Merck, SML1327-25MG, Glutaminase Inhibitor 968

General description
Glutaminase Inhibitor 968 belongs to the benzophenanthridinone family.
Application
Glutaminase inhibitor 968 has been used to study the role of glutamine metabolism in macrophage activation.
Biochem/physiol Actions
Glutaminase Inhibitor 968 is an allosteric inihibitor of the mitochondrial enzyme glutaminase C (GAC), which is overexpressed in a number of cancer cell lines. Glutaminase Inhibitor 968 shows 21% inhibition at 10 μM, 94% at 25 μM. Glutaminase Inhibitor 968 blocked human cancer cell proliferation in culture, and in inhibited tumor formation in mouse xenograft models.
Glutaminase Inhibitor 968 is an allosteric inihibitor of the mitochondrial enzyme glutaminase C (GAC).
Variation in the 3-bromo-4-(dimethylamino)phenyl ring of glutaminase inhibitor 968, leads to loss of its inhibitory activity. Glutaminase catalysed glutamine metabolism maintains intracellular pH of cancer cells. Inhibition by glutaminase inhibitor 968 is known to hinder cell proliferation as a consequences of low intracellular pH.