| Bioactivity | 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]. |
| Target | Ki: 0.032 μM (KPC-2). |
| Invitro | 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: |
| Name | KPC-2-IN-1 |
| CAS | 2232877-85-7 |
| Formula | C13H12BN3O2S |
| Molar Mass | 285.13 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |