TPI-1


Catalog No. size PriceQuantity
M6547-2 2mg solid $84
M6547-10 10mg solid $320

Description

Cas:79756-69-7

Product Information:

TPI-1, also known as Tyrosine Phosphatase Inhibitor 1, is a SHP-1 inhibitor. TPI-1 selectively increased SHP-1 phospho-substrates (pLck-pY394, pZap70, and pSlp76) in Jurkat T cells but had little effects on pERK1/2 or pLck-pY505 regulated by phosphatases SHP-2 or CD45, respectively. TPI-1 induced mouse splenic-IFN-gamma(+) cells in vitro, approximately 58-fold more effective than sodium stibogluconate, and increased mouse splenic-pLck-pY394 and -IFN-gamma(+) cells in vivo.

 

Chemical Formula: 12H6Cl2O2

 

Exact Mass: 251.9745

 

Molecular Weight: 253.078

 

Elemental Analysis: C, 56.95; H, 2.39; Cl, 28.02; O, 12.64

 

Synonym:

 

TPI-1

TPI 1

TPI1

Tyrosine Phosphatase Inhibitor 1

 

Chemical Name:

2-(2,5-dichlorophenyl)-2,5-cyclohexadiene-1,4-dione

 

InChi Key: 

ZKHFYORNAYYOTM-UHFFFAOYSA-N

 

InChi Code: InChI=1S/C12H6Cl2O2/c13-7-1-3-11(14)9(5-7)10-6-8(15)2-4-12(10)16/h1-6H

 

Smiles Code:

O=C1C(C2=CC(Cl)=CC=C2Cl)=CC(C=C1)=O

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

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. 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.

 

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. 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.

 

 

References

 

  1. Kundu S, Fan K, Cao M, Lindner DJ, Zhao ZJ, Borden E, Yi T. 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. Epub 2010 Apr 26. PubMed PMID: 20421638; PubMed Central PMCID: PMC3049920.

 

Products are for research use only. Not for human use.

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