MK-2206 free base is an allosteric Akt inhibitor that is both potent and selective, administered orally, exhibiting IC50 values of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. It demonstrates sensitivity in various breast cancer cell lines, including those with PIK3CA mutations and those exhibiting PTEN loss, indicating its potential for anticancer activities [1] [2].

Lenalidomide-C9-aldehyde is a synthesized E3 ligase ligand-linker conjugate that incorporates the Lenalidomide based cereblon ligand and a linker. Lenalidomide-C9-aldehyde can be used in the synthesis of a series of PROTACs, such as INY-03-041. INY-03-041

Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM). It has potent and balanced activity.

AKT-IN-5 (Example 8) is a chemical compound known as an Akt inhibitor, specifically targeting Akt1 and Akt2. Its potency is reflected in IC50 values of 450 nM and 400 nM for Akt1 and Akt2, respectively [1].

Miransertib hydrochloride (ARQ-092 hydrochloride) is a powerful, orally bioavailable, selective, and allosteric inhibitor of Akt. It exhibits an inhibitory concentration (IC50) of 2.7 nM, 14 nM, and 8.1 nM against Akt1, Akt2, and Akt3, respectively. In addition to its Akt inhibitory activity, Miransertib hydrochloride also demonstrates significant potency as an inhibitor of the AKT1-E17K mutant protein. This compound shows promise in research related to PI3K/AKT-driven tumors and Proteus syndrome. Furthermore, Miransertib hydrochloride displays efficacy against Leishmania [1, 2].

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, and Akt3 with IC50 values of 2.0 nM, 6.8 nM, and 3.5 nM, respectively[1].