3,6-DICHLORO-BENZO[B]THIOPHENE-2-CARBOXYLIC ACID

3,6-dichloro-benzo[b]thiophene-2-Carboxylic acid is an inhibitor of myeloid cell leukemia 1 (Mcl-1) with a K_i value of 59 μM for binding of FITC-Mcl-1-BH2 peptide binding to Mcl-1. It has been used as a building block in the synthesis of inhibitors of Mcl-1, the toll-like receptor 3/double-stranded RNA (TLR3/dsRNA) complex, and D-amino acid oxidase (DAO).

1) Tso et al. (2014), Benzothiophene carboxylate derivatives as novel allosteric inhibitors of branched-chain α-ketoacid dehydrogenase kinase; J. Biol. Chem., 289 20583 2) Friberg et al. (2013), Discovery of potent myeloid cell leukemia (Mcl 1) inhibitors using fragment based methods and structure based design; J. Med. Chem. 56 15