DASK1-VHL

DASK1-VHL is an orally active PROTAC degrader targeting ASK1. dASK1-VHL can effectively bind VHL and promote the selective degradation of ASK1. dASK1-VHL effectively reduces ASK1 protein levels, inhibits the activation of p38 MAPK, and reduces liver lipid content. dASK1-VHL provides new ideas for the study of Metabolic dysfunction-associated steatohepatitis (MASH) (Pink: ASK1 ligand 1 ; Blue: E3 ligand (S, R, S) -AHPC (HY-125845) ; Black: Linker, (S, R, S) -AHPC-CO-C2-PEG-NHCO-C2-COOH (HY-174861).

C48H57F2N11O8S

986.1

O=C(NC1=NC(C2=NN=CN2C(C)C)=CC=C1)C3=CC(NC(CCC(NCCOCCC(N[C@H](C(N4[C@@H](C[C@H](C4)O)C(NCC5=CC=C(C=C5)C6=C(N=CS6)C)=O)=O)C(C)(C)C)=O)=O)=O)=C(F)C=C3F

ASK1; p38 MAPK; PROTACs

Room temperature