akt1

Akt1-IN-1 is a potent and selective inhibitor of Akt1, demonstrating an IC50 of 18.79 nM in MIA PaCa-2 cells, indicating its high efficacy in inhibiting this specific kinase. Notably, it shows no significant teratogenicity, hepatotoxicity, or cardiotoxicity (No Observed Adverse Effect Level > 100 µM), making it a viable candidate for anticancer research.

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.

Tubulin/AKT1-IN-1 (Compound D1-1) serves as an inhibitor of both tubulin polymerization and AKT pathway activation, effectively suppressing proliferation and metastasis of H1975 cells while modestly inducing apoptosis. This compound is utilized in the study of non-small-cell lung cancer (NSCLC) [1].

Akt1&PKA-IN-1 is a potent dual inhibitor targeting Akt and PKA, exhibiting IC50 values of 0.11 μM for Akt, 0.03 μM for PKAα, and 9.8 μM for CDK2. Notably, it demonstrates selectivity for cyclin-dependent kinase 2 (CDK2).

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

Akt1&PKA-IN-2 ((R)-29), a compound with specificity towards PKB/AKT and notable selectivity for cyclin-dependent kinase 2 (CDK2), effectively inhibits AKT1, PKAa, and CDK2a with IC50 values of 0.007 µM, 0.01 µM, and 0.69 µM, respectively.

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

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

Akt/NF-κB/MAPK-IN-1 (compound 2m) serves as a potent, orally active inhibitor targeting NO with an IC50 of 7.70 μM and demonstrates low toxicity. This compound exerts anti-inflammatory effects by impeding the Akt/NF-κB and MAPK signaling pathways [1].

PI3K/Akt/CREB Activator 1 is a potent, orally active compound that acts as an activator for the PI3K/Akt/CREB pathway. It enhances neuronal proliferation, induces differentiation of Neuro-2a cells into neuron-like morphology, and accelerates axon-dendrite polarization in primary hippocampal neurons by upregulating brain-derived neurotrophic factor. This compound is utilized in vascular dementia (VaD) research.

PI3K/AKT-IN-1 is a potent, dual PI3K/AKT inhibitor that acts on PI3Kγ (IC50: 6.99 μM), PI3Kδ (IC50: 4.01 μM) and AKT (IC50: 3.36 μM). PI3K/AKT-IN-1 induces caspase 3-dependent apoptosis by inhibiting the PI3K/AKT pathway. caspase 3-dependent apoptosis and exhibited anticancer effects.

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

Akt/NF-κB/JNK-IN-1 (Compound 2i) is an inhibitor of Akt, NF-κB and JNK signalling pathways.Akt/NF-κB/JNK-IN-1 exhibits an inhibitory effect on nitric oxide production (IC50: 3.15 μM) and shows anti-inflammatory effects.

Ipatasertib (GDC-0068) (GDC-0068), a highly specific pan-Akt inhibitor, targets Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM, respectively.

MK-2206 dihydrochloride (MK-2206 2HCl) is a variant Akt inhibitor that inhibits Akt1, Akt2, and Akt3 (IC50=8/12/65 nM) with orally active, highly potent and selective potency. MK-2206 dihydrochloride exhibits antitumor activity.

Uprosertib (GSK2141795) (GSK2141795) is a selective, ATP-competitive, and orally bioavailable Akt inhibitor with IC50 of 180 nM, 328 nM, and 38 nM for Akt 1, 2 and 3, respectively. Phase 2.

Capivasertib (AZD5363) is a broad-spectrum AKT inhibitor with inhibitory activity against Akt1, Akt2, and Akt3 (IC50=3/7/7 nM) with oral activity. Capivasertib has antitumor activity for the treatment of breast cancer.

Oridonin (NSC-250682) is a diterpenoid isolated from Rabdosia rubescens with anti-tumor, anti-bacterial and anti-inflammatory effects. It acts as an inhibitor of AKT, with IC50s of 8.4 and 8.9 μM for AKT1 and AKT2.

Compound 1T-0216 is a blocker of AKT1-FAK interactions and reduces stimulation of FAK phosphorylation by extracellular stress in human SW620 colon cancer cells without affecting basal FAK phosphorylation.

A-674563 2HCl is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.

A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki: 11 nM for Akt1) [1]. It exhibits inhibitory activity against PKA and Cdk2 (IC50: 16/46 nM) but is 10- to >1, 800-fold selective for Akt1 versus additional kinases in th

MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities.

Compound 1T-0219 (SC) is a blocker of AKT1-FAK interaction reducing the stimulation of FAK phosphorylation in response to extracellular pressure in human SW620 colon cancer cells without affecting basal FAK phosphorylation.

Akt-I-1,2 is a selective inhibitor of Akt1 and Akt2.

Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective and ATP-competitive inhibitor of pan-Akt (IC50s: 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively).

