Table 1.
compds tested | glutamine conc | phosphate conc | enzyme | preincubation time | detection method | IC50 (μM) for BPTES |
additional in vitro assays conducted | ref(s) |
---|---|---|---|---|---|---|---|---|
RPTES, 4-7 | 7 mM | 160 mM | hKGA1_669 | 20 min | GDH; formazan formation measured by absorbance at 570 nm | 0.19; 0.58 | 28 | |
8-10; 28; 29 | 2 mM | 45 mM | hKGA124-669 | 0 min | [3H]-glutamate | 3.3 | P493 proliferation | 22; 41 |
CB-839, 11-25; 30; 31 | 10 mM | 150 mM | GAC | 0 or 60 min | GDH; NADH formation measured by absorbance at 340 nm | 0.1 (60 min) 0.2 (0 min) | P493/MDA-MB-231 /HCC1806 proliferation | 44 |
26; 27; 52-67 | 13 mM or 1.8 mM | 100 mM | GAC | 60 min | GDH-diaphorase; resorufin formation measured at ex544/em590 nm | 0.1-0.5 | 45; 50-52 | |
32-36; 68; 101-104 | 10 mM | unknown | mouse brain/kidney homogenate | 0 min | ammonia formation detected by Nessler s reagent by absorbance at 450 nm | not tested | MDA-MB-231 proliferation | 46; 56 |
69-72 | no biochemical GLS assay data reported | BT20 cellular glutaminase | 53 | |||||
37-51; 105-106 | 1 mM | 50 mM | GAC | 10 min | GLOD-horseradish peroxidase; resorufin formation measured at ex530/em590 nm | not tested | A549 proliferation | 47—49; 57 |
73-87 | 50 mM | 100 mM | hKGA63_669 | 15 min | GLOD-horseradish peroxidase; resorufin formation measured at ex535/em590 nm | not tested | PC3 cellular glutaminase; NCI-H1703 proliferation | 23-27 |
88-100 | 18 mM | 135 mM | GAC | unknown | GDH; NADH formation measured by absorbance at 340 nm | 0.4 | MDA-MB-231 proliferation | 54 |