-HG) is a potent and competitive inhibitor of alpha-ketoglutarate (alpha-KG)-dependent dioxygenases with Ki value of 0.628 mM. In U-87MG cells, (R)-2-Hydroxyglutarate acts as weak antagonists of alpha-KG to inhibit alpha-KG-dependent histone demethylases and increases dimethylation on both H3K9 and H3K79. Besides, (R)-2-Hydroxyglutarate also inhibits ATP synthase and mTOR signaling, and therefore causes growth arrest and tumor cell killing. Inhibition of ATP synthase by 2-HG or alpha-KG in glioblastoma cells is sufficient for growth arrest and tumor cell killing under conditions of glucose limitation, e.g., when ketone bodies (instead of glucose) are supplied for energy. These findings inform therapeutic strategies and open avenues for investigating the roles of 2-HG and metabolites in biology and disease.

References: Cancer Cell. 2011 Jan 18; 19(1):17-30; Cell Metab. 2015 Sep 1; 22(3):508-15.

D-alpha-Hydroxyglutaric acid disodium salt; Disodium (R)-2-hydroxyglutarate; D-2-HGA; 2R-hydroxy-pentanedioic acid, disodium salt

Chemical Name: 2R-hydroxy-pentanedioic acid, disodium salt