Table 1. Inhibition of PTPs by Fumos in vitro.
PTP | IC50 (μM) | IC50 selective |
---|---|---|
Shp2 | 6.31 ± 0.52 | 1 |
PTP1B | 14.04 ± 0.60 | 2 |
TCPTP | 29.65 ± 0.42 | 5 |
SHP1 | 34.70 ± 0.37 | 6 |
HePTP | >100 | >16 |
Lyp | >100 | >16 |
STEP | >100 | >16 |
PTPH1 | >100 | >16 |
PTPRA | >100 | >16 |
Cdc25b | >100 | >16 |
Meg2 | >100 | >16 |
Shp2 FL | 26.52 ± 0.37 | 4 |
Shp2 Y279A | – | – |
Each experiment was performed in triplicate. Data are presented as mean ± S.E.M. All PTP proteins contain only PTP domain except full lenth Shp2 (Shp2 FL) and Shp2 Y279A. Shp2 Y279A shows no enzyme activity. Na3VO4 potently inhibited Shp2 PTP domain and Shp2 FL with an IC50 of 620 μM and 630 μM, respectively.