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TPI-1

Catalog No. T3962   CAS 79756-69-7
Synonyms: TPI 1, TPI1

TPI-1 is a SHP-1 inhibitor.

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TPI-1 Chemical Structure
TPI-1, CAS 79756-69-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 48.00
2 mg In stock $ 70.00
5 mg In stock $ 117.00
10 mg In stock $ 198.00
25 mg In stock $ 387.00
50 mg In stock $ 588.00
100 mg In stock $ 838.00
500 mg In stock $ 1,720.00
1 mL * 10 mM (in DMSO) In stock $ 129.00
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Purity: 99.79%
Purity: 98.25%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description TPI-1 is a SHP-1 inhibitor.
Targets&IC50 SHP1:40 nM.
In vitro SHP-1 has been identified as a promising target for cancer therapy. TPI-1, starting at an effective concentration of 10 ng/mL, selectively enhances the phosphorylation of SHP-1 substrates (notably pLck-pY394) in Jurkat T cells, without significantly affecting pERK1/2 or pLck-pY505 levels. Moreover, TPI-1 promotes the induction of IFNγ+ cells both in mouse spleen and human peripheral blood[1], demonstrating its potential selectivity and therapeutic efficacy in a cellular context.
In vivo TPI-1 effectively suppresses the growth of B16 melanoma tumors in mice through a mechanism reliant on T cells when administered orally at tolerable doses, yet it demonstrates minimal impact on B16 cell proliferation in vitro. Additionally, TPI-1 enhances the levels of pLck-pY394 and IFNγ+ cells in mice, further contributing to its anti-tumor activity. Notably, TPI-1 also restricts B16 tumor expansion and extends the survival of mice bearing tumors when given as a subcutaneously tolerated agent[1].
Kinase Assay 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].
Synonyms TPI 1, TPI1
Molecular Weight 253.08
Formula C12H6Cl2O2
CAS No. 79756-69-7

Storage

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

Solubility Information

DMSO: 45 mg/mL (177.81 mM)

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Compound Library Bioactive Compound Library Immunology/Inflammation Compound Library Endocrinology-Hormone Compound Library Nuclear Receptor Compound Library Bioactive Compounds Library Max Glycometabolism Compound Library Phosphatase Inhibitor Library Metabolism Compound Library

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Keywords

TPI-1 79756-69-7 Endocrinology/Hormones Metabolism Phosphatase Glucocorticoid Receptor TPI 1 Inhibitor inhibit TPI1 inhibitor

 

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