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. 2020 Nov 5;477(21):4149–4165. doi: 10.1042/BCJ20200592

Table 1. Effect of BI01383298 on the uptake function of different transporters in HepG2 cells monitored with appropriate substrates and experimental conditions.

Substrate Control BI01383298 % Control
Citrate (7 µM) 483 ± 13 88.2 ± 5.6 18 ± 1**
Nicotinate (8 µM) 124 ± 3 123 ± 4 100 ± 3
Arginine (5 µM) 928 ± 31 935 ± 51 101 ± 5
Glutamine (5 µM) 319 ± 25 306 ± 3 92 ± 1
Tryptophan (5 µM) 80 ± 2 76 ± 3 95 ± 3
Lactate (3 µM) 141 ± 14 137 ± 7 97 ± 5

HepG2 cells were preincubated in NaCl buffer with or without 10 μM BI01383298 for 30 min. After washing the cells, uptakes of [14C]-citrate, [14C]-nicotinate, [3H]-arginine, [3H]-glutamine, [3H]-tryptophan, and [14C]-lactate were measured for a given time (which varied for different transporters) in NaCl buffer pH 7.5 (citrate, nicotinate, arginine), NMDG buffer pH 7.5 (glutamine, tryptophan) or NMDG pH 6 (lactate). The units for the uptake activity were pmol/mg of protein/30 min for citrate, pmol/mg of protein/15 min for nicotinate, arginine, glutamine, and tryptophan, and pmol/mg of protein/3 min for lactate. Data represent means ± S.D. ** P < 0.01 compared with the corresponding control uptake.