SHP2-IN-8

Modify Date: 2025-08-27 06:52:05

SHP2-IN-8 Structure
SHP2-IN-8 structure
Common Name SHP2-IN-8
CAS Number 1801692-60-3 Molecular Weight 398.35
Density N/A Boiling Point N/A
Molecular Formula C17H21Cl2N5S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of SHP2-IN-8


SHP2-IN-8 is a highly potent, selective, and cellularly active allosteric SHP2 inhibitor with IC50 value of 23 nM and Ki 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].

 Names

Name SHP2-IN-8

 SHP2-IN-8 Biological Activity

Description SHP2-IN-8 is a highly potent, selective, and cellularly active allosteric SHP2 inhibitor with IC50 value of 23 nM and Ki 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].
Related Catalog
Target

IC50: 23 nM (SHP2)[1] Ki: 22 nM (SHP2)[1]

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.
References

[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.

 Chemical & Physical Properties

Molecular Formula C17H21Cl2N5S
Molecular Weight 398.35
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