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AKT inhibitor
AKT inhibitor VIII is a cell-permeable and reversible quinoxaline compound that potently and selectively inhibits Akt1/Akt2 activity (IC50 = 58 nM, 210 nM, and 2.12 μM for Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays).- Bjune K, .et al. , PLoS One, 2019, Jun 19;14(6):e0218537 PMID: 31216345
- Hoshiba T, .et al. , Biochim Biophys Acta, 2016, Nov;1863(11):2749-2757 PMID: 27558478
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Akt inhibitor
Perifosine (also KRX-0401) acts as an Akt inhibitor and a PI3K inhibitor.- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Bjune K, .et al. , PLoS One, 2019, Jun 19;14(6):e0218537 PMID: 31216345
- Kyoung-Jae Won, .et al. , Cell Death Dis, 2017, Jan; 8(1): e2554 PMID: 28079882
- Zhipeng Li, .et al. , Oncotarget, 2016, May 31; 7(22): 31892-31906 PMID: 26895469
- Won KJ, .et al. , Apoptosis., 2014, Jan;19(1):179-90 PMID: 24085402
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Akt inhibitor
A-674563 is a B/Akt inhibitor with an IC50 of 14 nM and also shows inhibitory activity against PKA and CDK2 with IC50 of 16 and 46 nM, respectively.- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Kobayashi T, .et al. , Biochem Biophys Res Commun, 2018, Jan 1;495(1):1468-1475 PMID: 29196261
- Lin Xu, .et al. , Biochem Biophys Res Commun, 2016, Apr 15;472(4):662-8 PMID: 26920060
- Zou Y, .et al. , Biochem Biophys Res Commun, 2016, Aug 12;477(1):1-8 PMID: 26970307
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AKT inhibitor
GSK690693 is a novel ATP-competitive, low-nanomolar pan-Akt kinase inhibitor (IC50 values are 2, 13 and 9 nM of Akt1, 2 and 3 respectively).- Khan MI, .et al. , Prog Neuropsychopharmacol Biol Psychiatry, 2018, Mar 2;82:39-48 PMID: 9223784
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AKT inhibitor
Capivasertib (AZD5363) is a potent inhibitor of AKT with pharmacodynamic activity in vivo, has potential to treat a range of solid and hematologic tumors as monotherapy or a combinatorial agent.
- Léa-Isabelle Renaud, .et al. , PLoS One, 2024, Jun 21;19(6):e0302042 PMID: 38905217
- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Hiroyuki Tsuchiya, .et al. , Curr Issues Mol Biol, 2023, Jan 29;45(2):1073-1085 PMID: 36826016
- Giri R. Gnawali, .et al. , Medicinal Chemistry Research, 2022, 31: 1154-1175 PMID: 36389181
- Jeremiah J Bearss, .et al. , EMBO Rep, 2021, Apr 7;22(4):e50835 PMID: 33586867
- Jin H. Song, .et al. , Mol Cancer Ther, 2018, Dec;17(12):2710-2721 PMID: 30190422
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AKT Inhibitor
MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively.- Yanqiong Guo, .et al. , RSC Adv, 2026, Jul 2;16(34):32373-32384 PMID: 42395791
- Sholihah, I.A., .et al. , BioNanoSci, 2026, 16, 396
- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Yi-Ru Pan, .et al. , Int J Biol Sci, 2023, May 21;19(9):2772-2786 PMID: 37324940
- Giorgio Caratti, .et al. , EMBO Rep, 2023, Feb 6;24(2):e55363 PMID: 36520372
- Ming-Chun Hung, .et al. , Cell Biosci, 2022, 12: 122 PMID: 35918763
- Yusuke Murase, .et al. , Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Ali Nasrollahzadeh, .et al. , Biochim Biophys Acta Mol Cell Res, 2021, Jun 26;1868(10):119087 PMID: 34182011
- Rona Aviram, .et al. , PLoS Biol, 2021, Dec 30;19(12):e3001492 PMID: 34968386
- Cristina Roselló-Busquets, .et al. , Front Mol Neurosci, 2020, 13: 56 PMID: 32317932
- Dai-Chi Liu, .et al. , eNeuro, 2020, Mar 27;7(2):ENEURO.0438-19.2020 PMID: 32161037
- Nishihama K, .et al. , Metabolism, 2018, May;82:88-99 PMID: 29366755
- J Wei, .et al. , bioRxiv, 2018, 2018
- Joo Sang Lee, .et al. , Nat Commun, 2018, 9: 2546 PMID: 29959327
- Wan-Ting Hu, .et al. , Am J Cancer Res, 2018, 8(9): 1739-1751 PMID: 30323967
- Angela M. Gocher, .et al. , J Biol Chem, 2017, Aug 25; 292(34): 14188-14204 PMID: 28634229
- Kusuyama J, .et al. , Biochem J, 2017, Oct 5;474(20):3421-3437 PMID: 28887384
- Pi-Lin Sung, .et al. , Oncotarget, 2016, Jan 26; 7(4): 4036-4047 PMID: 26716408
- Mikaël M. Martino, .et al. , Nat Commun, 2016, 7: 11051 PMID: 27001940
- Dominik Schulz, .et al. , Am J Cancer Res, 2016, 6(9): 1963-1975 PMID: 27725902
