2. Signaling Pathways
  3. PI3K/Akt/mTOR
  4. Akt

Akt

PKB; Protein kinase B

Akt

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Akt/PKB (Protein kinase B), a serine/threonine protein kinase with antiapoptotic activity, is one of the major downstream targets of PtdIns(3,4,5)P3 signaling pathway. It contains a pleckstrin homology domain (PH domain) that specifically binds PtdIns(3,4,5)P3 on the plasma membrane. Akt phosphorylation and activation are directly determined by the level of PtdIns(3,4,5)P3 on the plasma membrane, which is regulated by PI3K.

Akt consists of three isoforms: PKBα/Akt1, PKBβ/Akt2 and PKBγ/Akt3. Akt isoforms have an N-terminal PH (pleckstrin homology) domain and a kinase domain, which are separated by a 39-amino-acid hinge region. Catalytically active Akt regulates the function of numerous substrates involved in cell survival, growth, proliferation, metabolism and protein synthesis.

Akt is a crucial mediator of cell survival and its deactivation is implicated in various stress-induced pathological cell death and degenerative diseases.

Akt Isoform Specific Products:

Akt Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-157133
    TAS0612
    		Inhibitor 98.83%
    TAS0612 is the orally active inhibitor of RSK、AKT and S6K. TAS0612 has antitumor activity.
    TAS0612
  • HY-18296
    AKT-IN-1
    		Inhibitor 98.41%
    AKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM.
    AKT-IN-1
  • HY-N8307
    Syringaresinol
    		Inhibitor 99.15%
    Syringaresinol is a lignan-type phytochemical with anti-inflammatory activities. Syringaresinol inhibits the NF-κB and AKT signaling pathway in IL-1β-activated mouse chondrocytes. Syringaresinol increases phosphorylation of AMPK, eNOS, and intracellular Ca2+ levels in HUVECs. Syringaresinol attenuates osteoarthritis progression in mice with Destabilization of the Medial Meniscus (DMM)-induced osteoarthritis. Syringaresinol can be used for the study of osteoarthritis (OA).
    Syringaresinol
  • HY-121537
    CAY10404
    		Inhibitor 99.69%
    CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM and a selectivity index (SI; COX-1 IC50/COX-2 IC50) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities.
    CAY10404
  • HY-N6951
    Guaiazulene
    		Inhibitor 99.26%
    Guaiazulene is a bicyclic sesquiterpene that can cross the blood-brain barrier. Guaiazulene exhibits various biological activities such as anti-inflammatory, antioxidant, hepatoprotective, antibacterial, and anti-tumor properties. Guaiazulene is also commonly used as a colorant in cosmetics. Guaiazulene shows in vitro cytotoxicity to rat neuronal cells and N2a neuroblastoma cells at high concentrations.
    Guaiazulene
  • HY-N1505
    Loureirin A
    		Inhibitor 99.96%
    Loureirin A is a flavonoid extracted from Dragon's Blood, can inhibit Akt phosphorylation, and has antiplatelet activity.
    Loureirin A
  • HY-110077
    API-1
    		Inhibitor 99.62%
    API-1 is a potent selective Akt/PKB inhibitor that reduces the level of phosphorylated Akt (IC50 = 0.8 μM). API-1 binds to the PH domain and inhibits Akt membrane translocation. API-1 induces c-FLIP degradation. API-1 reduces cell proliferation and induces apoptosis. API-1 decreases tumor growth in mouse xenograft model.
    API-1
  • HY-124295
    Imofinostat
    		Inhibitor 99.40%
    Imofinostat (ABT-301; MPT0E028) is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. Imofinostat has a weak inhibitory effect on HDAC8 (IC50 of 2.5 ​​μM), but no inhibitory effect on HDAC4 (IC50>10 μM). Imofinostat reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. Imofinostat has a broad-spectrum antitumor activity, including colorectal cancer, B-cell lymphoma, non-small cell lung carcinoma (NSCLC), and pancreatic cancer, while also showing therapeutic potential in non-tumor diseases like emphysema and pulmonary fibrosis.
    Imofinostat
  • HY-B0194S
    Tizanidine-d4
    		Inhibitor 99.93%
    Tizanidine-d4 is the deuterium labeled Tizanidine (HY-B0194). Tizanidine, a skeletal muscle relaxant, is an orally effective central α2-adrenoceptor agonist (IC50 = 6.9 nmol). Tizanidine primarily exerts muscle relaxation effects by inhibiting the release of excitatory amino acids (glutamate and aspartate) from the presynaptic terminals of spinal cord interneurons. Tizanidine has anti-injury activity and can inhibit gastrointestinal (GI) transport. Tizanidine can inhibit the proliferation, migration, and invasion of lung cancer cells and induce cell apoptosis by upregulating Nischarin and inhibiting the AKT and Wnt3a/β-catenin signaling pathways. Tizanidine can be used to treat spasticity caused by diseases such as multiple sclerosis (MS), stroke, and spinal cord injury (SCI).
