Glutaminase C-IN-1

Glutaminase C-IN-1 (Compound 968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts In Vitro Glutaminase C-IN-1 (Compound 968) (10 μM; 14 d) inhibits cellular transformation in NIH 3T3 cells. ? Glutaminase C-IN-1 (10 μM; 6 d) blocks the signaling activity of a specific target of Dbl. ? Glutaminase C-IN-1 blocks the transforming activity of human breast cancer cells. ? Glutaminase C-IN-1 (10 μM) blocks glutaminolysis in transformed cells. ? Glutaminase C-IN-1 preferentially binds to the monomeric state of Glutaminase C. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: MDA-MB231 cells, SKBR3 cells, and NIH 3T3 cells Concentration: 10 μM Incubation Time: 5 h Result: Inhibited cell growth. In Vivo Glutaminase C-IN-1 (Compound 968) (200 μg/mouse; i.p.; daily for 12 days) reduces tumor volume in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SCID mice with P493 B lymphoma cells Dosage: 200 μg/mouse Administration: Intraperitoneal injection, daily for 12 days Result: Caused a ~50% reduction in the size of the tumors. IC50& Target:Glutaminase C

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