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A Four-Point Screening Method for Assessing Molecular Mechanism of Action (MMOA) Identifies Tideglusib as a Time-Dependent Inhibitor of Trypanosoma brucei GSK3β

Fig 7

Two point ATP competition analysis for TbGSK3β inhibitors.

Tideglusib, AZ960, CT99021, LY2784544, sorafenib, and TWS119 at 10μM GSM and 10 μM or 100 μM ATP. GSM mixed with 1x buffer and 10μM or 100μM ATP. TbGSK3β [5 nM] was added to start reaction and incubated at RT for 5 minutes. Reactions were stopped at 80°C and worked up as described in Materials and Methods. Experiments ran in duplicate, N = 2.

Fig 7