(4S)-PROTAC SOS1 degrader-1

(4S)-PROTAC SOS1 degrader-1 is a stereoisomer of PROTAC SOS1 degrader-1 (HY-145737). PROTAC SOS1 degrader-1 (Compound 9d) is a degrader of SOS1 PROTAC, with a DC₅₀ of 98.4 nM and a K_d value of 44 nM. PROTAC SOS1 degrader-1 induces the formation of a ternary complex with SOS1 and the VCB E3 ubiquitin ligase complex, thereby promoting the ubiquitination and proteasomal degradation of SOS1. PROTAC SOS1 degrader-1 reduces KRAS-GTP levels, inhibits the phosphorylation of ERK in the RAS-RAF-MEK-ERK pathway, and suppresses the proliferation of cancer cells carrying KRAS mutations. PROTAC SOS1 degrader-1 inhibits tumor growth in mouse xenograft models. PROTAC SOS1 degrader-1 can be used for the research of KRAS-driven cancers.
(Pink: SOS1 ligand (HY-111671); Blue: VHL ligand (HY-184855); Black: linker).

• Data Sheet (277 KB)