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. 2023 Apr 26;14(8):1492–1511. doi: 10.1039/d2md00371f

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 graphic file with name d2md00371f-u27.jpg 3.7 ± 1.7 15.9 ± 1.6 264.9b
40 graphic file with name d2md00371f-u28.jpg 3.9 ± 0.4 29 ± 4.3 126.8b
41 graphic file with name d2md00371f-u29.jpg 4.4 ± 0.4 12.4 ± 4 Not active
42 graphic file with name d2md00371f-u30.jpg 3.6 ± 0.7 9.3 ± 2.5 Not active
47 graphic file with name d2md00371f-u31.jpg 3.5 ± 1.3 27.3 ± 2.0 12.3c
48 graphic file with name d2md00371f-u32.jpg 3.0 ± 0.6 11.3 ± 2.4 Not active
49 graphic file with name d2md00371f-u33.jpg 5.2 ± 0.7 27.1 ± 0.8 Not active
a

IC50 and 95% CI of triplicates, n = 1, except

b

and

c

. Mean and SEM of 3 and 2 independent experiments, each in triplicate respectively.