An antitubercular agent; active against M. tuberculosis in vitro (MICs = 0.5-1.56 μM); inhibits DprE1 (IC50 = 32 nM); reduces lung bacterial burden in a mouse model of chronic tuberculosis infection at 300 mg/kg and exhibits a synergistic effect when administered in combination with TMC207

DprE1-IN-2 – 5 mg

Brand:
Cayman
CAS:
1615713-87-5
Storage:
-20
UN-No:
Non-Hazardous - /

DprE1-IN-2 is an antitubercular agent that is active against M. tuberculosis in vitro, with MIC values ranging from 0.5 to 1.56 μM.{32839} It is an inhibitor of decaprenylphosphoryl-β-D-ribose 2′-epimerase (DprE1; IC50 = 32 nM), an enzyme involved in mycobacterial cell wall biogenesis. DrpE1-IN-2 (300 mg/kg) reduces lung bacterial burden in a mouse model of chronic tuberculosis infection and exhibits a synergistic effect when administered in combination with TMC207 (Item No. 20247).  

 

Out of stock

Add to quotes
SKU: 21034 - Category:

Description

An antitubercular agent; active against M. tuberculosis in vitro (MICs = 0.5-1.56 μM); inhibits DprE1 (IC50 = 32 nM); reduces lung bacterial burden in a mouse model of chronic tuberculosis infection at 300 mg/kg and exhibits a synergistic effect when administered in combination with TMC207

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

Synonyms: 

Molecular weight: 368.4

CAS: 1615713-87-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Antibiotics||Product Type|Biochemicals|Small Molecule Inhibitors||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
    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 – 50 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 - 50 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
  • 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