Table 1. Selectivity Profile of mPTPA Inhibitor 2 against a Panel of Human PTPs, mPTPB, and a Cysteine Protease.
enzyme class | enzyme | IC50 (μM)a | selectivity |
---|---|---|---|
phosphatases | mPTPA | 0.53 ± 0.10 | |
mPTPB | >100 | >100 | |
STEP | 6.2 ± 2.9 | 12 | |
LMW-PTP | 43 ± 11 | 81 | |
PTP1B | 50 ± 20 | 94 | |
CD45 | >100 | >100 | |
LAR | >100 | >100 | |
TC-PTP | >100 | >100 | |
cysteine protease | cathepsin B | >100 | >100 |
IC50 values were determined in the presence of a physiological intracellular concentration of GSH (1 mM).