| Description | SHP2-IN-8 is a reversible, noncompetitive, selective and efficient allosteric SHP2 inhibitor (IC50=23 nM, Ki=22 nM), which also has effects in cells. SHP2-IN-8 can cause significant thermal displacement（ Δ Tm = 7.01 ℃）。 SHP2-IN-8 can inhibit the phosphorylation of AKT and induce apoptosis of Hela cells. |
| In vitro | SHP2-IN-8 (compound TK-453) (0-100 μM; 48 hours) has moderate inhibitory effects on the proliferation of KYSE-70, Hela and THP-1 cells [1]. SHP2-IN-8 (0-30 μM; 24 hours) induces the apoptosis of Hela cells in a concentration-dependent manner [1]. SHP2-IN-8 (0-30 μM; 0-2 hour）concentration- and time-dependently inhibits the phosphorylation of AKT in Hela and KYSE-70 cell lines [1]. Cell Proliferation Assay Cell Line: Hela, KYSE-70, THP-1 [1] Concentration: 0, 1, 3, 10, 30 and 100 μM Incubation Time: 48 hours Result: Showed moderate inhibitory effects on the proliferation of KYSE-70, Hela and THP-1 cells at the concentrations of 30 and 100 μM. Apoptosis Analysis Cell Line: Hela [1] Concentration: 0, 10 and 30 μM Incubation Time: 24 hours Result: Induced the apoptosis of Hela cells in a concentration-dependent manner. Western Blot Analysis Cell Line: Hela and KYSE-70 [1] Concentration: 0, 0.3, 1, 3, 10 and 30 μM; or 10 μM Incubation Time: 2 hours; or 0, 5, 10, 15, 30, 60, 120 min Result: Concentration- and time-dependently inhibited the phosphorylation of AKT in Hela and KYSE-70 cell lines. |
| molecular weight | 398.35 |
| Molecular formula | C17H21Cl2N5S |
| CAS | 1801692-60-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |