| Identification | Back Directory | [Name]
2-(2,5-dichlorophenyl)cyclohexa-2,5-diene-1,4-dione | [CAS]
79756-69-7 | [Synonyms]
TPI-1
TPI1;TPI 1
2-(2,5-Dichlorophenyl)-1,4-benzoquinone
Recombinant Human TIM/TPI1 Protein, His Tag
2,5-Cyclohexadiene-1,4-dione, 2-(2,5-dichlorophenyl)- | [Molecular Formula]
C12H6Cl2O2 | [MDL Number]
MFCD00448731 | [MOL File]
79756-69-7.mol | [Molecular Weight]
253.08 |
| Chemical Properties | Back Directory | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 1 mg/ml | [form ]
A crystalline solid | [color ]
White to yellow | [InChI]
1S/C12H6Cl2O2/c13-7-1-3-11(14)9(5-7)10-6-8(15)2-4-12(10)16/h1-6H | [InChIKey]
ZKHFYORNAYYOTM-UHFFFAOYSA-N | [SMILES]
O=C1C=CC(C(C2=C(C=CC(Cl)=C2)Cl)=C1)=O |
| Hazard Information | Back Directory | [Uses]
TPI-1, also known as Tyrosine Phosphatase Inhibitor 1, is a SHP-1 inhibitor; inhibits recombinant SHP-1 with an IC50 of 40 nM. | [Biological Activity]
TPI-1 (Tyrosine Phosphatase Inhibitor 1) is a potent SHP-1 inhibitor with IC50 of 40 nM for recombinant SHP-1. It has anticancer activity. | [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. It 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 < sup> + cells in human peripheral blood. | [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. It 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 sc agent. | [target]
| Target | Value | SHP-1
(Cell-free assay) | 40 nM |
| [References]
[1] Kundu S, et al. Novel SHP-1 inhibitors tyrosine phosphatase inhibitor-1 and analogs with preclinical anti-tumor activities as tolerated oral agents. J Immunol. 2010 Jun 1;184(11):6529-36. DOI:10.4049/jimmunol.0903562 |
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