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Fig. 1 | Journal of Biomedical Science

Fig. 1

From: Novel, thalidomide-like, non-cereblon binding drug tetrafluorobornylphthalimide mitigates inflammation and brain injury

Fig. 1

TFBP and TFNBP do not bind cereblon or lower levels of neo-substrate SALL4. Chemical structures of thalidomide (A) and pomalidomide (B). The binding of TFBP (C) and TFNBP (D) to cereblon was examined through use of a cereblon/BRD3 binding FRET assay (E). TFBP and TFNBP were not able to bind cereblon (IC50 53.45 μM and > 100 μM, respectively), compared to Pom (IC50 3.36 μM) (F). Concentration- dependent degradation of the downstream neo-substrates SALL4 was evaluated in human Tera-1 cells. TFBP and TFNBP at 0.1 μM and 1 μM did not lower expression levels of SALL4, in contrast to Pom at a 1 μM concentration (G, H). *p < 0.05 vs. control group. Values are presented as mean ± S.E.M., of n observations [N = 2 or 3 per group over 8 concentrations (E) to generate an IC50 value (F); N = 3 per group re: SALL4 expression (H)]

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