化合物TPI1 T3962

Product Introduction
Bioactivity


英文名: TPI-1

描述: TPI-1 是一种 SHP-1的抑制剂，其 IC50=40 nM。

激酶实验: Jump-In TI CHO-K cells stably expressing WT or mutant S1P3 are serum-starved for 4 hrs. They are then incubated at 4 °C for 30 min in the binding buffer containing 20 mM Tris-HCl (pH 7.5), 100 mM NaCl, 15 mM NaF, 0.5 mM EDTA, 1 mM Na3VO4, 0.5% fatty acid-free bovine serum albumin, and protease inhibitor mixture with 0.1 nM [33P]S1P and increasing concentrations of S1P, SPM-242, or CYM-5541. Cells are washed three times with cold binding buffer. Cell-bound radioactivity is measured by lysing the cells with 0.5% SDS followed by liquid scintillation counting. The raw data is normalized so that the level of [33P]S1P bound to each cell line (WT or mutant) in the absence of competing ligand is referenced as 100% for its own cell line[1].

体外活性: 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].

体内活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 45 mg/mL (177.81 mM)


关键字: TPI-1 | Inhibitor | inhibit | Phosphatase

相关产品: SHP099 hydrochloride | L-Ascorbic acid 2-phosphate magnesium | Calcineurin Autoinhibitory Peptide acetate | h-NTPDase-IN-1 | Ertiprotafib | 2-Bromo-4'-hydroxyacetophenone | h-NTPDase8-IN-1 | Disodium monofluorophosphate | D-ERYTHRO-SPHINGOSINE | Salubrinal

相关库: Glycometabolism Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Phosphatase Inhibitor Library | Inhibitor Library | Nuclear Receptor Compound Library | Metabolism Compound Library | Endocrinology-Hormone Compound Library | Bioactive Compound Library

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