2. Anti-infection Cell Cycle/DNA Damage
  3. Antibiotic Bacterial Topoisomerase DNA/RNA Synthesis
  4. GC-072

GC-072 is an orally active, 4-oxoquinolizine antibiotic that selectively inhibits bacterial DNA gyrase and Topo IV enzymes. GC-072 does not inhibit human topoisomerases I and II. GC-072 demonstrates strong antimicrobial activity against various bacterial strains, including Gram-positive, Gram-negative, and resistant bacteria. GC-072 also exhibits bactericidal activity against Burkholderia pseudomallei both extracellularly and intracellularly, leading to dose-dependent survival in mice exposed to lethal inhalational models of B. pseudomallei infection. GC-072 can be used for the research of melioidosis.

For research use only. We do not sell to patients.

GC-072

GC-072 Chemical Structure

CAS No. : 1371629-36-5

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GC-072 Related Antibodies

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Topoisomerase Topo I Topo II DNA gyrase

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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Description

GC-072 is an orally active, 4-oxoquinolizine antibiotic that selectively inhibits bacterial DNA gyrase and Topo IV enzymes. GC-072 does not inhibit human topoisomerases I and II. GC-072 demonstrates strong antimicrobial activity against various bacterial strains, including Gram-positive, Gram-negative, and resistant bacteria. GC-072 also exhibits bactericidal activity against Burkholderia pseudomallei both extracellularly and intracellularly, leading to dose-dependent survival in mice exposed to lethal inhalational models of B. pseudomallei infection. GC-072 can be used for the research of melioidosis[1].

IC50 & Target[1]

DNA Gyrase

2 μM (IC50, S. aureus)

TOPO IV

4-30 μM (IC50, S. aureus)

DNA Gyrase

0.18-1.5 μM (IC50, E.coli)

TOPO IV

4.22-8.45 μM (IC50, E.coli)

In Vitro

GC-072 (0.25 μg/mL, 2.5 μg/mL; 0, 1, 5, 24 hours) effectively inhibits the growth of intracellular B. pseudomallei in murine macrophage cells in a rapid time- and dose-dependent manner, with no viable bacteria detectable after 24 hours at either concentration[1].
GC-072 inhibits both E.coli and S. aureus gyrase and Topo IV. The IC50 values of 2 μM, 0.18-1.50 μM, 4-30 μM, and 4.22-8.45 μM for S. aureus gyrase, E.coli gyrase, S. aureus Topo IV, and E.coli Topo IV, respectively[1].
GC-072 demonstrates good activity against B. pseudomallei, with an MIC90 of 0.25 μg/mL and a range of ≤0.008 to 1 μg/mL[1].
The MIC90s of GC-072 against B. anthracis, Y. pestis, F. tularensis, and B. mallei are 0.002 μg/mL, 0.015 μg/mL, ≤0.0005 μg/mL, and 0.12 μg/mL, respectively[1].
GC-072 is fully active against the panel of drug-resistant B. pseudomallei strains tested (i.e., Ceftazidime (HY-B0593)-, Clavulanate (HY-A0256A)- and Trimethoprim (HY-B0510)-resistant strains)[1].

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

GC-072 Related Antibodies
In Vivo

GC-072 (1-30 mg/kg; oral (gavage); q8h; 14 days) and GC-072 (37.5-150 mg/kg; oral (gavage); q8h; 14 days) improve survival in pneumonic model of melioidosis (infected with B. pseudomallei strain 1026b via aerosol challenge)[1].

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

Animal Model: BALB/c (Female, 6 to 8 weeks, 19.75 g) (infected with B. pseudomallei strain 1026b via aerosol challenge)[1]
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration: oral (gavage); 1, 3, 10, 30 mg/kg; q8h; 14 days
Result: When treatment was initiated 8 h postchallenge, 0%, 0%, 70%, and 90% survival was observed in mice administered 1, 3, 10, and 30 mg/kg, respectively.
When treatment was initiated 16 h postchallenge, 50% and 100% survival was observed in the 10 and 30 mg/kg groups, respectively.
Animal Model: BALB/c (Female, 6 to 8 weeks, 19.75 g) (infected with B. pseudomallei strain 1026b via aerosol challenge)[1]
Dosage: 37.5 mg/kg, 75 mg/kg, 150 mg/kg
Administration: oral (gavage); 37.5, 75, 150 mg/kg; q8h; 14 days
Result: When initiated 8 h postexposure, mice in the 37.5-, 75-, and 150-mg/kg treatment groups demonstrated 90%, 90%, and 80% survival, respectively.
In the 24-h treatment initiation groups, overall survival was low. However, each dose provided a significant survival advantage compared to vehicle control.
Molecular Weight

370.35

Formula

C20H16F2N2O3
CAS No.
SMILES

O=C(C1=CC(C2CC2)=C3C(C)=C(C4=C(F)C=C(N)C(F)=C4)C=CN3C1=O)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GC-072 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:

GC-0721371629-36-5GC072GC 072AntibioticBacterialTopoisomeraseDNA/RNA Synthesisbacterial topoisomerasesreduced development of resistancefirst-lineoral treatmentdrug-resistant strainsmelioidosisbactericidallethal inhalational models4-oxoquinolizine antibioticoral administrationpotentextra- and intracellularlyselective inhibitory activityrapid killingdose-dependent survivalintragastricallyInhibitorinhibitorinhibit

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