TPI-1
(Synonyms: Tyrosine Phosphatase Inhibitor 1) 目录号 : GC18239An inhibitor of protein tyrosine phosphatases
Cas No.:79756-69-7
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | 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: [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. |
TPI-1, also known as Tyrosine Phosphatase Inhibitor 1, is a SHP-1 inhibitor; inhibits recombinant SHP-1 with an IC50 of 40 nM.
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].
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].
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.
Cas No. | 79756-69-7 | SDF | |
别名 | Tyrosine Phosphatase Inhibitor 1 | ||
化学名 | 2-(2,5-dichlorophenyl)-2,5-cyclohexadiene-1,4-dione | ||
Canonical SMILES | ClC1=C(C(C(C=C2)=O)=CC2=O)C=C(Cl)C=C1 | ||
分子式 | C12H6Cl2O2 | 分子量 | 253.1 |
溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 1 mg/ml | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 3.951 mL | 19.755 mL | 39.5101 mL |
5 mM | 0.7902 mL | 3.951 mL | 7.902 mL |
10 mM | 0.3951 mL | 1.9755 mL | 3.951 mL |
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