KPC-2-IN-1

Cat. No.: HY-150766: FAQs
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KPC-2-IN-1, boronic acid derivative, is a potent KPC-2 inhibitor with K_i 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.

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

KPC-2-IN-1 Chemical Structure

CAS No. : 2232877-85-7

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Description

IC₅₀ & Target

Ki: 0.032 μM (KPC-2)^[1].

In Vitro

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.

Cell Viability Assay^[1]

Cell Line:	E. coli BL21 DE3 (KPC-2 producing) and NCTC 10418
Concentration:	5, 50 μg/mL (combine with cefotaxime (CTX) or meropenem (MEM)).
Incubation Time:	16 h
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.

Molecular Weight

285.13

Formula

C₁₃H₁₂BN₃O₂S

CAS No.

2232877-85-7

SMILES

OB(C1=CC=CC(CN2N=NC(C3=CSC=C3)=C2)=C1)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

Handling Instructions (2659 KB)

References

[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]

KPC-2-IN-1 Related Classifications

Infection

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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:

KPC-2-IN-12232877-85-7Bacterialβ-lactamases inhibitorAMRboronic acid inhibitorsE. colicombination antibacterialInhibitorinhibitorinhibit

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