A metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-κB with an EC50 of 0.47 µM; has broad anticancer activity in mice when administered orally

CBL0137 – 10 mg

Brand:
Cayman
CAS:
1197996-80-7
Storage:
-20
UN-No:
Non-Hazardous - /

CBL0137 is a metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-κB with an EC50 of 0.47 µM.{30977} It functionally inactivates the facilitates chromatin transcription complex (FACT), driving the effects on p53 and NF-κB and promoting cancer cell death.{30977} CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates efficacy of gemcitabine (Item No. 11690) in preclinical models of pancreatic cancer.{30977,30976}  

 

Available on backorder

Add to quotes
SKU: - Category:

Description

A metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-κB with an EC50 of 0.47 µM; has broad anticancer activity in mice when administered orally

Formal name: 1,1′-[9-[2-[(1-methylethyl)amino]ethyl]-9H-carbazole-3,6-diyl]bis-ethanone

Synonyms:  CBLC137|Curaxin 137

Molecular weight: 336.4

CAS: 1197996-80-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Activators|Transcription Factors & Coactivators||Product Type|Biochemicals|Small Molecule Inhibitors|TNF-α/NF-κB Signaling||Research Area|Cancer|Cell Signaling|NF-κB Signaling||Research Area|Cancer|Cell Signaling|p53 Signaling||Research Area|Cancer|Transcription Factors|NF-κB||Research Area|Cancer|Transcription Factors|p53||Research Area|Immunology & Inflammation|Autoimmunity||Research Area|Immunology & Inflammation|Innate Immunity|Pattern Recognition||Research Area|Immunology & Inflammation|Innate Immunity|STING||Research Area|Infectious Disease

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

    Anhydrotetracycline (hydrochloride) – 100 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 - 100 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
  • 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 – 10 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 - 10 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page