3CAI is a potent and specific AKT1 and AKT2 inhibitor which showed significant inhibition of AKT in an in vitro kinase assay and suppressed expression of AKT direct downstream targets such as mTOR and GSK3β as well as induced growth inhibition and apoptosis in colon cancer cells.

MS170 is a highly effective and specific PROTAC AKT degrader compound that exhibits potent activity. It efficiently reduces the levels of total AKT (T-AKT) within cells, with a DC 50 value of 32 nM. Furthermore, MS170 demonstrates strong binding affinity towards AKT isoforms, specifically AKT1, AKT2, and AKT3, with respective dissociation constants (Kd) of 1.3 nM, 77 nM, and 6.5 nM.This compound is unstable in powder form and other related salt forms are recommended.

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

MK-2206 is an orally active, highly selective, metabotropic Akt inhibitor that acts on Akt1 (IC50: 8 nM), Akt2 (IC50: 12 nM) and Akt3 (IC50: 65 nM). Many breast cancer cell lines, PIK3CA mutants and PTEN-losing cell lines are sensitive to MK-2206, which has anti-cancer effects.

Afuresertib (GSK2110183) is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity.

GSK-690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.

AKT inhibitor VIII (AKTi-1/2) is a highly specific Akt1/2 inhibitor (IC50: 58/210 nM). The selectivity for Akt1 is higher about 36-fold than Akt3.

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].

INY-03-041, a potent and highly selective PROTAC-based pan-AKT degrader, inhibits AKT1, AKT2, and AKT3 with IC50s of 2.0 nM, 6.8 nM, and 3.5 nM, respectively. This compound consists of the ATP-competitive AKT inhibitor GDC-0068 conjugated to Lenalidomide.

Hu7691 free base is an orally active, potent and selective Akt inhibitor with anti-proliferative and neurogenic effects on a variety of neuroblastoma cell lines.Hu7691 free base inhibits Akt1, Akt2, and Akt3 and induces differentiation of neuroblastoma cells.

Vevorisertib (ARQ 751) is a highly effective oral compound that selectively inhibits pan-AKT serine/threonine kinases such as AKT1 (with an IC50 value of 0.55 nM), AKT2 (with an IC50 value of 0.81 nM), and AKT3 (with an IC50 value of 1.31 nM). This compound, either as a standalone treatment option or in combination with other anti-cancer agents, is ideally suited for conducting research on solid tumors characterized by PIK3CA/AKT/PTEN mutations[4].

NSC156529 downregulates AKT1 signaling. NSC156529 efficiently decreases the proliferation of human cancer cells in vitro, and substantially inhibits the growth of prostate tumor xenografts in vivo.

ALM301 is a highly specific, orally active AKT inhibitor that acts on AKT1 (IC50: 0.13 μM), AKT2 (IC50: 0.09 μM) and AKT3 (IC50: 2.75 μM). ALM301 inhibits AKT phosphorylation in vitro and has a regulatory effect on downstream signalling. ALM301 exhibits inhibitory effects on cancer cell proliferation and tumor growth.

DB07107 is a potent inhibitor of drug resistant T315I mutant Bcr-Abl tyrosine kinase and a potent Akt1 inhibitor (IC50: 360 nM).

A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.

AKT-IN-13 (compound 4b) is a potent inhibitor of Akt, acting on Akt1 (IC50: 1.6 nM), Akt2 (IC50: 2.4 nM) and Akt3 (IC50: 0.3 nM). AKT-IN-13 can be used in anticancer research.

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

AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1 / Akt2 / Akt3 and p70S6K / PKA kinase with IC 50 s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively. AT7867 dihydrochloride is able to induce pharmacodynamic changes and inhibit human tumor xenograft growth.

ETB067, an H-89 analog, acts as a PKA and AKT1 inhibitor with specificity on no longer inhibiting CAMK2B and neither affecting viability of mice nor causing any detectable tissue damage at the dose given.

MS98 is a highly effective and specific PROTAC AKT degrader compound that effectively targets and depletes total AKT (T-AKT) within cells, exhibiting a DC 50 value of 78 nM. This compound readily binds to AKT1, AKT2, and AKT3 with respective dissociation constants (Kd s) of 4 nM, 140 nM, and 8.1 nM.

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.

AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1/2/3, p70S6K, PKA, and ROCKI/II.

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].

AKT-IN-8 is a potent inhibitor of AKT, acting on AKT1 (IC50: 4.46 nM), AKT2 (IC50: 2.44 nM) and AKT3 (IC50: 9.47 nM).

24-Methylenecycloartanyl ferulate, a compound belonging to the γ-oryzanol family, demonstrates the ability to enhance parvin-beta expression within human breast cancer cells. Furthermore, it exhibits potential as an ATP-competitive Akt1 inhibitor, with an EC 50 value of 33.3 μM.