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 – 10 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).  

 

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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

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