SHP2-IN-8 是一种高效、具有选择性和细胞活性的变构SHP2抑制剂，IC50为 23 nM，Ki为 22 nM。SHP2-IN-8 可逆的、非竞争性的。SHP2-IN-8 能引起显著的热位移，ΔTm 为 7.01 ℃。SHP2-IN-8 可诱导 Hela 细胞凋亡 (Apoptosis)，抑制Akt的磷酸化。

SHP2-IN-8 is a highly potent, selective, and cellularly active allosteric SHP2 inhibitor with IC 50 value of 23 nM and K i of 22 nM. SHP2-IN-8 is reversible and noncompetitive. SHP2-IN-8 causes a significant thermal shift with the ΔTm of 7.01 ℃. SHP2-IN-8 induces the apoptosis and inhibits the phosphorylation of AKT in Hela cells [1].

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.

1801692-60-3

C17H21Cl2N5S

398.35

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years