AKT IN 1

AKT-IN-1 (AZD-26) is an allosteric AKT inhibitor (IC50: 1.04 μM).

ALK/PI3K/AKT-IN-1 (Compound 45) effectively inhibits the proliferation of cancer cell lines A549, H1975, and PC9, with IC50 values of 0.44, 0.83, and 1.51 μM, respectively. This compound enhances the expression of p21 and p27, and decreases the activity of CDK2 and p-Rb, causing cell cycle arrest at the G1 phase. It suppresses the ALK/PI3K/AKT signaling pathway, promotes mitochondrial membrane potential depolarization, and induces apoptosis in A549 cells. Furthermore, ALK/PI3K/AKT-IN-1 inhibits the formation and growth of A549 cell spheres.

STAT3/AKT-IN-1 is a dual inhibitor of the signal transducer and activator of transcription 3 (STAT3) and protein kinase B (AKT) signaling pathways, demonstrating anti-tumor activity and inducing apoptosis in SGC-7901 cells.

APN/AKT-IN-1 is a potent dual inhibitor of aminopeptidase N (APN) and protein kinase B (AKT), with IC50 values of 0.21 μM for APN and 0.27 μM for AKT inhibition. The compound effectively suppresses the phosphorylation of glycogen synthase kinase 3 beta (GSK3β), an intracellular substrate of AKT [1].

PI3K/AKT-IN-1 is a dual PI3K and AKT inhibitor with anti-cancer activity. It inhibits PI3Kγ, PI3Kδ, and AKT, suppressing the PI3K/AKT pathway and inducing caspase 3-dependent apoptosis, suitable for cancer research.

EGFR/Akt-IN-1 (compound 17) serves as an effective inhibitor of EGFR/Akt, exhibiting IC50 values of 12.89 μM and 10.88 μM in A549 cells, respectively. This compound induces cell cycle arrest at the S phase.

VEGFR-2/AKT-IN-1 (compound 17) is a dual inhibitor of VEGFR-2 and AKT with IC50 values of 0.164 μM and 0.452 μM, respectively. It exhibits antitumor activity.

Akt3 degrader 1 is a specific Akt3 degrader with anticancer and antiproliferative activity that inhibits tumor growth in mice.Akt3 degrader 1 is used in the study of non-small cell lung cancer and pancreatic cancer.

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/NF-κB/JNK-IN-1 (Compound 2i) is an inhibitor of the Akt, NF-κB, and JNK signaling pathways, demonstrating inhibition of nitric oxide production (IC50: 3.15 μM) and exhibiting anti-inflammatory effects.

PI3K/Akt/CREB activator 1 (AE-18) is a selective inducible nitric oxide synthase (iNOS) inhibitor that crosses the blood-brain barrier, reduces infarct size and restores blood supply deficits after ischemia-reperfusion in rats, and is used in studies of vascular dementia and Parkinson's disease.

Akt1&PKA-IN-1 is a potent dual inhibitor of Akt and PKA, with IC50 values of 0.11 μM for Akt, 0.03 μM for PKAα, and 9.8 μM for CDK2, demonstrating selective inhibition of cyclin-dependent kinase 2 (CDK2).

Akt/NF-κB/MAPK-IN-1 (compound 2m) is a potent, orally active inhibitor of NO with an IC50 of 7.70 μM and low toxicity, exhibiting anti-inflammatory effects by blocking the Akt/NF-κB and MAPK signaling pathways [1].

Tubulin/AKT1-IN-1 (Compound D1-1) is an inhibitor of tubulin polymerization and AKT pathway activation, suppressing proliferation and metastasis of H1975 cells while modestly inducing apoptosis. The compound is used in studying non-small-cell lung cancer (NSCLC) [1].

Akt/ROCK-IN-1 (B12) is a dual inhibitor of Akt and ROCK with IC50 values of 0.023 nM and 1.47 nM, respectively, and demonstrates antitumor efficacy against neuroblastoma [1].

Akt/mTOR-IN-1 (Compound 8r) is an inhibitor of the AKT/mTOR signaling pathway, exhibiting an IC50 of 0.8 µM and possessing anticancer activity. This compound decreases the expression of Caspase 3 while enhancing the expression of the autophagic protein Cyclin B1, thereby inducing autophagy and apoptosis. Akt/mTOR-IN-1 is applicable for research in the field of non-small cell lung cancer (NSCLC).

TAT-TCL1-Akt-in functions as an Akt inhibitor [1].

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.

Akt1-IN-8 (Compound JL18) is a potent AKT1 kinase inhibitor with oral bioavailability of 41% and an IC50 value of 8.8 nM. It exhibits significant antiproliferative effects against PC-3 prostate cancer cells, with an IC50 of 3.0 μM. Akt1-IN-8 also reduces phosphorylated GSK3β levels.

AKT1-IN-10 (Compound I-118) is a non-covalent allosteric inhibitor of AKT1, with an IC50 of less than 500 μM. It is orally bioavailable and can be used in cancer treatment.

AKT1-IN-11, a derivative of Podophyllotoxin, functions as a dual inhibitor of AKT1 and tubulin. It reduces phosphorylation levels of AKT kinase in tumor cells, disrupts cell proliferation, causes G2/M phase arrest, and induces apoptosis. Additionally, AKT1-IN-11 promotes tubulin depolymerization and is applicable in colorectal cancer research.

Akt3ligand-1 is an inhibitor of Akt3 with an IC50 of 0.1 nM and serves as a ligand for the PROTAC target protein (Akt3). It is utilized in the synthesis of PROTACAkt3Degrader-1.

PROTACAkt3Degrader-1 is an effective and selective PROTAC degrader targeting Akt3. It exhibits relatively weak antiproliferative activity across 36 cell lines. PROTACAkt3Degrader-1 is applicable in research on triple-negative breast cancer and melanoma.

AKT-I-1 is a selective and reversible inhibitor of Akt1.