CB-839 是一种有效的，选择性的，口服生物可利用的 glutaminase 抑制剂，对重组人GAC的 IC50 为 24 nM。Phase 1。
Combination treatment with a GLS1 inhibitor and PP242 induces cell death. a The SKOV3 and A2780 cells were incubated with DMSO (control), PP242 (1 μM), CB839 (1 μM), or their combination for 48 h. Cell morphology images were obtained under a microscope. b. Expression of the activated cleaved PARP content to GAPDH was observed using Western blot. c. Cell death was evaluated by flow cytometry after Annexin V and PI staining. Data are presented as means of triplicate samples, and error bars reflect SD.
BPTES是一种有效的选择性Glutaminase GLS1 (KGA)抑制剂，其IC50为0.16 μM。它对谷氨酸脱氢酶的活性没有影响，对γ谷氨酰转肽酶的活性只有很微弱的抑制作用。