A cell-permeable

NFAT Inhibitor – 10 mg

Brand:
Cayman
CAS:
249537-73-3
Storage:
-20
UN-No:
Non-Hazardous - /

The nuclear factor of activated T cells (NFAT) is a member of the REL family of transcription factors that is involved in regulating transcription of proinflammatory genes, including IL-2 and TNF-α. Calcineurin-mediated dephosphorylation promotes translocation of NFAT proteins into the nucleus, where they bind specific elements within target gene promoters, in many cases through association with other transcription factors such as AP-1, NFκB, MEF-2, and PPARγ. Molecules that interfere with this signaling pathway have potential to be effective in regulating immunosuppressive and anti-inflammatory responses. NFAT inhibitor is a cell-permeable compound that selectively inhibits calcineurin-mediated dephosphorylation of NFAT.{21639,21640,7199} At 100 μM, this inhibitor effectively blocks calcineurin binding to NFAT without disrupting other calcineurin-dependent pathways, unlike the immunosuppressants cyclosporin A and FK506 (Item No. 10007965) which indiscriminately block all calcineurin phosphatase activity.{21639,7199} NFAT inhibitor can disrupt NFAT-dependent expression of IL-2 and TNF-α when transfected in Jurak T cells and can prevent the activation and proliferation of T cells both in vitro (~ 43% at 1 µM using mixed lymphocyte cultures) and in vivo (10 mg/kg using C3H/HeN mice).{7199}  

 

Add to quotes
SKU: - Category:

Description

A cell-permeable, selective inhibitor of calcineurin-mediated dephosphorylation of NFAT that does not disrupt other calcineurin-dependent pathways; disrupts NFAT-dependent expression of IL-2 and TNF-α when transfected in Jurak T cells and prevents the activation and proliferation of T cells both in vitro (~ 43% at 1 µM using mixed lymphocyte cultures) and in vivo (10 mg/kg using C3H/HeN mice)

Formal name: L-methionyl-L-alanylglycyl-L-prolyl-L-histidyl-L-prolyl-L-valyl-L-isoleucyl-L-valyl-L-isoleucyl-L-threonylglycyl-L-prolyl-L-histidyl-L-α-L-glutamic acid

Synonyms: 

Molecular weight: 1,683.90

CAS: 249537-73-3

Purity: ≥95%

Formulation: A lyophilized powder

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors||Research Area|Immunology & Inflammation|Adaptive Immunity

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) – 10 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 - 10 µg

    Available on backorder

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

    Anhydrotetracycline (hydrochloride) – 50 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 - 50 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 – 100 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 - 100 mg

    Available on backorder

    Add to quotes
    View product page