Enzyme inhibitors

TMC-95B is a proteasome inhibitor produced by Apiospora montagnei Sacc. TC 1093. It inhibited the chymotrypsin-like (ChT-L), trypsin-like (T-L), and peptidylglutamyl-peptide hydrolyzing (PGPH) activities of 20S proteasome to the same extent as TMC-95A.

TMC-95C is a proteasome inhibitor produced by Apiospora montagnei Sacc. TC 1093.

TMC-95D is a proteasome inhibitor produced by Apiospora montagnei Sacc. TC 1093.

TMC-96 is a proteasome inhibitor produced by Saccharothrix sp. TC 1094. It inhibited the chymotrypsin-like and peptidylglutamyl-peptide hydrolyzing activities of 20S proteasome with IC50 values of 2.9 and 3.5 μmol/L, respectively.

TMC-256A1 is an inhibitor of IL-4 signal transduction isolated from the fermentation broth of Aspergillus niger var niger TC 1629. It inhibited the IL-4 driven luciferase activity with IC50 values of 25 μmol/L.

TMC-256C1 is an inhibitor of IL-4 signal transduction isolated from the fermentation broth of Aspergillus niger var niger TC 1629. It inhibited the IL-4 driven luciferase activity with IC50 values of 1.7 μmol/L.

TMC-260 is an inhibitor of IL-4 signal transduction produced by Acremonium kiliense Grütz TC 1703. It inhibited the IL-4 driven luciferase activity with IC50 values of 9 μmol/L.

TMC-264 is a STAT6 activation inhibitor produced by Phoma sp. TC 1674. It suppressed expression of IL-4 driven luciferase and germline Cepsilon mRNA with IC50 values of 0.3 and 0.4 μmol/L, respectively, and inhibited tyrosine phosphorylation of STAT6 with an IC50 value of 1.6 μmol/L.

Pyripyropene A is a powerful acyl-CoA: cholesterol acyltransferase 2 (ACAT2) inhibitor produced by the fungus Aspergillus fumigatus FO 1289. It inhibits acyl-CoA: cholesterol acyltransferase with an IC50 of 58 nmol/L.

A minor component of the oligomycin complex isolated from selected strains of streptomyces; an inhibitor of mitochondrial F1F0-atpas; used as an eukaryotic ATP synthase inhibitor, induces apoptosis.

A minor component of the oligomycin complex isolated from selected strains of streptomyces; an inhibitor of mitochondrial F1F0-atpas; used as an eukaryotic ATP synthase inhibitor, induces apoptosis.

The dominant analogue of a family of quinolone metabolites produced by penicillium citrinum; inhibit acetylcholinesterase and TNF production.

Rifaximin EP Impurity C is an antibacterial drug which functions by inhibiting bacterial RNA polymerase (RNAP), is an impurity of Rifaximin. It also has anti-gram-positive bacterial and mycobacterium activities.

β-Rubromycin is a quinone antibiotic originally isolated from Streptomyces. It is effective against Gram-positive bacteria. It inhibits the growth of HMO2, KATO-III, and MCF-7 cells with GI50 values of 0.5, 0.84, and <0.1 μM, respectively. β-rubromycin also inhibits HIV-1 reverse transcriptase activity.

An intense yellow pigment produced by some species of penicillium, aspergillus and the fungal symbiotants of some lichens; shows antibacterial and insecticidal activity; an inhibitor of RNA Polymerase and Rnase.

It is produced by the strain of Bacillus laterosporus BMI 156-14F1. It inhibits aminopeptidase M with IC50 of 0.2 μg/mL. It has no antimicrobial effects (100 μg/mL).

It is produced by the strain of Str. sp. K93-0711. It is an interleukin-6 inhibitor. It inhibits IL-6-dependent MH-60 cells and has no inhibitory effect on IL-6-independent MH-60 cells. In the presence of 0.1 U/mL IL-6, it inhibits IL-6-dependent MH-60 cells with IC50 of 8 μmol/L. It has no antimicrobial effect.

It is produced by the strain of Phoma sp. BAUA 2861 and Penicillum sp. BAUA 4206. Topopyrone A selectively inhibits topoisomerase I with the IC50 of 1.22 ng/mL. It also has anti-Gram-positive bacteria activity.

It is produced by the strain of Phoma sp. BAUA 2861 and Penicillum sp. BAUA 4206. Topopyrone B selectively inhibits topoisomerase I with the IC50 of 0.15 ng/mL. It also has anti-Gram-positive bacteria activity and it has a strong inhibitory effect on herpes virus, especially varicella zoster virus (VZV).

It is produced by the strain of Phoma sp. BAUA 2861 and Penicillum sp. BAUA 4206. Topopyrone C selectively inhibits topoisomerase I with the IC50 of 4.88 ng/mL. It also has anti-Gram-positive bacteria activity.