em-12

2-(2,6-Dioxopiperidin-3-yl)phthalimidine (EM-12 (2-(2,6-Dioxopiperidin-3-yl)phthalimidine)) is a teratogenic Thalidomide analogue that is more active and significantly more stable against hydrolysis than Thalidomide, enhancing 1,2-dimethylhydrazine-induced rat colon adenocarcinomas [1] [2].

HsTX1, a 34-residue, C-terminally amidated peptide isolated from the scorpion Heterometrus spinnifer, features four disulfide bridges and acts as a potassium channel inhibitor. It exhibits an IC50 of 12 pM for Kv1.3, impeding T EM cell activation and diminishing inflammation in autoimmune conditions [1] [2] [3].

SIAIS039 is an orally active PROTAC specifically targeting c-ros oncogene 1 (ROS1), demonstrating DC50 values of 154.46 nM, 126.47 nM, and 143.69 nM in HCC78 cells, Ba F3 cells expressing CD74-ROS1 fusion, and Ba F3 cells expressing SDC4-ROS1 fusion, respectively. This compound inhibits proliferation, induces cell cycle arrest, and triggers apoptosis in ROS1-positive cells, while also inhibiting colony formation. In vivo, SIAIS039 exhibits potent anti-tumoral activity against ROS1-driven tumor growth. The composition of SIAIS039 includes the ALK inhibitor Brigatinib, linker EM-12, and VHL E3 ubiquitin ligase ligand.