Akt1
AKT1 (protein kinase Bα, PKBα) is a serine/threonine kinase that functions as a central effector of the PI3K/AKT/mTOR signaling pathway, regulating cellular growth, survival, metabolism, proliferation, and differentiation across multiple tissues and cell types[1][2][3]. Activation of AKT1 occurs downstream of PI3K through phosphoinositide-dependent kinase-1 (PDK1)-mediated phosphorylation, enabling downstream regulation of targets involved in protein synthesis, apoptosis control, and metabolic adaptation[4][5]. Mechanistically, AKT1 contributes to angiogenesis, physiological tissue growth, immune-cell function, and stress-response signaling, making it a critical node in both normal physiology and disease-associated signaling networks[2][4][5]. In disease models, dysregulated AKT signaling is strongly associated with cancer, metabolic disorders, cardiovascular pathology, and inflammatory conditions, and constitutive activation of AKT-dependent pathways promotes oncogenic progression and therapeutic resistance[2][6][7]. Compared with related isoforms, AKT1 exhibits distinct biological functions despite substantial structural homology with AKT2 and AKT3; genetic studies demonstrate that AKT1 deficiency primarily causes growth retardation, whereas AKT2 deficiency induces insulin resistance and diabetes, and AKT3 loss predominantly affects brain development[4][5]. Isoform-specific investigations further show that AKT1 and AKT2 can exert non-redundant or even opposing effects on migration, invasion, inflammation, and fibrogenesis depending on cellular context[2][6][8]. For experimental applications, increasing efforts focus on developing AKT1-selective inhibitors and isoform-selective cellular models, which provide valuable tools for dissecting AKT isoform-specific signaling and for evaluating targeted therapeutic strategies with improved selectivity profiles[6][7][9].
References:
- [1]. Guerau-de-Arellano M, et al. Akt isoforms in the immune system. Front Immunol. 2022 Aug 23;13:990874. [Content Brief]
- [2]. Reyes-Gordillo K, et al. Akt1 and Akt2 Isoforms Play Distinct Roles in Regulating the Development of Inflammation and Fibrosis Associated with Alcoholic Liver Disease. Cells. 2019 Oct 29;8(11):1337. [Content Brief]
- [3]. O'Neill BT, et al. Akt1 in the cardiovascular system: friend or foe? J Clin Invest. 2005 Aug;115(8):2059-64. [Content Brief]
- [4]. Tellai AD, et al. The complex post-transcriptional regulation of genes coding for methionine adenosyl transferase: New insights for liver cancer. Biochimie. 2025 Nov;238(Pt A):19-28. [Content Brief]
- [5]. Quambusch L, et al. Cellular model system to dissect the isoform-selectivity of Akt inhibitors. Nat Commun. 2021 Sep 6;12(1):5297. [Content Brief]
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Akt1 Related Products (40)
Related Products (40)
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Antibodies (4)
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Moracin G
0 ImagesCat. No.: HY-N17632CAS No.: 73338-86-0Moracin G is a plant-derived kinase modulator and receptor ligand that forms stable bindings with multiple key proteins (AKT1, COX2 and Estrogen receptor 1) and competitively inhibits the activity of specific kinases. By binding to MELK to disrupt cell cycle regulation, Moracin G impairs the survival and proliferation of cancer cells, induces cancer cell apoptosis, and thereby exerts anti-tumor potential. Moracin G can be used in research related to periodontitis and breast cancer.
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AKT1-IN-10
0 ImagesCat. No.: HY-175716CAS No.: 3077847-90-3AKT1-IN-10 (Compound I-118) is a non-covalent allosteric AKT1 inhibitor with an IC50 of < 500 μM. AKT1-IN-10 has oral bioavailability.AKT1-IN-10 can be used in cancer.
