LPZ-51 

LPZ-51 is a Vibrio β-lactam resistance sensor kinase (VbrK) inhibitor with a K_i value of 1.09 μM. LPZ-51 inhibits blaA gene expression at the transcriptional level by blocking the kinase activity of VbrK, reduces β-lactamase synthesis, and does not affect bacterial growth. LPZ-51 acts synergistically with β-lactam antibiotics. LPZ-51 decreases bacterial load, alleviates intestinal inflammation, and improves survival rate in zebrafish infection models. LPZ-51 can be used in studies related to Vibrio parahaemolyticus infection^[1].

LPZ-51 inhibits purified recombinant VbrKCA domain protein with a K_i value of 1.09 μM^[1].
LPZ-51 (1, 10 μg/mL) suppresses blaA transcription in V. parahemolyticus, achieving 77% inhibition at 1 μg/mL^[1].
LPZ-51 (0.5-50 μg/mL) dose-dependently reduces β-lactamase activity in V. parahemolyticus^[1].
LPZ-51 directly engages VbrK in V. parahemolyticus cells, increasing VbrK thermal stability by a ΔT_m of 4.1 °C^[1].
LPZ-51 (up to 128 μg/mL) synergizes with a broad range of β-lactam antibiotics (penicillins, cephalosporins, monobactam) against β-lactam-resistant V. parahemolyticus O3:K6 strain RIMD 2210633, with no effect on vancomycin resistance^[1].
LPZ-51 (up to 64 μg/mL) strongly synergizes with Carbenicillin against both SBL-producing and MBL-producing/carbapenem-resistant β-lactam-resistant V. parahemolyticus isolates, with FICI values ≤ 0.05 and ≤ 0.03, respectively^[1].
LPZ-51 (2 μg/mL; 15 consecutive passages) imposes a higher barrier to resistance development in V. parahemolyticus^[1].
LPZ-51 (1-10 μM) shows preliminary selectivity against a panel of 80 human kinases, with >50% inhibition of 7 kinases at 10 μM and sustained inhibition of PIM1, GAK, and NEK1 at 1 μM^[1].
LPZ-51 (up to 100 μg/mL) minimally inhibits HaCaT human keratinocyte cell viability^[1].

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

LPZ-51 (0.5, 5 mg/kg; i.p.; once) combined with Carbenicillin (HY-B0525) (5 mg/kg; i.p.; once) improves the survival rate of Vibrio parahaemolyticus-infected zebrafish^[1].
LPZ-51 (0.5-1 mg/kg; i.p.; once) combined with Carbenicillin (5 mg/kg; i.p.; once) improves survival, reduces intestinal bacterial burden, alleviates intestinal inflammation and tissue lesions, and downregulates IL-1β, IL-6 and TNF-α expression in Vibrio parahaemolyticus-challenged zebrafish^[1].

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

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• [1]. Jin B, et al. Fluorescence Polarization-Based High-Throughput Screening Enables Identification of Vibrio β-Lactam Resistance Sensor Kinase Inhibitors to Counteract Antibiotic Resistance. J Med Chem. 2026;69(9):10924-10948.