79756-69-7
79756-69-7 structure
- Name: TPI-1
- Chemical Name: 2-(2,5-dichlorophenyl)cyclohexa-2,5-diene-1,4-dione
- CAS Number: 79756-69-7
- Molecular Formula: C12H6Cl2O2
- Molecular Weight: 253.08100
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphatase
- Create Date: 2017-02-25 04:35:32
- Modify Date: 2024-01-09 13:23:37
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TPI-1 is a SHP-1 inhibitor; inhibits recombinant SHP-1 with an IC50 of 40 nM.
| Name | 2-(2,5-dichlorophenyl)cyclohexa-2,5-diene-1,4-dione |
|---|---|
| Synonyms | TPI-1 |
| Description | TPI-1 is a SHP-1 inhibitor; inhibits recombinant SHP-1 with an IC50 of 40 nM. |
|---|---|
| Related Catalog | |
| Target |
IC50: 40 nM (recombinant SHP-1)[1] |
| In Vitro | SHP-1 has been implicated as a potential cancer therapeutic target. TPI-1 is effective starting at 10 ng/mL in increasing SHP-1 phospho-substrates pLck-pY394. TPI-1 selectively increases SHP-1 phospho-substrates (pLck-pY394, pZap70 and pSlp76) in Jurkat T cells but has little effects on pERK1/2 or pLck-pY505. TPI-1 induces mouse splenic-IFNγ+ cells and induces IFNγ+ cells in human peripheral blood[1]. |
| In Vivo | TPI-1 inhibits the growth of B16 melanoma tumors in mice at a tolerated oral dose in a T cell-dependent manner but has little effects on B16 cell growth in culture. TPI-1 thus also increases pLck-pY394 and IFNγ+ cells in mice. TPI-1 also inhibits B16 tumor growth and prolongs tumor mice survival as a tolerated s.c. agent[1]. |
| Animal Admin | Mice: For in vivo induction of pLck-pY394 and IFNγ+ cells in mice, C57BL/6J mice are treated with PBS or TPI-1 (1 or 3 mg/kg, s.c.) for 4 days. Spleens are harvested one hour post-treatment on day 4 and processed into splenocytes, which are used for assessing pLck-pY394 levels by SDS-PAGE/Western blotting and for quantification of IFNγ+ cells by ELISPOT assays. Mice are also treated with TPI-1 (10 mg/kg, daily, s.c.) to evaluate the toxicity of the compounds in vivo[1]. |
| References |
| Molecular Formula | C12H6Cl2O2 |
|---|---|
| Molecular Weight | 253.08100 |
| Exact Mass | 251.97400 |
| PSA | 34.14000 |
| LogP | 3.08480 |
| Storage condition | 2-8℃ |
