KPC-2-IN-1
KPC-2-IN-1, boronic acid derivative, is a potent KPC-2 inhibitor with Ki of 0.032 μM. KPC-2-IN-1 enhances the activity of cefotaxime in KPC-2 expressing E. coli. KPC-2-IN-1 exhibits well tolerated in human HEK-293 cells, which can be used for the study of E. coli resistance to β-lactam antibiotics.
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- CAS No.: 2232877-85-7
- Formule: C13H12BN3O2S
- Masse moléculaire:285.13
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Ki: 0.032 μM (KPC-2)[1].
KPC-2-IN-1 (compound 2e) (50 μg/mL; 16 h) enhances the activity of CTX or MEM in KPC-2 expressing E. coli and (5 μg/mL; 16 h) also shows good combination activity of increasing CTX or MEM susceptibility to E. coli NCTC 10418[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:E. coli BL21 DE3 (KPC-2 producing) and NCTC 10418
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Concentration:5, 50 μg/mL (combine with cefotaxime (CTX) or meropenem (MEM)).
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Incubation Time:16 h
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Result:Decreased the MIC of CTX (16 μg/mL) as well as MEM (>64 μg/mL) to ≤ 0.03 or ≤0.06 μg/mL (~512 to >1000-fold increase in susceptibility) againsted E. coli BL21 DE3 and NCTC 10418.
Chemical Information
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CAS No. 2232877-85-7
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Masse moléculaire 285.13
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Formule C13H12BN3O2S
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SMILES
OB(C1=CC=CC(CN2N=NC(C3=CSC=C3)=C2)=C1)O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Zhou J, et al. Triazole-substituted phenylboronic acids as tunable lead inhibitors of KPC-2 antibiotic resistance. Eur J Med Chem. 2022 Jun 28;240:114571. [Content Brief]
[2]. Zhou J, et al. Boronic acid inhibitors of the class A β-lactamase KPC-2. Bioorg Med Chem. 2018 Jul 15;26(11):2921-2927. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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