SHP2-IN-8 

SHP2-IN-8 is a highly potent, selective, and cellularly active allosteric SHP2 inhibitor with IC₅₀ 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].

IC₅₀: 23 nM (SHP2)^[1]
K_i: 22 nM (SHP2)^[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

398.35

C₁₇H₂₁Cl₂N₅S

1801692-60-3

NC1=NC(N2CCC(C)(CN)CC2)=CN=C1SC3=CC=CC(Cl)=C3Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Tang K, Zhao M, Wu YH, et al. Structure-based design, synthesis and biological evaluation of aminopyrazines as highly potent, selective, and cellularly active allosteric SHP2 inhibitors. Eur J Med Chem. 2022;230:114106.  [Content Brief]