A cell-permeable LXR inverse agonist that induces LXR-corepressor interaction at nanomolar concentrations; disrupts the Warburg effect in cancer cells in culture and in vivo

SR9243 – 1 mg

Brand:
Cayman
CAS:
1613028-81-1
Storage:
-20
UN-No:
Non-Hazardous - /

The liver X receptors (LXRs) are nuclear receptors that act as ligand-dependent transcription factors.{24819} They modulate lipid, cholesterol, and carbohydrate metabolism and homeostasis. SR9243 is a cell-permeable LXR inverse agonist that induces LXR-corepressor interaction at nanomolar concentrations.{29550} It reduces cancer cell viability (IC50 values range from 15 to 104 nM) without cytotoxicity against non-malignant cells.{29550} SR9243 disrupts the Warburg effect in cancer cells, suppressing the expression of glycolytic and lipogenic genes and reducing glycolytic metabolites and lipid production. It is effective in vivo, blocking glycolytic and lipogenic gene expression and inducing apoptosis in colon cancer xenografts without inducing weight loss in mice.{29550}  

 

Available on backorder

Add to quotes
SKU: - Category:

Description

A cell-permeable LXR inverse agonist that induces LXR-corepressor interaction at nanomolar concentrations; disrupts the Warburg effect in cancer cells in culture and in vivo, suppressing the expression of glycolytic and lipogenic genes and reducing glycolytic metabolites and lipid production

Formal name: N-[2-(3-bromophenyl)ethyl]-2,4,6-trimethyl-N-[[3’-(methylsulfonyl)[1,1’-biphenyl]-4-yl]methyl]-benzenesulfonamide

Synonyms: 

Molecular weight: 626.6

CAS: 1613028-81-1

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Inverse Agonists||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Metabolism||Research Area|Endocrinology & Metabolism|Carbohydrate Metabolism||Research Area|Endocrinology & Metabolism|Hormones & Receptors|FXRs & LXRs||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors

Related products

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

    1,2-Dipalmitoyl-sn-glycero-3-PC – 100 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 - 100 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 25 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 - 25 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 10 mg

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}  

     

    Brand:
    Cayman
    SKU:10009569 - 10 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) – 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
    Add to quotes
    View product page