Glutaminase

Inhibitory Selectivity
Solubility

Catalog No.	Product Name	Solubility(25°C)
Catalog No.	Product Name	Water	DMSO	Alcohol
S7655	CB-839	<1 mg/mL	100 mg/mL	<1 mg/mL
S7753	BPTES	<1 mg/mL	100 mg/mL	<1 mg/mL

Glutaminase Inhibitors (2)

Catalog No.	Information	Product Use Citations	Product Validations
S7655	CB-839 CB-839 is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. Phase 1.	Br J Cancer, 2018, 118(8):1074-1083 Biochem Pharmacol, 2018, 156:204-214 Tumour Biol, 2016, 37(8):11007-15	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.
S7753	BPTES BPTES is a potent and selective Glutaminase GLS1 (KGA) inhibitor with IC50 of 0.16 μM. It has no effect on glutamate dehydrogenase activity and causes only a very slight inhibition of γ-glutamyl transpeptidase activity.		Glu-dependent associates with sensitivity to glycolytic inhibitors 3-BrPA (left) and GLN-addicted associates with sensitivity to glutaminolytic inhibitors BPTEs.

Catalog No.

Information

Product Use Citations

Product Validations

S7655

CB-839

CB-839 is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. Phase 1.

Br J Cancer, 2018, 118(8):1074-1083

Biochem Pharmacol, 2018, 156:204-214

Tumour Biol, 2016, 37(8):11007-15

S7753

BPTES is a potent and selective Glutaminase GLS1 (KGA) inhibitor with IC50 of 0.16 μM. It has no effect on glutamate dehydrogenase activity and causes only a very slight inhibition of γ-glutamyl transpeptidase activity.