protac ido1 degrader 1

PROTAC IDO1 Degrader-1, a pioneering compound, efficiently targets indoleamine 2,3-dioxygenase 1 (IDO1) for ubiquitination and degradation by recruiting IDO1 to the CRBN E3 ligase, thereby facilitating its entry into the ubiquitin-proteasome system (UPS) with a DC50 of 2.84 μM. This compound also moderately enhances the tumor-killing efficacy of HER2 CAR-T cells[1].

NU227326 is a PROTAC degrader of indoleamine 2,3-dioxygenase 1 (IDO1) with a DC50 value of 4.5 nM. It effectively degrades IDO1 in U87 and GBM43 cells, with DC50 values of 7.1 nM and 11.8 nM, respectively. NU227326 exhibits favorable pharmacokinetic properties, with a plasma half-life of 5.7 hours and a brain tissue half-life of 11.8 hours. (Pink: ligand for target protein IDO1 ligand-1; Black: linker; Blue: ligand for E3 ligase Cereblon).