Enzyme inhibitors

SNF-4794-12 is produced by Chaetomella sp. It inhibits α-glucosidase with IC50 of 0.11 μg/mL.

TA-3037A is a glutathione S-transferase inhibitor isolated from the fermentation broth of Streptomyces sp. TA-3037.

TAN-931 is a nonsteroidal aromatase inhibitor produced by Penicillium funiculosum No. 8974.

TAN-1496A is a diketopiperazine antibiotic isolated from the culture broth of Microsphaeropsis sp. FL-16144. It inhibited the relaxation of supercoiled pBR322 DNA by calf thymus topoisomerase I but did not affect the decatenation of kinetoplast DNA by calf thymus topoisomerase II at concentration up to 500 microM.

Sirodesmin A is a diketopiperazine antibiotic isolated from the culture broth of Microsphaeropsis sp. FL-16144. TAN-1496 inhibited the relaxation of supercoiled pBR322 DNA by calf thymus topoisomerase I but did not affect the decatenation of kinetoplast DNA by calf thymus topoisomerase II at concentration up to 500 microM.

TAN-1496C is a diketopiperazine antibiotic isolated from the culture broth of Microsphaeropsis sp. FL-16144. TAN-1496 inhibited the relaxation of supercoiled pBR322 DNA by calf thymus topoisomerase I but did not affect the decatenation of kinetoplast DNA by calf thymus topoisomerase II at concentration up to 500 microM.

TAN-1496D is a diketopiperazine antibiotic isolated from the culture broth of Microsphaeropsis sp. FL-16144. TAN-1496 inhibited the relaxation of supercoiled pBR322 DNA by calf thymus topoisomerase I but did not affect the decatenation of kinetoplast DNA by calf thymus topoisomerase II at concentration up to 500 microM.

TAN-1496E is a diketopiperazine antibiotic isolated from the culture broth of Microsphaeropsis sp. FL-16144. TAN-1496 inhibited the relaxation of supercoiled pBR322 DNA by calf thymus topoisomerase I but did not affect the decatenation of kinetoplast DNA by calf thymus topoisomerase II at concentration up to 500 microM.

TAN-1518A is a naphthacenecarboxamide antibiotic isolated from a culture broth of Streptomyces sp. AL-16012. It inhibits DNA topoisomerase I.

TAN-1518B is a naphthacenecarboxamide antibiotic isolated from a culture broth of Streptomyces sp. AL-16012. It inhibits DNA topoisomerase I.

TAN-1813 is a Ras-farnesyltransferase inhibitor produced by a fungus strain, FL-41510. It inhibited rat brain farnesyltransferase and geranylgeranyltransferase I activity with IC50 values of 23 and 47 μg/mL, respectively. It also inhibited the proliferation of various human cancer cells.

TMC-2A is a dipeptidyl peptidase IV (DPIV) inhibitor isolated from the fermentation broth of Aspergillus oryzae A374. It inhibited rat kidney DPIV with IC50 value of 8.1 μmol/L.

TMC-2B is a dipeptidyl peptidase IV (DPIV) inhibitor isolated from the fermentation broth of Aspergillus oryzae A374. It inhibited rat kidney DPIV with IC50 value of 8.1 μmol/L.

TMC-2C is a dipeptidyl peptidase IV (DPIV) inhibitor isolated from the fermentation broth of Aspergillus oryzae A374. It inhibited rat kidney DPIV with IC50 value of 8.1 μmol/L.

TMC-66 is a selective endothelin conversion enzyme (ECE) inhibitor isolated from the culture broth of Streptomyces sp. A5008.

TMC-86A is a 20S proteasome inhibitor isolated from the fermentation broth of Streptomyces sp. A5008. It inhibited the chymotrypsin-like and peptidylglutamyl-peptide hydrolyzing activities of 20S proteasome with IC50 values of 5.1 and 3.7 μmol/L, respectively.

TMC-86B is a 20S proteasome inhibitor isolated from the fermentation broth of Streptomyces sp. A5008. It inhibited the chymotrypsin-like and peptidylglutamyl-peptide hydrolyzing activities of 20S proteasome with IC50 values of 1.1 and 31 μmol/L, respectively.

TMC-89A is a 20S proteasome inhibitor produced by streptomyces sp. TC 1087. It inhibited chymotrypsin-like (ChT-L), trypsin-like (T-L), and peptidylglutamyl-peptide hydrolyzing (PGPH) activities of 20S proteasome with IC50 of 1.1, 0.39 and 7.2 μmol/L, respectively.

TMC-89B is a 20S proteasome inhibitor produced by streptomyces sp. TC 1087. It inhibited chymotrypsin-like (ChT-L), trypsin-like (T-L), and peptidylglutamyl-peptide hydrolyzing (PGPH) activities of 20S proteasome with IC50 of 1.1, 0.51 and 7.1 μmol/L, respectively.

TMC-95A 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 with IC50 values of 5.4nM, 200nM, and 60nM, respectively.