9-Decyn-1-ol is an alkyl ether-based PROTAC linker suitable for synthesizing PROTACs. It serves as a conjugation agent to combine GDC-0068 and Lenalidomide, resulting in the formation of INY-03-041. INY-03-041 is a potent and highly selective pan-Akt degrader that operates through the PROTAC mechanism. It effectively inhibits Akt1, Akt2, andAkt3 with IC50 values of 2.0 nM, 6.8 nM, and 3.5 nM, respectively[1].
Lenalidomide-C9-aldehyde is a synthesized E3 ligase ligand-linker conjugate that incorporates the Lenalidomide based cereblon ligandand a linker. Lenalidomide-C9-aldehyde can be used in the synthesis of a series of PROTACs, such as INY-03-041. INY-03-041
AKT-IN-5 (Example 8) is a chemical compound known as an Aktinhibitor, specifically targeting Akt1 andAkt2. Its potency is reflected in IC50 values of 450 nM and 400 nM for Akt1 andAkt2, respectively [1].