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Table 2 Potency of CB-1158 on arginase activity in intact cells

From: Inhibition of arginase by CB-1158 blocks myeloid cell-mediated immune suppression in the tumor microenvironment

Intact cell assay

CB-1158, IC50 (μM)

Human HepG2 cell line

32 (±5.6)

Human K562 cell line

139 (±8.8)

Primary Human Hepatocytes

210

  1. 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