Name | TPI-1 |
Synonyms | TPI1 TPI 1 TPI-1 TPI1 TPI 1 2-(2,5-Dichlorophenyl)-1,4-benzoquinone 2',5'-Dichloro-[1,1'-biphenyl]-2,5-dione 2-(2,5-dichlorophenyl)cyclohexa-2,5-diene-1,4-dione 2,5-Cyclohexadiene-1,4-dione, 2-(2,5-dichlorophenyl)- |
CAS | 79756-69-7 |
Molecular Formula | C12H6Cl2O2 |
Molar Mass | 253.08 |
Solubility | 10 mM in DMSO |
Storage Condition | 2-8°C |
In vitro study | 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. |
In vivo study | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.951 ml | 19.757 ml | 39.513 ml |
5 mM | 0.79 ml | 3.951 ml | 7.903 ml |
10 mM | 0.395 ml | 1.976 ml | 3.951 ml |
5 mM | 0.079 ml | 0.395 ml | 0.79 ml |
biological activity | TPI-1 (Tyrosine Phosphatase Inhibitor 1) is an effective SHP-1 inhibitor, and the IC50 for recombinant SHP-1 is 40 nM. TPI-1 has anti-cancer activity. |
target | TargetValue SHP-1 (Cell-free say) 40 nM |
Target | Value |
SHP-1 (Cell-free assay) | 40 nM |
in vitro study | 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. |
in vivo studies | TPI-1 inhibits the growth of B16 melanoma tumours 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 tumour growth and prolongs tumour mice survival as a tolerated s.c. agent. |