1801692-60-3

1801692-60-3 structure

Name: SHP2-IN-8
Chemical Name: SHP2-IN-8
CAS Number: 1801692-60-3
Molecular Formula: C₁₇H₂₁Cl₂N₅S
Molecular Weight: 398.35
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2022-05-24 19:08:22
Modify Date: 2024-01-13 18:57:34
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].

Name	SHP2-IN-8

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	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphatase Signaling Pathways >> PI3K/Akt/mTOR >> Akt
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.

Molecular Formula	C₁₇H₂₁Cl₂N₅S
Molecular Weight	398.35

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