MS143 [CAS 2376137-41-4]

MS143 is a potent PROTAC AKT degrader (DC50=46 nM and GI50=0.8 μM in PC3 cells). MS143 induces rapid and robust AKT degradation in a concentration- and time-dependent manner via hijacking the ubiquitin-proteasome system. MS143 can suppress cancer cell growth (Pink: AKT ligand ; Blue: E3 ligase ligand (HY-125845) ; Black: linker).

[2376137-41-4]

C59H81ClN12O6S

1121.87

O=C(N1[C@@H](C[C@H](C1)O)C(NCC2=CC=C(C3=C(N=CS3)C)C=C2)=O)[C@H](C(C)(C)C)NC(CCCCCCCCCCC(N(CC4)CCN4CC[C@@H](C5=CC=C(C=C5)Cl)NC(C6(CCN(CC6)C7=C8C(NC=C8)=NC=N7)N)=O)=O)=O

Akt; PROTACs

10 mM in DMSO

Room temperature