Potency of CB-1158 on arginase activity in intact cells

Intact cell assayCB-1158, IC50 (μM)
Human HepG2 cell line32 (±5.6)
Human K562 cell line139 (±8.8)
Primary Human Hepatocytes210

Mean IC50 values in micromolar for CB-1158 inhibition of arginase activity in intact cells. Standard deviations are indicated in parentheses. HepG2 (N = 3) and K562 (N = 2) cell lines were plated in duplicate wells in the presence of 10 mM L-arginine. For primary human hepatocytes (N = 1), arginase activity was measured in duplicate wells in the presence of media containing 10 mM L-ornithine and lacking L-arginine. Arginase activity was measured as production of urea in the media after 24 h