Enzyme inhibitors

CJ-12372 is an inhibitor of DNAgyrase produced by an unidentified fungus N 983-46. It has anti-Gram-positive bacteria, including Staphylococcus, Streptococcus, Enterococcus and Ciprofloxacin (Ciprofloxacin) drug-resistant bacteria activity, with MIC of 25-100 μg/mL.

MY 336-a is a beta-adrenergic receptor antagonist produced by Streptomyces gabonae KY-2234.

It is produced by the strain of Str. sp OH-5186. It can inhibit α,β-glucosidase and mannose glycosidase. It can inhibit the influenza virus and has weak anti-microbial effect.

It is produced by the strain of Str. sp OH-5186. It can inhibit α,β-glucosidase and mannose glycosidase. It does not inhibit the influenza virus, but it has weak anti-microbial effect.

It is produced by the strain of Str. sp OH-5186. It can inhibit α,β-glucosidase and mannose glycosidase. It does not inhibit the influenza virus, but it has weak anti-microbial effect.

It is produced by the strain of Str. sp OH-5186. It can inhibit α,β-glucosidase and mannose glycosidase. It does not inhibit the influenza virus, but it has weak anti-microbial effect.

Castanospermine is an inhibitor of all forms of α- and β-glucosidases, especially glucosidase l. It inhibits lysosomal and neutral α-glucosidases with Ki values of 0.1 and 10 μM, respectively. It also inhibits lysosomal and cytosolic β-glucosidases with Ki values of 7 and 40 μM, respectively. It inhibits HIV syncytium formation and replication. It catalyzes the cleavage of individual glucosyl residues from various glycoconjugates, including complex carbohydrates and glycoproteins. It is effective both in vitro and in vivo. It blocks N-linked glycosylation during post-translational modification of proteins, affecting protein trafficking and cell functions, including angiogenesis. It also interferes with viral replication and infection. It is a potent and specific inhibitor of mammalian and plant α-and β-D-glucosidases in vitro.

Novobiocin Sodium is a very potent bacterial DNA gyrase and human organic anion transporter with Ki of 14.87 ± 0.40 μM for hOAT1, 4.77 ± 1.12 μM for hOAT3 and 90.50 ± 7.50 μM for hOAT4.

Tunicamycin, a mixture of homologous nucleoside antibiotics, has been used to study the effect of N-linked glycosylation of human proton-coupled folate transporter (HsPCFT) in HeLa cells. Tunicamycin blocks the formation of N-glycosidic linkages by inhibiting the first step in glycoprotein synthesis.

Desethyl KBT-3022 is the main active metabolite of KBT-3022 which is a potent and long-lasting anti-platelet agent. Desethyl KBT-3022 (1-40 μM) inhibits the thrombin-induced aggregation of washed platelets in a concentration-dependent manner.

Padanamide A is a metabolite produced by marine Streptomyces species. It inhibits cysteine and methionine biosynthesis.

Tosufloxacin is a fluoroquinolone antibiotic with activity against Gram-positive and Gram-negative aerobic bacteria, anaerobic bacteria and Chlamydia trachomatis. It acts as an inhibitor of bacterial DNA gyrase and topoisomerase IV.

HC Toxin is a cell-permeable histone deacetylase (HDAC) inhibitor (IC50 = 30 nM) that inhibits HDACs in maize, Physarum and chicken. HC Toxin is metabolized from H. carbonum (now C. carbonum), and displays antifungal and antiproliferative effects.

Nalidixic acid sodium salt is an inhibitor of bacterial DNA polymerase (DNA gyrase) and avian myeloblastoma virus reverse transcriptase. It inhibits nucleic acid and protein synthesis in Saccharomyces cerevisiae. It is a naphthyridone antibiotic similar in structure and mechanism to quinolones.

Lipstatin, a potent inhibitor of the pancreas lipase, is reported to be useful in the treatment and prevention of obesity and related diseases. It is a natural product that was first isolated from Actinobacterium Streptomyces toxytricini.

Lesraurtinib, also known as CEP701, KT 5555, SP 924, is an orally bioavailable indolocarbazole derivative with antineoplastic properties. Lestaurtinib inhibits autophosphorylation of FMS-like tyrosine kinase 3 (FLT3), resulting in inhibition of FLT3 activity and induction of apoptosis in tumor cells that overexpress FLT3.

Caffeic acid phenethyl ester is a potent and specific inhibitor of NF-κB activation, and also displays antioxidant, immunomodulatory and antiinflammatory activities. It is the main active component of propolis. It has powerful antioxidant, anti-inflammatory and antibacterial activities, and can play a role in multiple targets of inflammation.

Kendomycin is an endothelin receptor antagonist and proteasome inhibitor. It induces apoptosis in lymphoma. It is a potent antibacterial agent against gram-positive and gram-negative bacteria, including MRSA strains.

LL Z1640-2 is a macrolide antibiotic produced by the strain of Deuteromyces sp. It is an irreversible and highly selective TAK 1 inhibitor and a member of the MAPKKK family that activates JNK/p38 and NF-κB pro-inflammatory signaling pathways. It effectively prevents inflammation in animal models. LL Z1640-2 is a covalent inhibitor that acts against the several protein kinases (e.g. ERK2 and TAK1) which possess a free cysteine at the gatekeeper-2 position.

CGP049090 is a novel inhibitor of Wnt/beta-catenin/lef-1 signaling inducing apoptosis in chronic lymphocytic leukemia cells in vitro and in vivo.