A non-covalent inhibitor of bacterial DprE1; inhibits wild-type M. smegmatis DprE1 and DprE1C394G (IC50 = 0.01 µM for both) but not DprE1Y321H (IC50 = >10 µM); active against wild-type M. tuberculosis DprE1 (MIC = 1.56 µM) and DprE1C387S or DprE1C387G (MICs = 0.39 and 0.78 µM

AZ 7371 – 25 mg

Brand:
Cayman
CAS:
1494675-86-3
Storage:
-20
UN-No:
Non-Hazardous - /

AZ 7371 is a non-covalent inhibitor of decaprenylphosphoryl-β-D-ribose 2’-epimerase (DprE1; IC50 = 10 nM), an enzyme involved in mycobacterial cell wall biogenesis.{32839} It inhibits wild-type M. smegmatis DprE1 and DprE1 harboring the drug-resistance mutation C394G (IC50 = 0.01 µM for both) but not the Y321H mutation (IC50 = >10 µM).{54377} AZ 7371 is active against wild-type M. tuberculosis DprE1 (MIC = 1.56 µM) and M. tuberculosis harboring C387S or C387G mutations (MICs = 0.39 and 0.78 µM, respectively), which confer resistance to the antibiotic BTZ043 (Item No. 22930), but not the Y314H mutation (MIC = >200 µM). It is selective for these targets over Gram-positive and Gram-negative bacteria but does inhibit phosphodiesterase 6 (PDE6; IC50 = 4 µM).  

 

Available on backorder

Add to quotes
SKU: - Category:

Description

A non-covalent inhibitor of bacterial DprE1; inhibits wild-type M. smegmatis DprE1 and DprE1C394G (IC50 = 0.01 µM for both) but not DprE1Y321H (IC50 = >10 µM); active against wild-type M. tuberculosis DprE1 (MIC = 1.56 µM) and DprE1C387S or DprE1C387G (MICs = 0.39 and 0.78 µM, respectively) but not DprE1Y314H (MIC = >200 µM); selective for these targets over Gram-positive and Gram-negative bacteria but does inhibit phosphodiesterase 6 (PDE6; IC50 = 4 µM)

Formal name: N-(2-hydroxyethyl)-1-[(6-methoxy-5-methyl-4-pyrimidinyl)methyl]-6-methyl-1H-pyrrolo[3,2-b]pyridine-3-carboxamide

Synonyms: 

Molecular weight: 355.4

CAS: 1494675-86-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Antibiotics||Product Type|Biochemicals|Small Molecule Inhibitors|Phosphodiesterases||Research Area|Cell Biology|Cell Signaling|cGMP Signaling||Research Area|Immunology & Inflammation||Research Area|Infectious Disease|Bacterial Diseases|Tuberculosis

Related products

  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 50 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 - 50 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 – 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
  • 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 zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 50 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 - 50 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page