MS1-96

MS1-96 is an orally active PD-L1 (programmed death-ligand 1) degrader. MS1-96 effectively reduced PD-L1 protein levels across multiple colorectal cancer (CRC) cell lines. MS1-96 loses its ability to induce PD-L1 degradation upon HIP1R knockdown. MS1-96 directly binds to PD-L1 (KD = 2.58 μM) and enhances the interaction between HIP1R and PD-L1, thereby altering the intracellular trafficking of PD-L1 within clathrin-coated vesicles. MS1-96 induces abnormal N-glycosylation of PD-L1, destabilizing the protein and hastening its lysosome-mediated degradation. MS1-96 can be used for the study of colorectal cancer[1].

C25H29NO2

375.5

O=C(NC1=CC(CC[C@]2([H])[C@]3([H])CC[C@@]4(C)[C@@]2([H])CC[C@@H]4O)=C3C=C1)C5=CC=CC=C5

PD-1/PD-L1

Room temperature