1. Metabolic Enzyme/Protease
    PI3K/Akt/mTOR
    Apoptosis
  2. Phosphatase
    Akt
    Apoptosis
  3. SHP2-IN-8

SHP2-IN-8 

Cat. No.: HY-144396
Handling Instructions

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.

For research use only. We do not sell to patients.

SHP2-IN-8 Chemical Structure

SHP2-IN-8 Chemical Structure

CAS No. : 1801692-60-3

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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].

IC50 & 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].

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

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

Formula

C17H21Cl2N5S

CAS No.
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Storage

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

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SHP2-IN-8
Cat. No.:
HY-144396
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