FIGURE

Fig. 6

ID

ZDB-FIG-221212-6

Publication

Lu et al., 2021 - Discovery of a subtype-selective, covalent inhibitor against palmitoylation pocket of TEAD3

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Fig. 6

Figure 6. DC-TEAD3in03 selectively engaged TEAD3 in cells. (A) HEK293T cells were treated with 50 μmol/L DC-TEADin1072 for 6 h in CETSA experiments to demonstrate the direct binding of DC-TEADin1072 with TEAD1 and TEAD3 in intact cells. (B) HEK293T cells were treated with 50 μmol/L DC-TEAD3in03 for 6 h in CETSA experiments to demonstrate that DC-TEAD3in03 significantly increased the thermal stability of TEAD3 in intact cells. (C) and (D) The effect of DC-TEAD3in03 on TEAD-dependent/independent reporter system. The results shown are mean ± SD of three technical replicates (∗P < 0.05, ∗∗P < 0.01, ∗∗∗P < 0.001, ∗∗∗∗P < 0.0001, N.S.: P > 0.05), n = 3. (E) The effect of DC-TEAD3in03 on TEAD1, TEAD2, TEAD3, and TEAD4 activities in GAL4 reporter system. HEK293T cells were transfected with a GAL4-LUC reporter, together with expression vectors for GAL4-TEADs constructs as indicated. The results shown are mean of three technical replicates, n = 3.

Expression Data

Expression Detail

Antibody Labeling

Phenotype Data

Phenotype Detail

Acknowledgments

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