Table 4.
concn of 19 (nm) |
inhibition of [3H]CPX binding (% control) |
reversal of inhibition (% control) |
|
---|---|---|---|
(−H2NOH) | (+H2NOH) | ||
100 | 54.4 | 34.5 | 20 |
250 | 63.3 ± 1.2 | 43.6 ± 4.9 | 20 |
500 | 76.0 ± 3.0 | 54.0 ± 4.0 | 22 |
Data are means ± s.e.m. of three experiments or a single experiment. After incubation with the isothiocyanate derivative at 37 °C for 1 h, membranes were washed three times, incubated with hydroxylamine (500 mM, 37 °C for 1 h), washed twice, and then incubated with 0.2 nM [3H]CPX (14). When the hydroxylamine incubation was carried out at 25 °C for 1 h, the degree of reversal was 8% (100 nM 19), 9% (250 nM 19), or 15% (500 nM 19).