A selective inhibitor of the mouse carboxylesterases Ces3 and Ces 1f (IC50 = ~0.1 µM); corrects multiple features of metabolic syndrome in obese-diabetic db/db mice and in mice with diet-induced obesity; also inhibits hCES1

WWL113 – 10 mg

Brand:
Cayman
CAS:
947669-86-5
Storage:
-20
UN-No:
Non-Hazardous - /

Mouse carboxylesterase 3 (Ces3, also named Ces 1d) mediates triglyceride hydrolysis in white adipose tissue, liberating free fatty acids into circulation.{26465} Although important for basal lipolysis, Ces3 expression can be induced by xenobiotics.{26466,26464} Ces3 activity is significantly elevated during adipocyte differentiation.{26463} WWL113 is a selective inhibitor of Ces3 and the structurally related Ces 1f (IC50 = ~0.1 µM) without significantly affecting several related enzymes.{26463} It significantly reduces basal lipolysis in adipocytes.{26463} More interestingly, WWL113 corrects multiple features of metabolic syndrome in obese-diabetic db/db mice, including changes in weight gain, glucose tolerance, and levels of nonesterified free fatty acids, triglycerides, total cholesterol, and fasted glucose.{26463} It has similar effects in mice with diet-induced obesity.{26463} WWL113 also inhibits the human ortholog of mouse Ces3, hCES1 (IC50 = ~50 nM), which has a similar tissue expression pattern to Ces3.{26464,26463}  

 

Add to quotes
SKU: - Category:

Description

A selective inhibitor of the mouse carboxylesterases Ces3 and Ces 1f (IC50 = ~0.1 µM); corrects multiple features of metabolic syndrome in obese-diabetic db/db mice and in mice with diet-induced obesity; also inhibits hCES1, the human ortholog of mouse Ces3 (IC50 = ~50 nM)

Formal name: 4′-[[[methyl[[3-(4-pyridinyl)phenyl]methyl]amino]carbonyl]oxy]-[1,1′-biphenyl]-4-carboxylic acid, ethyl ester

Synonyms: 

Molecular weight: 466.5

CAS: 947669-86-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Metabolic Syndrome||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Obesity

Related products

  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 100 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 - 100 µg

    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 – 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
    View product page
  • A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 25 mg

    The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 25 mg

    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