Beta-lactamase Inhibitor

Cbz-Gly-Pro-Ala-O-cinnamyl (compound 25) is a small peptide targeting BACE-1 and AChE with the IC₅₀ values of 0.02 μM and 1 μM, respectively. Cbz-Gly-Pro-Ala-O-cinnamyl shows neuroprotective effect and can be used for study of Alzheimer’s disease.

β-Lactamase/Ferroptosis-IN-1 is a dual inhibitor of β-Lactamase and ferroptosis, β-Lactamase/Ferroptosis-IN-1 inhibits NDM-1 (metallo-β-lactamase, MBLs, IC₅₀ = 1.8 μM) and KPC-2 (serine-β-lactamase, SBLs, IC₅₀ = 2.6 μM). β-Lactamase/Ferroptosis-IN-1 exerts synergistic antibacterial effects with antibiotics against multidrug-resistant Gram-negative bacteria (MDR-GNB), and alleviates LPS (HY-D1056)-induced acute lung injury by inhibiting ferroptosis via upregulating FTH1 and GPX4 expression and reducing MDA levels. β-Lactamase/Ferroptosis-IN-1 can be used for the study of MDR-GNB infections and acute lung injury.

Pilabactam (ANT3310) is a broad-spectrum covalent Serine β-Lactamase inhibitor, with IC₅₀ values ranging from 1 nM to 175 nM (a panel of Serine β-Lactamase). Pilabactam potentiates activity of β-lactam antibiotics against Carbapenem-Resistant Enterobacterales (CRE) and Acinetobacter baumannii (CRAB). Pilabactam can be used in the research of bacterial infection.

Metallo-β-lactamase-IN-11 (compound 5f) is a Metallo-β-lactamases (MBLs) inhibitor, potent against bacterial metallophyllactamase CphA (IC₅₀=45 µM). Metallo-β-lactamase-IN-11 (10 µM) inhibits NDM-1 by 49% and AIM-1 by 61%. Metallo-β-lactamase-IN-11 can be used in the research of inhibiting antibiotic resistance.

β-Lactamase-IN-5 is a β-lactamase inhibitor extracted from patent WO2013149121A1, compound 720. β-Lactamase-IN-5 can be used for the research of bacterial infections.

β-Lactamase-IN-6 is a β-Lactamase inhibitor that shows high antibacetrial activity.

GT-055 free base (LCB18-055 free base) is a broad-spectrum β-lactamase inhibitor and penicillin-binding protein 2 (PBP2) inhibitor. GT-055 free base inactivates β-lactamase, protects GT-1 from hydrolysis, and binds tightly to PBP2, thereby inhibiting cell wall biosynthesis. GT-055 free base can be used for research on bacterial infections.

ANT2681 is a potent NDM inhibitor with a K_i value of 0.04 μM against NDM-1. ANT2681 also inhibits other MBLs, such as VIM-1 and IMP-1 with K_i values of 0.63 μM and 3.81 μM, respectively. ANT2681 can be used in combination with Meropenem (HY-13678) to inhibit infections caused by NDM-producing Enterobacteriaceae.

BLI-489 free base is a Beta-lactamase inhibitor. BLI-489 free base is an antibacterial adjuvant that significantly enhances the antibacterial efficacy of β-lactam antibiotics. BLI-489 free base blocks the hydrolytic activity of the enzyme by forming a stable intermediate in serine Beta-lactamase, or by coordinating with the binuclear Zn²⁺ through an oxygen atom in metallo-Beta-lactamase. BLI-489 free base can be used for research on bacterial infections.

β-Lactamase-IN-10 (Compound CB1) is a dual-metal β-lactamase (MLB) and serine β-lactamase (SLB) inhibitor. β-Lactamase-IN-10 exhibits antibacterial (antibacterial) activity against various drug-resistant bacteria. β-Lactamase-IN-10 can be used in the research of Gram-negative superbug infections.

YL6113 is a potent and selective dual inhibitor of metallo-β-lactamases (MBLs) and serine-β-lactamases (SBLs). YL6113 shows inhibitory effect to MBLs, such as NDm-1, VIM-2, IMP-1, with IC₅₀ values of 0.25, 27.16 and 3.55 μM. YL6113 shows inhibitory effect to SBLs, such as KPC-2, AmpC, OXA-48, with IC₅₀ values of 0.2, 34.1 and 1.31 μM. YL6113 enhances the antibacterial efficacy of Meropenem (HY-13678) against carbapenem-resistant Gram-negative bacteria. YL6113 can be used for the research of infection.

