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Glutaminase inhibitor compound 968 (968) is an inhibitor of glutaminase C (GAC; IC50 = 9.3 µM).1 It was previously proposed that 968 contained a benzo[c]phenanthridine structure, but it was later shown that the correct structure contains the isomeric benzo[c]acridine.2,3 968 inhibits the proliferation and invasion of, and induces apoptosis in, MDA-MB-231 breast cancer cells at 10 µM.1,4 It also inhibits viral replication in Vero E6 cells infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) at 2.5 µM.5 In vivo, 968 reduces tumor volume in a P493 B cell lymphoma mouse xenograft model.2 This product has been verified to contain the benzo[c]acridine structure.
WARNING This product is not for human or veterinary use.
1. Dibenzophenanthridines as inhibitors of glutaminase C and cancer cell proliferation. Mol. Cancer Ther. 11(6), 1269-1278 (2012).
2. Targeting mitochondrial glutaminase activity inhibits oncogenic transformation. Cancer Cell 18(3), 2007-2219 (2010).
3. Structural reassignment of compund 968, an allosteric glutaminase inhibitor. Beilstein J. Org. Chem. 22, 455-460 (2026).
4. Modifying metabolically sensitive histone marks by inhibiting glutamine metabolism affects gene expression and alters cancer cell phenotype. Epigenetics 7(12), 1413-1420 (2012).
5. Glutamine metabolism is essential for coronavirus replication in host cells and in mice. The Journal of Biological Chemisty 301(1), 108063 (2025).