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-159517
    PI3K/Akt/mTOR-IN-5
    		Inhibitor
    PI3K/Akt/mTOR-IN-5 (compound D3) is a derivative of Pseudolaric Acid B (HY-N6939) with anti-tumor activity. PI3K/Akt/mTOR-IN-5 inhibits excessive proliferation of tumor cells through the PI3K/AKT/mTOR and STAT3/GPX4 pathways. PI3K/Akt/mTOR-IN-5 effectively inhibits EDU positivity, reduces colony formation, places HCT-116 cells in the S phase and G2/M phase, and induces apoptosis.
    PI3K/Akt/mTOR-IN-5
  • HY-176299
    Tanerasertib
    		Inhibitor
    Tanerasertib (Compound 456) is an AKT1 inhibitor with an IC50 of less than 15 nM against AKT1 E17K. Tanerasertib can be used in the study of cancer.
    Tanerasertib
  • HY-138767
    AKT-IN-5
    		Inhibitor
    AKT-IN-5 (Example 8) is a Akt inhibitor with IC50 values of 450 nM and 400 nM for Akt1 and Akt2, respectively.
    AKT-IN-5
  • HY-148937
    Oroselol
    		Inhibitor
    Oroselol is a coumarin commonly found in a variety of plants, especially in the roots of angelica plants and the bark of cinnamon trees. Oroselol has potential medicinal properties, including anti-inflammatory, antioxidant and anti-tumor effects. Oroselol can be used in the production of fragrances, flavors and medicines
    Oroselol
  • HY-144254
    PI3Kδ-IN-10
    		Inhibitor
    PI3Kδ-IN-10 is a highly potent and orally active PI3Kδ inhibitor with IC50 of 2 nM. PI3Kδ-IN-10 robustly suppresses the downstream AKT pathway to induce subsequent apoptosis in hepatocellular carcinoma models.
    PI3Kδ-IN-10
  • HY-127067
    Yuanhuadin
    		Inhibitor
    Yuanhuadin, extracted from Genkwa Flos Daphne genkwa, has antitumor activity through inhibiting Akt/mTOR and EGFR pathways, induce cell-cycle arrest and abortion.
    Yuanhuadin
  • HY-123035
    Gamendazole
    		Inhibitor 99.44%
    Gamendazole, an indazole carboxylic acid (ICA), is an orally active, selective HSP90AB1 (HSP90BETA) and EEF1A1 (eEF1A) inhibitor. Gamendazole binds to the C-terminal nucleotide binding pocket of HSP90 and cause downregulation of clients AKT1 and ERBB2, but stabilizes the HSP90 heterocomplex. Gamendazole specifically inhibits the actin bundling function of EEF1A1, but does not bind to the nucleotide docking pocket nor inhibits the ribosome charging or protein translation functions of EEF1A1. Gamendazole, an antispermatogenic compound with antifertility effects, has the potential for reversible non-hormonal male contraceptive agent research.
    Gamendazole
  • HY-146218
    MMP-9-IN-5
    		Inhibitor
    MMP-9-IN-5 is a MMP-9 inhibitor (IC50: 4.49 nM) that forms hydrogen bond with MMP-9. MMP-9-IN-5 also inhibits AKT activity (IC50: 1.34 nM). MMP-9-IN-5 shows cell cytotoxicity and induces cell apoptosis. MMP-9-IN-5 can be used in the research of cancers.
    MMP-9-IN-5
  • HY-P991234
    COVA208
    		Inhibitor
    COVA208 is a bispecific FynomAb (a fusion protein of an antibody and a Fyn SH3-derived binding protein) that targets HER2. COVA208 induces the degradation of HER2, reduces the levels of HER2, HER3, and EGFR, thereby effectively blocking the downstream signaling pathways of HER2, including the HER3-PI3K-AKT and MAPK pathways, and simultaneously inducing apoptosis of tumor cells. COVA208 is promising for research of cancers, such as HER2-positive breast cancer, gastric cancer, and colorectal cancer.
    COVA208
  • HY-P990248
    Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1)
    		Inhibitor
    Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) is an anti-mouse E-Cadherin/CD324 IgG1 monoclonal antibody. Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) can downregulate the HER signaling axis and PI3K/Akt/mTOR signaling pathway. Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) can inhibit the proliferation of tumor cells and induce their apoptosis. Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) can be used for researches on cancer and inflammation conditions such as breast cancer, chronic compression injury (CCI) and asthma.
    Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1)
  • HY-N6872R
    Actein (Standard)
    		Inhibitor
    Actein (Standard) is the analytical standard of Actein. This product is intended for research and analytical applications. Actein, a triterpene glycoside, shows an inhibitory effect on cancer cells, which is isolated from the rhizomes of Cimicifuga foetida. Actein suppresses cell proliferation, induces autophagy and apoptosis through promoting ROS/JNK activation, and blunting AKT pathway in bladder cancer. Actein has little toxicity in vivo.
