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[1][2].

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> Bacterial

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]. 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.

[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.

[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.