An inhibitor of protein tyrosine phosphatases; increases phosphorylated substrates of the phosphatase SHP-1 in Jurkat T cells; selective for SHP-1 over SHP-2

TPI-1 – 5 mg

Brand:
Cayman
CAS:
79756-69-7
Storage:
-20
UN-No:
Non-Hazardous - /

TPI-1 is an inhibitor of protein tyrosine phosphatases.{41578} TPI-1 (10 ng/ml) increases phosphorylated substrates of the phosphatase SHP-1 in Jurkat T cells, including pLck-pY394, pZap70, and pSlp76. It is selective for SHP-1 over SHP-2, having low activity at the SHP-2 substrate pERK1/2. It increases pLck-pY394 levels by approximately 3.3-fold and increases the number of IFN-γ+ cells in mouse spleen ex vivo following a dose of approximately 3 mg/kg. Oral administration of TPI-1 (3 mg/kg per day) inhibits tumor growth in a B16 melanoma mouse xenograft model.  

 

Out of stock

Add to quotes
SKU: 22480 - Category:

Description

An inhibitor of protein tyrosine phosphatases; increases phosphorylated substrates of the phosphatase SHP-1 in Jurkat T cells; selective for SHP-1 over SHP-2, having low activity at the SHP-2 substrate pERK1/2; increases pLck-pY394 levels by ~3.3-fold and increases the number of IFN-γ+ spleen cells in mouse spleen ex vivo (~3 mg/kg); inhibits tumor growth in a B16 melanoma mouse xenograft model (3 mg/kg per day, oral)

Formal name: 2-(2,5-dichlorophenyl)-2,5-cyclohexadiene-1,4-dione

Synonyms:  Tyrosine Phosphatase Inhibitor 1

Molecular weight: 253.1

CAS: 79756-69-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phosphatases||Research Area|Cancer|Cell Signaling

Related products

  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 50 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 50 mg

    Available on backorder

    Add to quotes
    View product page
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 50 µg

    The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.  

     

    Brand:
    Cayman
    SKU:10009531 - 50 µg

    Available on backorder

    Add to quotes
    View product page
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 250 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 250 mg

    Available on backorder

    Add to quotes
    View product page
  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 500 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 500 mg

    Available on backorder

    Add to quotes
    View product page