Inhibition of c3A4- and MkLM-mediated MDZ 1′-hydroxylation by KTZ and TAO
Incubation conditions were as follows: substrate: MDZ (5 µM), protein concentration: 10 nM for c3A4 and 0.5 mg/ml for MkLM, incubation time: 10 minutes.
| System | Inhibitor | IC50, 0 min | IC50, 20 min | IC50 Shift | Reference |
|---|---|---|---|---|---|
| µM | µM | ||||
| c3A4 | KTZ | 0.03 | na | na | |
| MkLM | KTZ | 0.016 | na | na | |
| h3A4 | KTZ | 0.037 | na | na | |
| HLM | KTZ | 0.025 | na | na | |
| c3A4 | TAO | 1.1 | 0.17 | 8x | |
| MkLM | TAO | 20.5 | 2.3 | 9x | |
| h3A4 | TAO | >40 | 3.8 | >10x | |
| HLM | TAO | 23 | 0.85 | 27x | (Parkinson et al., 2011) |
na, not applicable.