产品描述: TPI-1, also known as Tyrosine Phosphatase Inhibitor 1, is a SHP-1 inhibitor; inhibits recombinant SHP-1 with an IC50 of 40 nM |
靶点:
IC50: 40 nM (recombinant SHP-1);Phosphatase;GlucocorticoidReceptor |
体外研究:
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 |
体内研究:
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 |
参考文献:
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. |
溶解性:
soluble in DMSO |
保存条件:
-20℃ |
配置溶液浓度参考:
|
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 |
50 mM |
0.079 ml |
0.395 ml |
0.79 ml |
|
注意: |
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