Metallo-β-lactamase-IN-9 (Compound 23) is a pan metallo-beta-lactamase (MBL) inhibitor with IC₅₀s of 35, 269 and 369 nM against NDM-1, VIM-1 and IMP-1, respectively.

NDM-1-IN-12 (Compound 10c) is an inhibitor of NDM-1 metallo-β-lactamase, with an IC₅₀ value of 9 nM. NDM-1-IN-12 effectively reverses bacterial resistance to β-lactam antibiotics and shows an additive effect when used in combination with antibiotics and SBL inhibitors. NDM-1-IN-12 can be used in the research of anti-multi-drug resistant bacteria.

Nacubactam (Standard) is the analytical standard of Nacubactam (HY-109008). This product is intended for research and analytical applications. Nacubactam (OP0595 free acid) is a potent non-β-lactam-β-lactamase inhibitor with activity against class A and C β-lactamases. Nacubactam acts as a penicillin binding protein (PBP) 2-active antibacterial, and gives β-lactamase-independent potentiation of β-lactams targeting other PBPs. Nacubactam potentiates the antimicrobial activities of Piperacillin (HY-B1923), Cefepime (HY-B0692), and Meropenem (HY-13678) against CTX-M-15-positive Escherichia coli and KPC-positive Klebsiella pneumoniae.

PhoPS is the photocaged inhibitor for β-lactamase. PhoPS is activated upon light irradiation, and active β-lactamase inhibitor Sulbactam (HY-B0334) is released. PhoPS inhibits the synthesis of bacterial cell wall and the formation of E. coli biofilm, exhibits antimicrobial activity.

Cefditoren Pivoxil-d₃ (Cefditoren pivoxyl-d₃) is deuterium labeled Cefditoren Pivoxil. Cefditoren Pivoxil (ME 1207) is a broad-spectrum, third-generation, oral cephalosporin antibacterial with enhanced stability against many common β lactamases. Cefditoren Pivoxil has activity against Gram-negative organisms and Gram-positive organisms. Cefditoren Pivoxil can be used in the research of infection diseases such as acute exacerbations of chronic bronchitis, community-acquired pneumonia (CAP), streptococcal pharyngitis/tonsillitis, or uncomplicated skin and skin structure infections.

Cefotaxime (sodium) (Standard) is the analytical standard of Cefotaxime (sodium). This product is intended for research and analytical applications. Cefotaxime (Cefotaxim) sodium, a β-lactamase stable cephalosporin and a third-generation cephalosporin antibiotic, possesses broad-spectrum antibiotic activity against numerous Gram-positive and Gram-negative bacteria.

ML121 is a selective and potent VIM-2 inhibitor with an IC₅₀ of 54 nM and a K_i of 148 nM. ML121 shows inactive in IMP-1 and TEM-1 beta-lactamase assays. ML121 can potentiate the antibiotic activity of Imipenem (HY-B1369A) in VIM-2 transformed E.coli.

Aspergillomarasmine A is a fungal secondary metabolite derived from natural amino acids, with inhibitory activity against metallo-β-lactamases. Aspergillomarasmine A selectively inhibits the metallo-β-lactamases NDM-1 and VIM-2, but shows weak inhibitory activity against IMP-7. Aspergillomarasmine A exhibits metal ion selectivity, which enables it to capture spontaneously dissociated Zn²⁺ from NDM-1, inducing the monozincation and inactivation of the enzyme; the inactivated metallo-β-lactamase undergoes protein degradation in the bacterial periplasm, thereby restoring the bacteriostatic efficacy of carbapenem antibiotics. Aspergillomarasmine A can be used in studies related to bacterial infections.

Cefonicid sodium (Standard) is the analytical standard of Cefonicid sodium (HY-B1300). This product is intended for research and analytical applications. Cefonicid sodium is a long-acting cephalosporin antibiotic. Cefonicid sodium also acts as a noncompetitive class I β-lactamase inhibitor with a K_i value of 0.8 μM. Cefonicid sodium exhibits broad-spectrum antimicrobial activity and is effective against a variety of Gram-positive and Gram-negative bacteria. Cefonicid sodium can be used for research on infections.