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

Akt

PKB; Protein kinase B

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-132302A
    Hu7691 free base
    Inhibitor
    Hu7691 free base 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 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice.
    Hu7691 free base
  • HY-118998
    TX2-121-1
    Inhibitor
    TX2-121-1 is a potent and selective Her3 (ErbB3) degrader that contains a hydrophobic adamantane moiety. TX2-121-1 has an IC50 of 49 nM for Her3. TX2-121-1 inhibits Her3-dependent signaling and heterodimerization of Her3. TX2-121-1 has the ability to inhibit cell proliferation. TX2-121-1 can be used in the study of tumors. (Pink: Her3 inhibitor (HY-164988); Black: Linker; Blue: Adamantane (HY-N2427)).
    TX2-121-1
  • HY-N2907R
    Atranorin (Standard)
    Inhibitor
    Atranorin (Standard) is the analytical standard of Atranorin (HY-N2907). This product is intended for research and analytical applications. Atranorin is a secondary metabolite of lichens and AKT inhibitor. Atranorin possesses multiple activities such as antibacterial, anti-inflammatory, antioxidant, anti-glycation, analgesic, and anti-tumor effects. Atranorin has IC50 values for scavenging DPPH and ABTS free radicals of 117 μM and less than 10 μM, respectively. Additionally, Atranorin also exhibits effects in promoting wound healing. Atranorin can be used in the research of various diseases, including myelodysplastic syndromes, tumors, and inflammatory conditions.
    Atranorin (Standard)
  • HY-145281
    MS98
    Inhibitor
    MS98 is a potent and selective PROTAC AKT degrader. MS98 depletes cellular total AKT (T-AKT) with the DC50 value of 78 nM. MS98 binds to AKT1, AKT2, and AKT3 with Kds of 4 nM, 140 nM, and 8.1 nM, respectively.
    MS98
  • HY-171334A
    P1D-34
    Inhibitor
    P1D-34 is a Pin1 PROTAC degrader with a DC50 value of 177 nM. P1D-34 also down-regulates Pin1 client proteins such as Cyclin D1, Rb, Mcl-1, Akt, and c-Myc. P1D-34 shows anti-proliferative activities in a panel of acute myeloid leukemia (AML) cell lines. P1D-34 induces cell DNA damage and apoptosis by releasing ROS generation. Pink: PIN1 ligand (HY-171442A), Blue: CRBN ligand (HY-14658), Black: Linker (HY-W014883).
    P1D-34
  • HY-12059B
    AT7867 hydrochloride
    Inhibitor
    AT7867 hydrochloride is a potent and orally active inhibitor of AKT and p70 S6 kinase. AT7867 hydrochloride has anticancer effect.
    AT7867 hydrochloride
  • HY-172581
    Clifutinib
    Inhibitor
    Clifutinib (Compound 9e) is an orally active and selective internal tandem duplication mutation of FMS-like tyrosine kinase 3 (FLT3-ITD) inhibitor with an IC50 value of 15.1 nM. Clifutinib inhibits the activity of FLT3-ITD kinase and blocks the downstream RAS/MAPK, PI3K/AKT, and JAK/STAT5 signaling pathways of FLT3. Clifutinib induces apoptosis of acute myeloid leukemia (AML) cells with FLT3-ITD mutations. Clifutinib is promising for research of relapsed/refractory FLT3-ITD-positive acute myeloid leukemia.
    Clifutinib
  • HY-112148
    AKT-IN-2
    Inhibitor
    AKT-IN-2 is a potent, selective and orally bioavailable AKT inhibitor with an IC50 of 5 nM for AKT1.
    AKT-IN-2
  • HY-10357
    MK-2206 free base
    Inhibitor
    MK-2206 free base is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206 free base. MK-2206 free base has anticancer activities.
    MK-2206 free base
  • HY-P991243
    MP-RM-1
    Inhibitor
    MP-RM-1 is a selective murine monoclonal antibody inhibitor targeting human epidermal growth factor receptor 3 (ErbB-3). MP-RM-1 blocks the activation of ErbB-3 induced by neuregulin 1 (NRG-1β) and promotes the internalization and degradation of ErbB-3, inhibiting downstream signaling pathways such as PI3K-Akt. MP-RM-1 is promising for research of ErbB-3 highly expressed solid tumors such as breast cancer, melanoma, and prostate cancer.
    MP-RM-1
  • HY-W745090
    Isomaltulose monohydrate
    Inhibitor
    Isomaltulose monohydrate is a fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Isomaltulose monohydrate can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Isomaltulose monohydrate inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM) , cathepsin G release (IC< sub>50: 2.76 μM) and chemotaxis. Isomaltulose monohydrate can improve excessive activation of neutrophils and reduce inflammation or tissue damage. A series of derivatives of Isomaltulose monohydrate are found to have inhibitory effects on FSGS-related TRPC6 functional mutants.
    Isomaltulose monohydrate
  • 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-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-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)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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