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Anticancer agent 331
0 ImagesCat. No.: HY-184487Anticancer agent 331 is an anticancer agent with favorable cell permeability and limited blood-brain barrier penetration. Anticancer agent 331 forms stable long-acting complexes with TNF-α, PI3K p110α, AKT1 and mTOR, and exerts cytotoxic effects on cancer cells. Anticancer agent 331 can be used in the research of colorectal cancer.
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AKT1-IN-13
0 ImagesCat. No.: HY-184145AKT1-IN-13 is an orally active AKT1 inhibitor with an IC50 of 5.17 μM. AKT1-IN-13 also exhibits high inhibitory activity against PAK1, PKA, MAP2K1 (MEK1 / MAPKK1) and MAPK1 (ERK2). AKT1-IN-13 induces cell apoptosis, activates the pro-apoptotic protein BAX, inhibits the anti-apoptotic protein Bcl-2, and activates caspase 3 simultaneously. As a cytotoxic agent, AKT1-IN-13 exerts a killing effect on orthotopically transplanted liver cancer in an AKT1-dependent manner. AKT1-IN-13 can be used in studies related to hepatocellular carcinoma.
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Akt1-IN-5
0 ImagesCat. No.: HY-163577CAS No.: 3034252-53-1Akt1-IN-5 (Compound 115) is an Akt1 inhibitor (IC50: <15 nM)
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CK2-TN03
0 ImagesCK2-TN03 is an ATP-competitive casein kinase 2 (CK2) inhibitor, with an IC50 of 165 nM and a Ki of 20 nM. CK2-TN03 inhibits CK2-mediated survivin activation and reduces CK2-dependent phosphorylation levels of BRD4/MYCN and AKT1. CK2-TN03 exerts anti-neuroblastoma effects by inhibiting survivin, leading to mitotic catastrophe and apoptosis of cancer cells. CK2-TN03 can be used in studies related to neuroblastoma.
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Ipatasertib tosylate
0 ImagesCat. No.: HY-15186CCAS No.: 1491138-24-9Synonyms: GDC-0068 tosylate; RG7440 tosylateIpatasertib (GDC-0068) tosylate is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib tosylate synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib tosylate also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models.
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Multi-kinase-IN-7
0 ImagesCat. No.: HY-178142Multi-kinase-IN-7 is a multikinase inhibitor with IC50s of 2.19, 2.95, 3.59 and 9.31 μM against EGFR, VEGFR2, TrKA and CDK2, respectively. Multi-kinase-IN-7 shows moderate and weaker activity against FAK, AKT1, GSK3β and CDK5 with IC50 values of 6.3, 9.2, 11.7 and 23.4 μM, respectively. Multi-kinase-IN-7 displays broad spectrum antiproliferative potential against NCI cancer cell lines. Multi-kinase-IN-7 induces cell cycle arrest, apoptosis and necrosis. Multi-kinase-IN-7 Inhibitor can be used for the study of breast cancer.
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Solenopsin
0 ImagesCat. No.: HY-16461CAS No.: 137038-57-4Synonyms: (-)-Solenopsin ASolenopsin ((-)-Solenopsin A) is an ATP-competitive and selective Akt-1 inhibitor with an IC50 of 5-10 μM, and also acts as an RSK1 inhibitor. Solenopsin inhibits the activities of PDK1 in lipid rafts, downregulates PI3K, blocks PI3K-dependent generation of 3-phosphoinositides, and suppresses the phosphorylation of FOXO1a. Solenopsin induces Mitophagy and ROS production, reduces mitochondrial oxygen consumption, and exhibits antiproliferative and antiangiogenic activities. Solenopsin can be used in research related to hyperproliferative skin diseases and malignant diseases.
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Psoralenol
0 ImagesCat. No.: HY-N19906CAS No.: 70522-30-4Psoralenol is a binder with strong binding affinity for ACTB and AKT1. Psoralenol forms stable complexes with ACTB and AKT1 through hydrogen bonding and protein interactions. Psoralenol exhibits larvicidal activity against brine shrimp. Psoralenol inhibits methicillin-resistant Staphylococcus aureus, Vibrio parahaemolyticus, Candida albicans, and Pseudomonas aeruginosa. Psoralenol can be used in research related to chronic obstructive pulmonary disease, bacterial infections, and fungal infections.
