1. PI3K/Akt/mTOR
  2. Akt

Akt

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 Related Products (378):

Cat. No. Product Name Effect Purity
  • HY-10358
    MK-2206 dihydrochloride Inhibitor
    MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active, BBB-penetrated allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy[1][2].
  • HY-B0988
    Deferoxamine mesylate Activator
    Deferoxamine mesylate (Deferoxamine B mesylate) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine mesylate upregulates HIF-1α levels with good antioxidant activity. Deferoxamine mesylate also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine mesylate can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19[1][2][3][4][5].
  • HY-18749
    SC79 Activator
    SC79, a unique specific and BBB permeable Akt activator, activates Akt in the cytosol and inhibits Akt membrane translocation. SC79 specifically binds to the PH domain of Akt[1][2][3].
  • HY-15431
    Capivasertib Inhibitor
    Capivasertib (AZD5363) is an orally active and potent pan-AKT kinase inhibitor with IC50 of 3, 7 and 7 nM for Akt1,Akt2 and Akt3, respectively.
  • HY-18723
    Yoda 1 Activator 99.98%
    Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca2+ influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1 activation[1][2][3].
  • HY-159577
    Nic-15 Modulator
    Nic-15 (compound 4n) is an anti-constrictive agent used to antagonize the hypovascularity of pancreatic tumors. The hypovascularity allows cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop drug resistance. Nic-15 can regulate the PI3K/Akt/mTOR pathway and alleviate ER stress induced by Gemcitabine (HY-17026). Nic-15 can significantly inhibit the migration and colony formation of MIA PaCa-2 and PANC-1 pancreatic cancer cells. The combination of Nic-15 and Gemcitabine can effectively solve the problem of pancreatic tumor resistance. In an in vivo xenograft model, Nic-15 can significantly enhance the efficacy of Gemcitabine[1].
  • HY-164400
    SIJ1777 Inhibitor
    SIJ1777 is a GNF-7 (HY-10943) derivative, possesses potent anti-cancer effects on melanoma cells harboring BRAF class I/II/III mutations. SIJ1777 substantially inhibits the activation of MEK, ERK, and AKT. SIJ1777 remarkably induces apoptosis and significantly blocks migration, invasion, and anchorage-independent growth of melanoma cells harboring BRAF class I/II/II mutations[1].
  • HY-164399
    SST0116CL1 Degrader
    SST0116CL1 is a HSP90 inhibitor (IC50: 0.21 μM). SST0116CL1 binds to the ATP binding pocket of Hsp90, and interferes with Hsp90 chaperone function thus resulting in client protein (EGFR, CDK4 and AKT) degradation. SST0116CL1 induces degradation of Her2 in BT-474 cell (IC50: 0.2 μM). SST0116CL1 has antiproliferative activity and inhibits tumor growth[1].
  • HY-125542
    DCZ3301 Inhibitor
    DCZ3301 is a potent aryl-guanidino inhibitor. DCZ3301 inhibits cell proliferation, induces G2/M cell cycle arrest and apoptosis. DCZ3301 inhibits the activation of the PI3K/AKT pathway by downregulating the protein expression of PI3K and phosphorylation of AKT. DCZ3301 can be used in research of cancer[1].
  • HY-N4327
    Eurycomalactone Inhibitor 98.99%
    Eurycomalactone is an active quassinoid could be isolated from Eurycoma longifolia Jack. Eurycomalactone is a potent NF-κB inhibitor with an IC50 value of 0.5 μM. Eurycomalactone inhibits protein synthesis and depletes cyclin D1. Eurycomalactone enhances radiosensitivity through arrest cell cycle at G2/M phase and delayed DNA double-strand break repair. Eurycomalactone inhibits the activation of AKT/NF-κB signaling, induces apoptosis and enhances chemosensitivity to Cisplatin (HY-17394)[1][2][3].
  • HY-N1914
    Ergothioneine Inhibitor
    Ergothioneine is an imidazole-2-thione derivative with orally active histidine betaine. Ergothioneine is a specific inhibitor of p38-MAPK and Akt, which plays a protective role in cell apoptosis induced by stress. Ergothioneine has antioxidant activity[1][2].
  • 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[1].
  • HY-N3426
    Kazinol B Activator
    Kazinol B, a prenylated flavan with a dimethyl pyrane ring, is an inhibitor of nitric oxide (NO) production. Kazinol B improves insulin sensitivity by enhancing glucose uptake via the insulin-Akt signaling pathway and AMPK activation. Kazinol B has the potential for diabetes mellitus research[1][2].
  • HY-18296
    AKT-IN-1 Inhibitor 98.41%
    AKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM.
  • HY-N9149
    Cryptanoside A Inducer
    Cryptanoside A, a cardiac glycoside epoxide, can be isolated from the stems of Cryptolepis dubia. Cryptanoside A has potent cytotoxicity against cancer cells. Cryptanoside A also inhibits Na+/K+-ATPase activity. Cryptanoside A increases the expression of Akt and the p65 subunit of NF-κB[1].
  • HY-15965
    Uprosertib Inhibitor 99.74%
    Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.
  • HY-P0093
    Sincalide Modulator 99.51%
    Sincalide (Cholecystokinin octapeptide, CCK‐8) is a rapid-acting amino acid polypeptide hormone analogue of cholecystokinin (CCK) for intravenous use in postevacuation cholecystography. CCK‐8 is a major bioactive segment of CCK that retains most of the biological activities of CCK. CCK‐8 can promote gallbladder contraction by injection and helps diagnose gallbladder and pancreas disorders. CCK‐8 can increase bile secretion, cause the gallbladder to contract and relax the sphincter of Oddi, resulting in bile drainage into the duodenum. CCK‐8 is a major bioactive segment of CCK that retains most of the biological activities of CCK[1][2][3].
  • 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[1].
  • HY-101364A
    CHPG sodium salt Activator 99.25%
    CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells[1]. CHPG sodium salt protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways.[2].
  • HY-121012
    (rac)-AG-205
    (rac)-AG-205 is a potent inhibitor of progesterone receptor membrane component 1 (Pgrmc1) that induces genes involved in sterol synthesis, including the INSIG1 protein, which forms a complex with PGRMC1. (rac)-AG-205 prevents neuronal resistance to hypoxic ischaemia by blocking NF-kB signalling and activation of the BDNF/PI3K/AKT pathway[1].