An inhibitor of ASCT2; inhibits glutamine uptake (IC50s = 9 and 9.6 µM for the rat and human transporters

V-9302 – 1 mg

Brand:
Cayman
CAS:
1855871-76-9
Storage:
-20
UN-No:
Non-Hazardous - /

V-9302 is an inhibitor of amino acid transporter 2 (ASCT2).{56045} It inhibits glutamine uptake with IC50 values of 9 and 9.6 µM for the rat and human transporters, respectively. V-9302 also inhibits glutamine uptake in HEK293 cells and reduces cell viability of a variety of cancer cell lines, including HCT116, HT-29, COLO 205, and RKO cells (EC50s = 8.9, 9.4, 14.5, and 8.3 µM, respectively).{56046} It reduces glutamine uptake into tumor tissue and prevents tumor growth in HCT116 and HT-29 mouse xenograft models expressing K-RasG13D and BRAFV600E mutations, respectively, when administered at a dose of 75 mg/kg per day for 21 days.  

 

Available on backorder

Add to quotes
SKU: 27688 - 1 mg Category:

Description

An inhibitor of ASCT2; inhibits glutamine uptake (IC50s = 9 and 9.6 µM for the rat and human transporters, respectively); reduces cell viability of a variety of cancer cell lines, including HCT116, HT-29, COLO 205, and RKO cells (EC50s = 8.9, 9.4, 14.5, and 8.3 µM, respectively); reduces glutamine uptake into tumor tissue and prevents tumor growth in HCT116 and HT-29 mouse xenograft models expressing K-RasG13D and BRAFV600E mutations, respectively, at 75 mg/kg per day for 21 days

Formal name: (2S)-2-amino-4-[bis[[2-[(3-methylphenyl)methoxy]phenyl]methyl]amino]-butanoic acid

Synonyms: 

Molecular weight: 538.7

CAS: 1855871-76-9

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Cancer|Tumor Microenvironment

Related products

  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 25 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 - 25 µg

    Available on backorder

    Add to quotes
    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
    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 – 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
    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
    Add to quotes
    View product page