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Akt1-IN-8
0 ImagesCat. No.: HY-173122CAS No.: 2247688-87-3Akt1-IN-8 (Compound JL18) is a potent and oral bioavailable (41%) inhibitor of AKT1 kinase, with an IC50 of 8.8 nM. Akt1-IN-8 exhibits significant antiproliferative effects against PC-3 prostate cancer cells, with an IC50 of 3.0 μM. Akt1-IN-8 can reduce phosphorylated GSK3β levels.
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EGFR-IN-201
0 ImagesCat. No.: HY-181659CAS No.: 3103654-99-2EGFR-IN-201 is a potent EGFR inhibitor, with an IC50 of 0.091 μM against wild-type EGFR; for mutant EGFR variants, the IC50 values of EGFRT790M, EGFRL858R and EGFRC797S are 0.147 μM, 0.221 μM and 0.703 μM, respectively. EGFR-IN-201 inhibits EGFR downstream signaling proteins AKT1 (IC50 = 0.225 μg/mL) and ERK1 (IC50 = 0.705 μg/mL). EGFR-IN-201 induces G0/G1 cell cycle arrest, apoptosis and low-level necrosis in cancer cells. EGFR-IN-201 is applicable to research on cancers such as colon cancer.
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Akt1-IN-6
0 ImagesCat. No.: HY-163578CAS No.: 3034254-12-8Akt1-IN-6 (Compound 273) is an Akt1 inhibitor (IC50: <15 nM)
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JAK1-IN-21
0 ImagesCat. No.: HY-184592JAK1-IN-21, biotin-conjugated isoxazole derivative, is a JAK1 inhibitor. JAK1-IN-21 directly engages and stabilizes JAK1, reduces the phosphorylation of JAK1, STAT1 and AKT, induces apoptotic marker cleavage (PARP, Caspase-3, Caspase-7) and exhibits broad-spectrum antiproliferative activity against cancer cells. JAK1-IN-21 can be used for the study of liver cancer, prostate cancer, and breast cancer.
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Akt1-IN-7
0 ImagesCat. No.: HY-163579CAS No.: 3034255-09-6Akt1-IN-7 (Compound 370) is an Akt1 inhibitor (IC50: <15 nM).
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NSC 850745
0 ImagesCat. No.: HY-175848NSC 850745 is a selective and potent c-Met/STAT3 inhibitor with IC50 values of 210 and 670 nM. NSC 850745 can inhibit cell proliferation, induce G2/M phase arrest and induce apoptosis. NSC 850745 can downregulate AKT-1, VEGF and Bcl-2 expression and upregulate p53, Bax and caspase expression. NSC 850745 can be used for the research of cancer, such as leukemia and colon cancer.
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Akt1-IN-4
0 ImagesCat. No.: HY-161439CAS No.: 3033577-05-5Akt1-IN-4 (Compound 62) is an AKT1-E17K inhibitor with an IC50 value of less than 15 nM.
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BRD4/AKT-IN-1
0 ImagesCat. No.: HY-183273CAS No.: 3087270-50-3BRD4/AKT-IN-1 is a BRD4/AKT inhibitor with BRD4 IC50 66.12 nM and AKT1 IC50 143.81 nM. BRD4/AKT-IN-1 blocks BRD4-mediated c-Myc transcriptional regulation, modulates AKT1 signaling, decouples AKT phosphorylation from pro-survival effectors. BRD4/AKT-IN-1 induces G0/G1 cell cycle arrest via downregulated phosphorylated RB, cyclin E1, CDK2. BRD4/AKT-IN-1 elevates LC3B levels to promote autophagy. BRD4/AKT-IN-1 promotes apoptosis in cancer cells. BRD4/AKT-IN-1 can be used for the research of metastatic castration-resistant prostate cancer.
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