A reactivator of p53; impairs the interaction between FAK and p53 and restores p53 transcriptional activity at 111

Roslin-2 – 25 mg

Brand:
Cayman
CAS:
29574-21-8
Storage:
-20
UN-No:
Non-Hazardous - /

Roslin-2 is a reactivator of p53.{46386} Roslin-2 (111, 333, and 1000 µM) impairs the interaction between focal adhesion kinase (FAK) and p53 and restores p53 transcriptional activity. It reverses FAK-mediated suppression of the expression of p53-dependent p21, MDM2, and Bax in wild-type p53 HCT116 colon and MCF-7 breast cancer cells, but not in p53 mutant SW620 colon cancer cells, when used at concentrations ranging from 1 to 50 µM. Roslin-2 (10 µM) potentiates the pro-apoptotic effect of doxorubicin (Item No. 15007) and 5-fluorouracil (Item No. 14416) in p53+/+, but not p53-/-, HCT116 cells. It reduces tumor growth and activates p21 in p53+/+, but not p53-/- tumors, in HCT116 mouse xenograft models when administered at a dose of 60 mg/kg.  

 

Out of stock

Add to quotes
SKU: 21985 - Category:

Description

A reactivator of p53; impairs the interaction between FAK and p53 and restores p53 transcriptional activity at 111, 333, and 1000 µM; reverses FAK-mediated suppression of the expression of p53-dependent p21, MDM2, and Bax in wild-type p53 HCT116 colon and MCF-7 breast cancer cells, but not in p53 mutant SW620 colon cancer cells at 1-50 µM; potentiates the pro-apoptotic effect of doxorubicin and 5-fluorouracil in p53+/+, but not p53-/-, HCT116 cells at 10 µM; reduces tumor growth and activates p21 in p53+/+, but not p53-/- tumors, in HCT116 mouse xenograft models at 60 mg/kg

Formal name: 1-(phenylmethyl)-3,5,7-triaza-1-azoniatricyclo[3.3.1.13,7]decane, monobromide

Synonyms: 

Molecular weight: 311.2

CAS: 29574-21-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Activators|Transcription Factors & Coactivators||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|p53 Signaling||Research Area|Cancer|Transcription Factors|p53

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 – 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
  • 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
    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
  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 250 mg

    1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}  

     

    Brand:
    Cayman
    SKU:10009473 - 250 mg

    Available on backorder

    Add to quotes
    View product page