2030241-59-7

TAM-16 is a potent and orally active polyketide synthase 13 (Pks13) inhibitor with an IC50 value of 0.32 μM. TAM-16 has promising activity against Mycobacterium tuberculosis. TAM-16 inhibits hERG cardiac ion channel[1][2].

TAM16 is a potent and selective inhibitor of the thioesterase activity of Mycobacterium tuberculosis polyketide synthase Pks13. TAM16 is a highly potent bactericidal agent th at exhibits activity against drug-susceptible and drug-resistant clinical isolates of M. tuberculosis. It is effective in both acute and chronic mouse TB models.

[1] Scullion P, et, al. Optimization of TAM16, a Benzofuran That Inhibits the Thioesterase Activity of Pks13; Evaluation toward a Preclinical Candidate for a Novel Antituberculosis Clinical Target. J Med Chem. 2022 Jan 13;65(1):409-423. DOI:10.1021/acs.jmedchem.1c01586
[2] Aggarwal A, et, al. Development of a Novel Lead that Targets M. tuberculosis Polyketide Synthase 13. Cell. 2017 Jul 13;170(2):249-259.e25. DOI:10.1016/j.cell.2017.06.025