DKM 2-93

DKM 2-93 is a cysteine-reactive covalent inhibitor of ubiquitin-like modifier activating enzyme 5 (UBA5; IC₅₀ = 450 µM).¹ It decreases survival of PaCa-2 pancreatic cancer cells without affecting human pancreatic ductal epithelial cells (HPDEs) when used at a concentration of 50 µM. In vivo, DKM 2-93 (50 mg/kg per day) reduces tumor volume without reducing body weight in a PaCa-2 pancreatic cancer mouse xenograft model. It has also been used as an intermediate in the synthesis of topoisomerase I inhibitors and compounds active against M. tuberculosis.^2,3

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1. Roberts, A.M., Miyamoto, D.K., Huffman, T.R., et al. Chemoproteomic screening of covalent ligands reveals UBA5 as a novel pancreatic cancer target. ACS Chem. Biol. 12(4), 899-904 (2017).

2. Kadagathur, M., Patra, S., Devabattula, G., et al. Design, synthesis of DNA-interactive 4-thiazolidinone-based indolo-/pyrroloazepinone conjugates as potential cytotoxic and topoisomerase I inhibitors. Eur. J. Med. Chem. 238, 114465 (2022).

3. Lee, R.E., Protopopova, M., Crooks, E., et al. Combinatorial lead optimization of [1,2]-diamines based on ethambutol as potential antituberculosis preclinical candidates. J. Comb. Chem. 5(2), 172-187 (2003).