GMB-475 是一种靶向蛋白水解的嵌合体(PROTAC)，它以变构方式靶向 BCR-ABL1 蛋白并募集 the E3 ligase Von Hippel-Lindau (VHL)，从而导致泛素化并随后降解致癌融合蛋白 Information GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein. Targets BCR-ABL1 ; E3 ligase In vitro GMB-475 induces rapid proteasomal degradation and inhibition of downstream biomarkers, such as STAT5 in both human CML K562 cells and murine Ba/F3 cells expressing BCR-ABL1. GMB-475 inhibits the proliferation of certain clinically relevant BCR-ABL1 kinase domain point mutants and further sensitizes Ba/F3 BCR-ABL1 cells to inhibition by imatinib, while demonstrating no toxicity toward Ba/F3 parental cells. Cell Research(from reference) Cell lines：K562 cell line, Ba/F3 murine cell lines (Ba/F3 BCR-ABL1 cells, Ba/F3 parental cells) Concentrations：0.001-0.300 μM, 5 μM Incubation Time：3 days, 8 h