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. Author manuscript; available in PMC: 2023 Apr 19.

Published in final edited form as: J Med Chem. 2022 Dec 2;65(24):16432–16450. doi: 10.1021/acs.jmedchem.2c01300

Figure 4. — SOS1 degradation in colorectal cancer cell lines. (A) Immunoblots in SW620 cells treated with P7 for 6 hours in comparison to SOS1 inhibitor BI3406 and siSOS1. (B) Immunoblots in SW620 cells treated with SOS1 degrader P7 and inactive compound P2, with GAPDH used as the loading control at different time points; Cells were treated with 1 μM of P7 and P2 for indicated times, respectively. (C) SW620 cells were pre-treated with cycloheximide (CYC) for 1 hour at 100 μg/mL, followed by addition of DMSO or 1 μM P7. At the indicated times, cells were lysed and SOS1 levels were analyzed by western blot. (D) Mechanistic investigation of SOS1 degradation induced by P7 in SW620 cells. Cells were pretreated with BI3406 10 μM, lenalidomide 10 μM, MLN4924 0.5 μM, and MG132 3 μM for 1 hour, followed by a 24 h treatment with P7 at 1 μM. (E) SOS1 degradation in colorectal cancer cells treated with SOS1 degrader P7 at different concentrations for 24 hours.

Figure 4. — SOS1 degradation in colorectal cancer cell lines. (A) Immunoblots in SW620 cells treated with P7 for 6 hours in comparison to SOS1 inhibitor BI3406 and siSOS1. (B) Immunoblots in SW620 cells treated with SOS1 degrader P7 and inactive compound P2, with GAPDH used as the loading control at different time points; Cells were treated with 1 μM of P7 and P2 for indicated times, respectively. (C) SW620 cells were pre-treated with cycloheximide (CYC) for 1 hour at 100 μg/mL, followed by addition of DMSO or 1 μM P7. At the indicated times, cells were lysed and SOS1 levels were analyzed by western blot. (D) Mechanistic investigation of SOS1 degradation induced by P7 in SW620 cells. Cells were pretreated with BI3406 10 μM, lenalidomide 10 μM, MLN4924 0.5 μM, and MG132 3 μM for 1 hour, followed by a 24 h treatment with P7 at 1 μM. (E) SOS1 degradation in colorectal cancer cells treated with SOS1 degrader P7 at different concentrations for 24 hours.