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. Author manuscript; available in PMC: 2022 Jan 21.
Published in final edited form as: Cell Chem Biol. 2020 Nov 5;28(1):34–45.e6. doi: 10.1016/j.chembiol.2020.10.007

Fig. 4.

Fig. 4.

Compounds designed to target r(CUG)exp engage the target in DM1 fibroblasts, as determined by C-Chem-CLIP. (A) Chem-CLIP target engagement in cells using Chem-CLIP probe 2H-K4NMeS-CA-Biotin, which selectively cross-links and enriches r(CUG)exp-containing DMPK transcripts in DM1 fibroblasts. The probe does not enrich DMPK in wild-type fibroblasts. (n = 3 for both DM1 and WT fibroblasts). Data for WT fibroblasts was previously collected in Rzuczek et al. (Rzuczek et al., 2017). **, P < 0.01, as determined by a two-tailed Student t-test. (B) Competitive Chem-CLIP (C-Chem-CLIP) to study target engagement by 2b and 3b. DM1 fibroblasts were co-treated with 100 nM of 2H-K4NMeS-CA-Biotin and varying concentrations of 2b or 3b to calculate the IC50s, or relative target occupancy in cells (n = 3). For 2b the IC50 is 38±9 nM, and for 3b the IC50 is 3400±60 nM. Data are represented as mean ± SD. See also Figure S3.