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. Author manuscript; available in PMC: 2022 Dec 1.
Published in final edited form as: Oncogene. 2022 May 7;41(24):3328–3340. doi: 10.1038/s41388-022-02340-8

Fig. 1. Design of the CRBN-based WDR5 PROTAC MS40 and measurement of MS40 binding to WDR5 and Cereblon (CRBN).

Fig. 1

A, B Chemical structures of MS40 A and its CRBN-inactive analogue MS40N1 B. C Replicated inverse ITC titrations of WDR5 into MS40 (top), CRBN’s thalidomide-binding domain (TBD) into MS40 (middle) and WDR5 into the complex of CRBN TBD and MS40 (bottom) for measuring the binding kinetics and cooperativity (α) for MS40. The calculated values represent the mean ± SD from three independent experiments. First injection has been removed from the fitting. D Replicated inverse ITC titrations of CRBN TBD into MS40N1 for measuring binding kinetics.