Enzyme inhibitors

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 19.63 ng/mL.

Topostatin is originally isolated from Thermomonos pora alba No. 1520. It has inhibitory effects on human tumor cells, and the IC50 of SNB-75 and SNB-78 were 0.4 μmol/L and 7 μmol/L, respectively.

It is produced by the strain of Str. dimorphogenes NR-320-OM7HB. Trestatin A has a strong inhibitory effect on pancreatic α-amylase, and also inhibits the α-amylase of Bacillus subtilis and Aspergillus oryzae.

It is produced by the strain of Str. dimorphogenes NR-320-OM7HB. Trestatin B has a strong inhibitory effect on pancreatic α-amylase, and also inhibits the α-amylase of Bacillus subtilis and Aspergillus oryzae.

It is produced by the strain of Str. dimorphogenes NR-320-OM7HB. Trestatin C has a strong inhibitory effect on pancreatic α-amylase, and also inhibits the α-amylase of Bacillus subtilis and Aspergillus oryzae.

Trichodion is originally isolated from Trichosporiella sp. It inhibits the expression of secretion alkaline phosphatase (SEAP) Reporter gene mediated by IFN-V with IC50 of 5-10 μg/mL, and it also inhibits the expression of human IFN-α promoter-driven Luciferase Reporter gene with IC50 of 2.5-5μg/mL.

It is produced by the strain of Kitasatospora sp. MK993-dF2. Tyropeptin A inhibited CHT-L and T-L activity of 20S proteasome with IC50 of 0.10 and 1.5 μg/mL, respectively.

It is produced by the strain of Kitasatospora sp. MK993-dF2. The inhibitory activity of B against CHT-L and T-L of 20S proteasome was half that of A.

Vanoxonin is produced by the strain of Saccharopolyspora hirsuta. It can inhibit thymidylate synthase (IC50 = 0.7μg/mL). And the MIC of the complex against L-1210 and Ehrlich ascites cancer cells was 25 μg/mL.

Bu-2743E is a leucine aminopeptidase (LAP) inhibitor originally isolated from Bacillus circulans J725-B93. It inhibits the LAP with an IC50 of 0.51 μg/mL.

It is produced by the strain of Gilmaniella sp. FA4459. The IC50 of beta-1,3-glucan synthase of Candida albicans A9540 was 0.25 μg/mL. BU-4794F had anti-yeast and Candida activities, and the MIC was 0.1-0.4 μg/mL.

It is produced by the strain of Streptomyces griseus subsp. cryophilus C-19393. C-19393 E5 has anti-gram-positive and anti-gram-negative bacteria activity and strong β-lactamase inhibition.

CJ-12371 is a DNA gyrase inhibitor originally isolated from N 983-46. It was resistant to Gram-positive bacteria, including Staphylococcus, Streptococcus, Enterococcus and Ciprofloxacin, with MIC of 25-100 μg/mL.

CJ-12373 is produced by the strain of Penicillum sp. CL22557. It inhibits the superhelix and relaxation mediated by DNA gyrase, not form cracking intermediates, also inhibits the relaxation mediated by eukaryotic topoisomerase II. And it also has anti-Gram-positive bacteria, including Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pyogenes and Streptococcus agalactiae, which are sensitive and resistant to ciprofloxacin.

It is originally isolated from CL15036. CJ-13981 inhibited SSASE in rat liver and human liver with IC50 of 4.4 μmol/L and 2.8 μmol/L respectively.

CJ-15183 is originally isolated from Aspergillus aculeatus CL38916. It has strong inhibitory activity against rat liver, human liver and Candida albicans SSase, and has antifungal activity against filamentous fungi and yeast-like fungi.

It is produced by the strain of Chloridium sp. CL48903. The IC50 of CJ-21164 inhibiting G6Pase in rat liver microsomes was 1.6 μmol/L.

It is produced by the strain of Streptomyces sp. CK-4416. CKD-711 strongly inhibited mammalian α-glucosidase activity, but weakly inhibited mammalian α-amylase from microorganism and mammal, which was similar to acarbose in vivo and in vitro.

CP-225917 inhibits Ras farnesyl transferase from the mouse brain and Squalene synthase.

CP-263114 inhibits Ras farnesyl transferase from the mouse brain and Squalene synthase.