Table 2. Inhibition Profiles of Human Factor XIIIa (FXIIIa), Human α-Thrombin (α-Th), Human Factor Xa (FXa), and Papain by Iodoacetamide (IAA) and the NSGMs 13 and 14.a.
| Inhibitor | IC50 (μM) | HS | ΔY (%) |
|---|---|---|---|
| IAA (FXIIIa) | 2.9 ± 0.4b | 0.8 ± 0.2 | 105 ± 10 |
| 13 (FXIIIa) | 36.2 ± 4.5 | 0.9 ± 0.2 | 98 ± 11 |
| 14 (FXIIIa) | 118.0 ± 49.9 | 1.1 ± 0.5 | 93 ± 30 |
| 13 (α-Th) | >930 | NDc | ND |
| 13 (FXa) | 313.5 ± 119.6 | 0.9 ± 0.4 | 71 ± 22 |
| 13 (Papain) | >1000 | ND | ND |
a The IC50, HS, and ∆Y values were obtained following non-linear regression analysis of direct inhibition of FXIIIa, α-Th, FXa, or papain in appropriate TrisHCl buffers of pH 7.4–8.0 at 37°C containing appropriate concentrations of NaCl and CaCl2. See Materials and Methods for details.
b Errors represent ± 1 S.E.
c Not determined.