SHP2 protein degrader-1 is a highly efficient allosteric inhibitor targeting SHP2. It effectively induces degradation of SHP2 protein, resulting in cell apoptosis. This compound shows promising potential for studying diseases associated with SHP2.

SHP2 protein degrader-1 (compound SP4) (0-200 μM; 24 hours) inhibits the growth of Hela cells, with IC 50 of 5.77 and 4.30 nM, respectively, which are about 100 times higher than the activity of SHP099 (SHP2 inhibitor)[1]. SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) induces 54.01% apoptotic death compared with 0.13% of the control at 100 nM[1]. SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) induces cell cycle arrested at the G1 phase in Hela cells[1]. SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) significantly inhibits the phosphorylation of JNK, Erk and p38[1]. SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) inhibits RAS/MAPK signaling and cellular responses by a mechanism involving inhibition of SHP2 catalytic activity[1]. Cell Viability Assay[1]Cell Line: Hela cells Concentration: 0-200 ?μM Incubation Time: 24 hours Result: Strongly inhibited the growth of Hela cells, with IC 50 of 5.77 and 4.30 nM, respectively, which were about 100 times higher than the activity of SHP099 (SHP2 inhibitor). Apoptosis Analysis[1]Cell Line: Hela cells Concentration: 0-100 ?μM Incubation Time: 96 hours Result: Induced 54.01% apoptotic death compared with 0.13% of the control at 100 nM. While SHP099 at 1000 nM could induce 33.74% apoptotic death compared with 0.13% of the control. Cell Cycle Analysis[1]Cell Line: Hela cells Concentration: 0-100 ?μM Incubation Time: 96 hours Result: Induced cell cycle arrested at the G1 phase in Hela cells. Western Blot Analysis[1]Cell Line: Hela cells Concentration: 0-100 ?μM Incubation Time: 96 hours Result: Significantly inhibited the phosphorylation of JNK, Erk and p38.