DKM 2-93

DKM 2-93 (CAS No.: 65836-72-8) is a small-molecule, cysteine-reactive covalent inhibitor of ubiquitin-like modifier activating enzyme 5 (UBA5), a key component of the UFMylation pathway implicated in protein homeostasis and cancer cell survival, and is primarily utilized as a chemical probe in oncology-focused drug discovery and mechanistic studies. It exhibits relatively selective inhibition of UBA5 with activity in the mid-micromolar range, and has been shown to reduce viability of pancreatic cancer cell lines, including PaCa-2 and Panc-1 cells, while sparing nonmalignant human pancreatic ductal epithelial cells under comparable conditions, indicating a degree of tumor-selective cytotoxicity. Functional studies suggest that disruption of UBA5-mediated UFMylation contributes to impaired cancer cell survival and tumor progression. In vivo, administration in pancreatic cancer xenograft mouse models leads to a marked reduction in tumor growth without significant effects on body weight or overt toxicity, supporting its utility as a tool compound for evaluating UBA5 as a therapeutic target. In experimental settings, DKM 2-93 is commonly applied in cell-based assays and animal models to interrogate ubiquitin-like modification pathways, with concentrations or dosing regimens adjusted according to specific study designs, and it has also been employed as a synthetic intermediate in broader medicinal chemistry efforts.