    Tizanidine-d<sub>4</sub>
  • HY-N2255
    Crebanine
    		Inhibitor 99.83%
    Crebanine is an isoquinoline-like alkaloid that can be derived from Stephania. Crebanine is an antagonist of the α7-nAChR with an IC50 of 19.1 μM. Crebanine suppresses the proliferation, migration, and invasion of cancer cells, triggers reactive oxygen species (ROS) burst, and promotes apoptosis. Crebanine inhibits the AKT/FoxO3a, NF-κB and MAPK signaling pathways. Crebanine attenuates NOX2 hyperactivation, exhibits antioxidant properties by reducing reactive oxygen species and peroxidation. Crebanine inhibits voltage-dependent Na+ current in guinea-pig ventricular myocytes. Crebanine has high inhibitory activity against gram-positive animal pathogenic bacteria. Crebanine ameliorates ischemia-reperfusion brain damage in middle cerebral artery occlusion and reperfusion (MCAO/R) rats. Crebanine significantly improves Scopolamine (HY-N0296)-induced cognitive deficits in ICR mice. Crebanine can be used for the study of hepatocellular carcinoma (HCC), cerebral ischemia and Alzheimer's disease.
    Crebanine
  • HY-U00458
    K-80003
    		Inhibitor 98.83%
    K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.
    K-80003
  • HY-162382
    KTC1101
    		Inhibitor 98.09%
    KTC1101 is an orally active pan-PI3K inhibitor. KTC1101 can inhibit the PI3K signaling pathway, reduce downstream AKT and mTOR phosphorylation, and reduces the expression of Ki67. The anti-tumor effect of KTC1101 has a dual mechanism of action: directly inhibiting tumor cell growth and dynamically enhancing immune response.
    KTC1101
  • HY-N1401
    20(R)-Ginsenoside Rh2
    		Inhibitor 98.0%
    20(R)-Ginsenoside Rh2 is an orally active protopanaxadiol-type saponin with multiple biological activities. 20(R)-Ginsenoside Rh2 exerts a significant inhibitory effect on non-small cell lung cancer and liver cancer by inducing cell cycle arrest and promoting apoptosis. 20(R)-Ginsenoside Rh2 exerts anti-γ-herpesvirus effects by inhibiting viral DNA replication. 20(R)-Ginsenoside Rh2 inhibits inflammatory mediators by reducing the levels of NO, PGE2, and ROS; it can delay skin photoaging by reducing ROS and inhibiting MMP-9/2 activity. 20(R)-Ginsenoside Rh2 accelerates the recovery after muscle injury by activating the Akt1/PKB signaling pathway. 20(R)-Ginsenoside Rh2 can inhibit osteoclast formation and exert an anti-osteoporosis effect.
    20(R)-Ginsenoside Rh2
  • HY-126066
    (-)-Syringaresinol
    		Inhibitor 99.95%
    (-)-Syringaresinol is an orally active isomer of syringaresinol (HY-N8307) found in Annona Montana. (-)-Syringaresinol exhibits antioxidant, anti-inflammatory, and anticancer activities. (-)-Syringaresinol can alleviate ulcerative colitis via the PI3K-Akt/MAPK/Wnt signaling pathway. (-)-Syringaresinol inhibits HL-60 cell proliferation by arresting the G1 phase and inducing apoptosis. (-)-Syringaresinol inhibits LPS (HY-D1056)-induced microglial activation by downregulating the NF-κB p65 signaling pathway and its interaction with ERβ, exerting anti-neuroinflammatory effects.
    (-)-Syringaresinol
  • HY-15966A
    GSK2110183 analog 1 hydrochloride
    		Inhibitor 99.83%
    GSK2110183 analog 1 hydrochloride is the structural analogue of GSK2110183.
    GSK2110183 analog 1 hydrochloride
  • HY-16666
    3CAI
    		Inhibitor 98.32%
    3CAI is a potent and specific AKT1 and AKT2 inhibitor.
    3CAI
  • HY-162143
    SKI-349
    		Inhibitor 99.58%
    SKI-349 is a dual-targeted inhibitor of sphingosine kinase 1/2 (SPHK1/2) and microtubule assembly (MDA). SKI-349 has anticancer activity. SKI-349 can inhibit the vitality, invasion, and AKT/mTOR signaling pathway of liver cells.
    SKI-349
  • HY-17617
    Nastorazepide
    		Inhibitor 99.95%
    Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain.
    Nastorazepide
  • HY-10721
    PF-AKT400
    		Inhibitor 98.0%
    PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC50=0.5 nM) than PKA (IC50=450 nM).
    PF-AKT400
  • HY-132302
    Hu7691
    		Inhibitor 99.91%
    Hu7691 is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 inhibits tumor growth and enables decrease of cutaneous toxicity in mice.
    Hu7691
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Akt Isoform Comparison

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