akt1-e17k

Miransertib (ARQ-092) is an orally bioavailable, selective, and potent allosteric Akt inhibitor.

Afuresertib hydrochloride is an inhibitor of Akt kinase (Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively)

AKT1-IN-9 (4) is a selective inhibitor of the AKT1(E17K) mutation, exhibiting EC50 values of 9 nM in LAPC4-CR cells and 995 nM in SkBr3 cells.

Tanerasertib is an AKT1 inhibitor that can specifically target the AKT1 E17K mutant. The EC₅₀ of tanerasertib ranges from 15 to 60 nM, making it applicable to cancer-related research.

Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally bioavailable, selective, and allosteric inhibitor of Akt with an IC50 of 2.7 nM, 14 nM, and 8.1 nM against Akt1, Akt2, and Akt3, respectively. It also shows significant potency against the AKT1-E17K mutant protein and holds promise for research on PI3K/AKT-driven tumors and Proteus syndrome. Additionally, Miransertib hydrochloride exhibits efficacy against Leishmania [1, 2].

Vevorisertib trihydrochloride (ARQ 751 trihydrochloride) is a selective and potent inhibitor of pan-AKT and AKT1-E17K mutations, inhibiting AKT1, AKT2 and AKT3. Vevorisertib trihydrochloride is used in the study of hepatocellular carcinoma and advanced solid tumours.

Akt1-IN-3 (Compd 7) serves as an AKT1 inhibitor, specifically targeting AKT1-E17K with an IC50 of less than 15 nM [1].

Akt1-IN-4 (Compound 62) serves as an inhibitor of AKT1-E17K, exhibiting potent activity with an IC50 value below 15 nM [1].