Beta-lactamase Inhibitor

Avibactam sodium (NXL-104) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC₅₀s of 8 nM and 5 nM, respectively.

Ceftazidime (GR20263), an antibiotic, has a broad spectrum activity against Gram-positive and Gram-negative aerobic bacteria. Ceftazidime is also active against Enterobacteriaceae (including β-lactamase-positive strains) and is resistant to hydrolysis by most β-lactamases.

Tubastatin A is a potent and selective HDAC6 inhibitor with an IC₅₀ of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).

Vaborbactam (RPX7009) is a cyclic boronic acid pharmacophore β-lactamase inhibitor.

Clavulanic acid is a naturally occurring powerful bacterial β-lactamases inhibitor for research of infections caused by bacteria, including infections of the ears. Clavulanic acid is active against a wide spectrum of gram-positive and gram-negative bacterias.

Amoxicillin-clavulanate potassium is an orally active antibacterial composition consisting of Amoxicillin (HY-B0467A) and the β-lactamase inhibitor Clavulanate potassium (HY-A0256A). In Amoxicillin-clavulanate potassium, Amoxicillin binds to bacterial penicillin-binding proteins to inhibit peptidoglycan synthesis and exert a bactericidal effect; Clavulanate potassium protects Amoxicillin from hydrolysis by β-lactamase. Amoxicillin-clavulanate potassium exhibits antibacterial activity against β-lactamase-producing Gram-positive and Gram-negative bacteria. Amoxicillin-clavulanate potassium dose-dependently interferes with the function of ameloblasts at the maturation stage, disrupts the enamel mineralization process, and induces enamel developmental defects. Amoxicillin-clavulanate potassium can be used in research related to bacterial infections.

Augpenin (Ticarcillin-clavulanic acid mixt.; BRL28500) is a compound β-lactam antibacterial mixture of Ticarcillin (HY-139805) and Clavulanic acid (HY-A0256) in a 15:1 ratio. Ticarcillin in Augpenin acts on bacterial penicillin-binding proteins, while Clavulanic acid acts as an irreversible β-lactamase inhibitor that protects Ticarcillin from hydrolysis and restores its inhibitory activity against resistant strains. Augpenin significantly reduces the bacterial load of Legionella pneumophila in lung tissue of Cyclophosphamide (HY-17420)-induced neutropenic young rats. Augpenin can be used in research related to bacterial infections.

Cefpiramide sodium (SM-1652) is a semisynthetic cephalosporin with broad-spectrum antibacterial activity. Cefpiramide sodium shows strong antibacterial effect on both gram-positive bacteria and gram-negative bacteria. Cefpiramide sodium is moderately susceptible to β-lactamase.

Relebactam is a diazabicyclooctane inhibitor with activity against a wide spectrum of β-lactamases, including class A (extended-spectrum β-lactamases and KPC) and class C (AmpC) enzymes. Relebactam shows antibacterial activity.

Tubacin is a potent and selective inhibitor of HDAC6, with an IC₅₀ value of 4 nM and approximately 350-fold selectivity over HDAC1. Tubacin also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2).

Taniborbactam hydrochloride (VNRX-5133 hydrochloride) is a reversible and selective boronic acid-containing pan-spectrum β-lactamase inhibitor with IC₅₀s of 8-530 nM. Taniborbactam hydrochloride has IC₅₀s of 30 nM, 32 nM, 42 nM, 20 nM for KPC-2, AmpC, OXA-48, and VIM-2. Taniborbactam hydrochloride is against Gram-negative bacteria.

Cefotaxime, a β-lactamase stable cephalosporin and a third-generation cephalosporin antibiotic, possesses broad-spectrum antibiotic activity against numerous Gram-positive and Gram-negative bacteria.

Zidebactam (WCK-5107) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC₅₀ of 0.26 μg/mL.

Tubastatin A Hydrochloride (Tubastatin A HCl) is a potent and selective HDAC6 inhibitor with IC₅₀ of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A Hydrochloride also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).

Eravacycline dihydrochloride (TP-434 dihydrochloride) is a potent and broad-spectrum antibacterial agent.

Penicillin G sodium salt is a typical β-lactam antibiotic.

Tazobactam (CL-298741) is a potent β-lactamases inhibitor and penicillin antibiotic. Tazobactam has antibacterial activity. Tazobactam can be used for pneumonia research.

Piperacillin is a semisynthetic broad-spectrum β-lactam antibiotic which exhibits potent bactericidal activity against Gram-negative bacteria as well as select Gram-positive strains through penicillin-binding proteins. Piperacillin is most commonly used in combination with the β-lactamase inhibitor Tazobactam.

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.

Pracinostat is a potent histone deacetylase (HDAC) inhibitor, with IC₅₀s of 40-140 nM, used for cancer research. Pracinostat also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) hydrolase activity with an EC₅₀ below 10 nM.