Effect of different xanthates on the 7-EFC O-deethylation activity of P-450 2B1
Xanthate | KI | kinactivation | T1/2 | Partition Ratio | Ki |
---|---|---|---|---|---|
μM | min−1 | min | μM | ||
C2 | 27 | 0.22 | 3.2 | 43 | 66 |
C3 | 40 | 0.21 | 3.3 | 33 | 21 |
C3iso | 5.4 | 0.05 | 15 | 99 | 3.5 |
C3allyl | 11 | 0.07 | 9.5 | 108 | 26 |
C4 | 23 | 0.09 | 7.5 | 63 | 5.0 |
D609 | 15 | 0.10 | 7.2 | 42 | 20 |
Cyclohexyl | 16 | 0.06 | 12 | 62 | 71 |
C5 | 10 | 0.07 | 9.5 | 56 | 7.2 |
C8 | 2.4 | 0.07 | 10 | 4 | 6.4 |
C10 | 8.3 | 0.11 | 6.6 | 47 | 8.2 |
C12 | 14 | 0.12 | 5.6 | 51 | 5.8 |
C14 | 21 | 0.05 | 14 | 201 | 3.6 |
C16 | 52 | 0.03 | 21 | 530 | 3.3 |
C18 | 31 | 0.02 | 33 | 594 | 3.0 |
C20 | 69 | 0.03 | 25 | 600 | 2.3 |
Assay conditions were as described in Experimental Procedures. The data shown represent the mean from three to five separate experiments.