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
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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]. |
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| 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 |
| Molecular Formula | C17H21Cl2N5S |
|---|---|
| Molecular Weight | 398.35 |