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-B0633I
    Hyaluronic acid sodium (MW 800kDa)
    Hyaluronic acid sodium (MW 800kDa) is a biopolymer composed of repeating units of disaccharides with various applications. Hyaluronic acid sodium is a major component of the extracellular matrix (ECM). Hyaluronic acid sodium is synthesized at the plasma membrane. Increased hyaluronic acid sodium levels are associated with tumor cell growth, adhesion, migration, invasion and angiogenesis in digestive cancers. Hyaluronic acid sodium participates in tissue remodeling and rapid cell proliferation in some physiological processes including embryonic morphogenesis and wound-healing. Hyaluronic acid sodium activates the PI3K-Akt signaling. Hyaluronic acid sodium acts as a regulator of cancer-associated lymphangiogenesis. Hyaluronic acid sodium also enhances cell invasion and angiogenesis by promoting proteolytic MMP-9 binding to cell surface or stimulating MMP-9 binding to cell surface. Hyaluronic acid sodium can be used as drug delivery for sodium butyrate to improve the anti-proliferative activity on breast cancer cell line. Hyaluronic acid sodium can be studied in joint diseases, wound healing and cancer.
    Hyaluronic acid sodium (MW 800kDa)
  • HY-B0380
    Trimebutine
    		Inhibitor 99.42%
    Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
    Trimebutine
  • HY-N1103
    Vasicine
    		Activator 98.80%
    Vasicine (peganine) is a quinazoline alkaloid isolated from Justicia adhatoda. Vasicine activates PI3K/Akt signaling pathway, exhibits antioxidant, anti-inflammatory and antibacterial activities.
    Vasicine
  • HY-134877
    BAY 2476568
    		Inhibitor 99.88%
    BAY 2476568 is a potent and mutant-selective inhibitor targeting EGFR exon20 insertion variants. BAY 2476568 potently inhibits the kinase activity of EGFR exon20 insertion mutants (insASV, insSVD, insNPG) with IC50 values of 0.09 nM, 0.21 nM, and 0.11 nM, respectively. BAY 2476568 inhibits EGFR (Y1068) phosphorylation and reduces the phosphorylation of ERK1/2 and Akt (S473) in Ba/F3 cells expressing EGFR exon20 insertion mutants (insASV, insSVD). BAY 2476568 can be used for the study of non-small cell lung cancer (NSCLC) driven by EGFR exon20 insertion mutations.
    BAY 2476568
  • HY-157133
    TAS0612
    		Inhibitor 98.83%
    TAS0612 is the orally active inhibitor of RSK、AKT and S6K. TAS0612 has antitumor activity.
    TAS0612
  • HY-N0167
    Gynostemma Extract
    		Inhibitor 99.92%
    Gynostemma Extract (Gypenoside IX) is a triterpenoid saponin. Gynostemma Extract can be isolated from Panax notoginseng. Gynostemma Extract reduces NFκB nuclear translocation and transcriptional activity by inhibiting the p38 MAPK/Akt/NFκB signaling pathway. Gynostemma Extract reduces the expression of cytokines (COX-2, IL-6) and the production of NO. Gynostemma Extract has anti-inflammatory activity. Gynostemma Extract can be used in the study of liver injury and neuroinflammation.
    Gynostemma Extract
  • HY-106263B
    Tyroserleutide hydrochloride
    		Inhibitor 99.92%
    Tyroserleutide hydrochloride is a tripeptide isolated from the degradation products of porcine spleen with antitumor activity. Tyroserleutide hydrochloride can upregulate the expression of the tumor suppressor gene PTEN and inhibit the activity of AKT and PDK1. Tyroserleutide hydrochloride inhibits tumor cell proliferation and MDM2 phosphorylation by inhibiting the PI3K/AKT pathway, and also upregulates P21, P27, P53, and induces mitochondrial damage and cell apoptosis.
    Tyroserleutide hydrochloride
  • HY-16441
    Tegafur-gimeracil-oteracil potassium
    		Inhibitor 99.96%
    Tegafur-gimeracil-oteracil potassium (S-1; TS-1) is an orally active anticancer agent composed of Tegafur (HY-17400), Gimeracil (HY-17469), and Oteracil potassium (HY-17511). Tegafur-gimeracil-oteracil potassium inhibits the proliferation, migration and invasion of endometrial cancer cells and induces apoptosis by blocking the PI3K/AKT/mTOR signaling pathway. Tegafur-gimeracil-oteracil potassium can be used in research related to endometrial cancer and gastric cancer with peritoneal metastasis.
    Tegafur-gimeracil-oteracil potassium
  • 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 in microglia cells. 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-13254A
    A-674563 hydrochloride
    		Inhibitor 99.61%
    A-674563 hydrochloride is a potent and selective Akt1 inhibitor with Ki of 11 nM.
    A-674563 hydrochloride
  • HY-12059A
    AT7867 dihydrochloride
    		Inhibitor 99.73%
    AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
    AT7867 dihydrochloride
  • HY-50862
    Akt1/Akt2-IN-1
    		Inhibitor 99.30%
    Akt1/Akt2-IN-1 (Compound 17) is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM), with potent and balanced activity.
    Akt1/Akt2-IN-1
  • HY-128393
    Trilinolein
    		Inhibitor 98.0%
    Trilinolein is an orally active triglyceride that inhibits the PI3K/Akt, Ras/MEK/ERK signaling pathways, and MMP-2. Trilinolein can reduce oxidative stress, induce apoptosis, and inhibit cell migration. Trilinolein can be used in the research fields of cardiovascular disease, cerebrovascular disease (such as cerebral ischemia), and non-small cell lung cancer.
    Trilinolein
  • HY-N2232
    N-​Feruloyloctopamine
    		Inhibitor 99.91%
    N-Feruloyloctopamine (N-trans-Feruloyloctopamine) is an antioxidant component that can be isolated from garlic skin. N-Feruloyloctopamine can inhibit tumor cell proliferation and invasion, and induce apoptosis. N-Feruloyloctopamine has antitumor activity and can be used in the research of tumors such as hepatocellular carcinoma.
    N-​Feruloyloctopamine
  • HY-162143
    SKI-349
    		Inhibitor 99.48%
    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-N0430A
    Coptisine Sulfate
    		Inhibitor 99.37%
    Coptisine Sulfate is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine Sulfate is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine Sulfate suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine Sulfate shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine Sulfate inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine Sulfate inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine Sulfate downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine Sulfate be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease.
    Coptisine Sulfate
  • HY-B0194
    Tizanidine
    		Inhibitor 99.58%
    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
  • HY-109061B
    Lazertinib mesylate
    		Inhibitor 99.85%
    Lazertinib (YH25448; GNS-1480) mesylate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia.
    Lazertinib mesylate
  • HY-119152
    CMX-2043
    		Activator 98.80%
    CMX-2043 is a novel analogue of α-Lipoic Acid (HY-N0492). CMX-2043 is effective in antioxidant effect, activation of insulin receptor kinase, soluble tyrosine kinase, and Akt phosphorylation. CMX-2043 shows protection against ischemia-reperfusion injury (IRI) in rat model.
    CMX-2043
  • HY-15673
    KP372-1
    		Inhibitor 99.5%
    KP372-1 is an Akt inhibitor that inhibits proliferation and induces apoptosis and anoikis. KP372-1 is also an NQO1 redox cycling agent that causes DNA damage (including DNA breakage) by generating ROS. KP372-1 can be used in cancer research (such as head and neck squamous cell carcinoma (HNSCC) and pancreatic cancer).
    KP372-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Akt Isoform Comparison

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