2. Anti-infection
  3. Antibiotic
  4. BB-3497

BB-3497 is a potent, orally active and selective peptide deformylase (PDF) inhibitor. BB-3497 is highly selective for PDF (IC50 = 7 nM for E. coli PDF.Ni) over the other mammalian metalloenzymes (MMP-1/2/3/7 and enkephalinase). BB-3497 exhibits potent activity against gram-positive bacteria and some gram-negative pathogens. BB-3497 protects mice from infection in systemic models of Staphylococeus aureus. BB-3497 can be used for anti-bacterial infection research.

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BB-3497

BB-3497 Chemical Structure

CAS No. : 235784-88-0

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Description

BB-3497 is a potent, orally active and selective peptide deformylase (PDF) inhibitor. BB-3497 is highly selective for PDF (IC50 = 7 nM for E. coli PDF.Ni) over the other mammalian metalloenzymes (MMP-1/2/3/7 and enkephalinase). BB-3497 exhibits potent activity against gram-positive bacteria and some gram-negative pathogens. BB-3497 protects mice from infection in systemic models of Staphylococeus aureus. BB-3497 can be used for anti-bacterial infection research[1].

In Vitro

BB-3497 binds to PDF such that the oxygen atoms of its N-formyl-hydroxylamine group occupy the positions of the two Ni-bound water molecules observed in the PDF-Met-Ala-Ser product complex[1].
BB-3497 shows superior in vitro antibacterial activity against E. coli DH5α and E. coli BL21(DE3) strains harboring a control plasmid (pET24) or pET24-PDF, with MIC values of 4, 8, 32, and 128 μg/mL, but shows an MIC of >128 μg/mL against an E. coli formyltransferase mutant, confirming that its antibacterial action is mediated through PDF inhibition[1].
BB-3497 (4-8x MIC, 24 h) results in <1-log-unit decreases in viable counts of S. aureus and E. coli, conforming its antibacterial effect[1].
BB-3497 (2-4x MIC, 24 h) results in resistant mutants at frequencies of 1 x 10-7 for E. coli and 2 x 10-7 for S. aureus, with high-level resistance conferred by mutations in the fmt gene and low-level resistance exhibited by mutants having a wild-type def-fmt operon[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BB-3497 Related Antibodies
In Vivo

BB-3497 (3-100 mg/kg, p.o. or i.v., single dose at 1 h after bacterial challenge) protects mice from infection with S. aureus and methicillin-resistant S. aureus[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male ICR-derived mice intraperitoneally inoculated with S. aureus[1]
Dosage: 3, 6, 10, 30, 60 and 100 mg/kg
Administration: p.o. or i.v., single dose at 1 h after bacterial challenge
Result: Rescued mice from infection with an ED50 of 7 mg/kg (i.v.) and 8 mg/kg (p.o.), respectively.
Animal Model: Male ICR-derived mice intraperitoneally inoculated with methicillin-resistant S. aureus[1]
Dosage: 3, 6, 10, 30, 60 and 100 mg/kg
Administration: p.o., single dose at 1 h after bacterial challenge
Result: Showed an ED50 of 14 mg/kg.
Molecular Weight

329.44

Formula

C16H31N3O4
CAS No.
SMILES

CCCC[C@@H](C(N[C@@H](C(C)(C)C)C(N(C)C)=O)=O)CN(O)C=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
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References
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BB-3497 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BB-3497235784-88-0BB3497BB 3497AntibioticPDFStaphylococeus aureusE. coliformyltransferase mutantantibacterialICR-derived miceInhibitorinhibitorinhibit

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