    Actein (Standard)
  • HY-P10833
    C-VGB3
    		Inhibitor
    C-VGB3 is a selective vascular endothelial growth factor receptor 2 (VEGFR2) antagonist, which inhibits VEGFR2-mediated PI3K/AKT/mTOR and PLCγ/ERK1/2 signaling pathways. C-VGB3 binds to the extracellular domain of VEGFR2, blocking ligand-receptor interaction and inducing apoptosis in endothelial and tumor cells through both intrinsic (involving Bcl2 family and caspases) and extrinsic (death receptor-mediated) pathways. C-VGB3 is promising for research of angiogenesis-related cancers, such as breast cancer.
    C-VGB3
  • HY-155721
    22-(4′-py)-JA
    		Inhibitor
    22-(4′-py)-JA is a semisynthetic derivative of junamycin A (JA) that can be isolated from the Thai blue sponge (Xestospongia sp.). 22-(4′-py)-JA has antimetastatic activity and can inhibit AKT/mTOR/p70S6K signaling. 22-(4′-py)-JA inhibits tumor cell invasion and tube formation in human umbilical vein endothelial cells (HUVEC), downregulates metalloproteinases (MMP-2 and MMP-9), hypoxia-inducible factor 1α (HIF-1α) and vascular endothelial growth factor (VEGF). 22-(4′-py)-JA has potent anticancer activity against non-small cell lung cancer (NSCLC).
    22-(4′-py)-JA
  • HY-116604
    RLX
    		Inhibitor
    RLX (PD 139530) is a PI3K/Akt/FoxO3a signaling inhibitor, possessing significant therapeutic potential in experimental colon cancer. RLX can effectively modulate the tumor microenvironment, enhancing the efficacy of cancer immunotherapy. RLX demonstrates the ability to improve the retention time of therapeutic agents within the tumor microenvironment by utilizing advanced nanoparticle delivery systems. RLX can be integrated with various treatment modalities, such as chemotherapy and radiotherapy, to enhance overall tumor therapy effectiveness. RLX highlights the necessity for further research into the tumor microenvironment’s dynamics to develop more tailored treatment approaches for diverse tumor types.
    RLX
  • HY-174415
    ZSH-2117
    		Inhibitor
    ZSH-2117 is a covalent and selective EGFR PROTAC degrader with a DC50 of 45 nM in Ba/F3-EGFRL858R/T790M/C797S cells. ZSH-2117 significantly inhibits cell proliferation and reduces the downstream EGFR signaling proteins level of AKT and ERK. ZSH-2117 effectively inhibits tumor growth in Ba/F3-EGFRL858R/T790M/C797S xenograft mice model. Pink: EGFR ligand (HY-175162); Blue: NEDD4 ligase ligand (HY-175159); Black: linker
    ZSH-2117
  • HY-N6896R
    Isoviolanthin (Standard)
    		Inhibitor
    Isoviolanthin (Standard) is the analytical standard of Isoviolanthin (HY-N6896). This product is intended for research and analytical applications. Isoviolanthin is a flavonoid glycoside. Isoviolanthin can be extracted from Dendrobium officinale. Isoviolanthin has a strong affinity for binding to KDM6B, CHAC2, ESCO2, and IPO4. Isoviolanthin decreases MMP-2 and MMP-9. Isoviolanthin inhibits TGF-β/Smad and PI3K/Akt/mTOR signaling pathways. Isoviolanthin increases Fhl3 expression. Isoviolanthin has cytoprotective effects. Isoviolanthin has anticancer activity against hepatocellular carcinoma.
    Isoviolanthin (Standard)
  • HY-109198A
    Zandelisib hydrochloride
    		Inhibitor
    Zandelisib (ME-401) hydrochloride is a selective, orally active, non-covalent inhibitor of PI3Kδ. Zandelisib hydrochloride can sustainably inhibit AKT phosphorylation and downstream signaling pathways. Zandelisib hydrochloride can be used in the study of malignancies such as relapsed/refractory B-cell lymphoma.
    Zandelisib hydrochloride
  • HY-153640
    AKT-IN-14
    		Inhibitor
    AKT-IN-14 (Example 2) is a potent AKTinhibitor with the IC50 values of <0.01 nM, 1.06 nM and 0.66 nM for AKT1, AKT2, AKT3, respectively. AKT-IN-14 can be used in cancer research.
    AKT-IN-14
  • HY-173188
    EGFR-IN-154
    		Inhibitor
    EGFR-IN-154 (compound 4c) is an EGFR inhibitor with EC50 values of 0.16 μM, 21.73 μM and 41.56 μM against EGFR Del19, EGFR WT and EGFR L858R, respectively. EGFR-IN-154 shows anticancer activity on various cance cell lines. EGFR-IN-154 induces mitochondrial apoptosis, and decreases pERK1/2 and pAkt levels, but increases pJNK and pp38 levels.
    EGFR-IN-154
  • HY-174379
    KRAS IN-44
    		Inhibitor
    KRAS IN-44 (Compound S2C2M2) is a PDE6D degrader. KRAS IN-44 inhibits PDE6D-dependent KRAS trafficking and KRAS downstream signaling pathways. KRAS IN-44 down-regulates EGF-induced the phosphorylation of PI3K, AKT, and mTOR. KRAS IN-44 increases Apoptosis. KRAS IN-44 has antitumor activity against hepatoblastoma.
    KRAS IN-44
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Akt Isoform Comparison

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