Effect of analogues 33, 40–42, 47 and 48 on purified dyn I lipid-stimulated GTPase activity (IC50a (μM)), in-cell endocytosis of Alexa labelled Tfn in U2OS cells (CME) or depolarisation-stimulated uptake of the styryl dye FM4-64 in synaptosomes (SVE).
Compound | Structure | Dynamin I IC50a (μM) | CME IC50 (μM) | SVE IC50 (μM) |
---|---|---|---|---|
33 | 3.7 ± 1.7 | 15.9 ± 1.6 | 264.9b | |
40 | 3.9 ± 0.4 | 29 ± 4.3 | 126.8b | |
41 | 4.4 ± 0.4 | 12.4 ± 4 | Not active | |
42 | 3.6 ± 0.7 | 9.3 ± 2.5 | Not active | |
47 | 3.5 ± 1.3 | 27.3 ± 2.0 | 12.3c | |
48 | 3.0 ± 0.6 | 11.3 ± 2.4 | Not active | |
49 | 5.2 ± 0.7 | 27.1 ± 0.8 | Not active |
IC50 and 95% CI of triplicates, n = 1, except
and
. Mean and SEM of 3 and 2 independent experiments, each in triplicate respectively.