- Jewett KA, .et al. , J Neurochem., 2015, Oct;135(2):226-33 PMID: 26250624
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AKT Inhibitor
Palomid 529 is a dual TORC1/2 inhibitor of the PI3K/Akt/mTOR pathway having broad activity in angiogenesis and cellular proliferation. -
AKT Inhibitor
Triciribine phosphate inhibits the phosphorylation, activation, and signalling of Akt-1, -2, and -3, which may result in the inhibition of Akt-expressing tumor cell proliferation. -
PI3K/Akt/mTOR Inhibitor
Veratramine is a selective inhibitor of the PI3K/Akt/mTOR signaling pathway and serves as a modulator of SIGMAR1. This compound facilitates autophagic apoptosis in tumor cells, effectively induces G0/G1 cell cycle arrest, and diminishes epithelial-mesenchymal transition (EMT) markers, thereby reducing tumor migration. Additionally, Veratramine exhibits neuroprotective effects by inhibiting SIGMAR1 interactions with NMDAR and the phosphorylation of NMDAR Ser896, resulting in reduced neurological damage in neuropathy models. Its diverse biological activities make it suitable for research on liver cancer, osteosarcoma, and diabetic peripheral neuropathy. -
PI3K/AKT Inhibitor
PI3K/AKT-IN-1 is a potent dual inhibitor of the PI3K/AKT signaling pathway, exhibiting IC50 values of 6.99 μM for PI3Kγ, 4.01 μM for PI3Kδ, and 3.36 μM for AKT. This compound demonstrates significant anticancer activity by disrupting the PI3K/AKT axis, leading to the induction of caspase-3 dependent apoptosis. It serves as a valuable tool for research in cancer biology and therapeutic development targeting the PI3K/AKT pathway. -
Akt Allosteric Inhibitor
AKT-IN-28 is an allosteric inhibitor of Akt, a key protein involved in cell survival and metabolism. It exhibits a binding affinity with a Kd of 2.07 μM and demonstrates the ability to significantly inhibit Akt activity. This compound induces apoptosis, arrests the cell cycle in the G2/M phase, and suppresses proliferation, migration, and metabolic processes in KRAS mutant colorectal cancer cells, making it a valuable tool for cancer research applications focused on targeting the Akt pathway. -
Akt1/Akt2 Inhibitor
Akt1/Akt2-IN-2 is an allosteric dual inhibitor targeting Akt1 and Akt2, exhibiting IC50 values of 138 nM and 212 nM, respectively. This compound enhances caspase-3 activity and effectively reduces the viability of various tumor cell lines. Its application in cancer research highlights its potential for investigating therapeutic strategies that disrupt Akt-mediated signaling pathways. -
fMLP inhibitor
Larixol is an fMLP inhibitor that also suppresses key signaling pathways involved in immune regulation, including Src kinase, ERK1/2, p38, and AKT phosphorylation. It disrupts the interaction between the βγ subunit of the fMLP receptor Gi protein and downstream effectors, thereby inhibiting fMLP-induced respiratory burst. Larixol effectively inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM), cathepsin G release (IC50: 2.76 μM), and neutrophil chemotaxis. It mitigates neutrophil hyperactivation and helps reduce inflammation and tissue damage. Additionally, Larixol derivatives have shown inhibitory activity against TRPC6 functional mutants associated with focal segmental glomerulosclerosis (FSGS). -
PI3K/Akt/mTOR inhibitor
PI3K/Akt/mTOR-IN-2 is an inhibitor of the PI3K/AKT/mTOR signaling pathway with demonstrated anticancer activity. It selectively inhibits the proliferation of MDA-MB-231 cells with an IC50 of 2.29 μM and induces cell cycle arrest and apoptosis, making it a promising candidate for cancer research. -
PGAM1 inhibitor
HKB99 is an allosteric inhibitor of phosphoglycerate mutase 1 (PGAM1) that induces apoptosis and suppresses cell migration by inhibiting the formation of invasive pseudopodia. It increases oxidative stress, activates the JNK/c-Jun pathway, and downregulates AKT and ERK signaling. HKB99 is a promising compound for the study of non-small cell lung cancer (NSCLC). -
ALK/ROS1 inhibitor
Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor that effectively blocks tyrosine autophosphorylation of ALK, mutant ALK, and EGFR, with IC50 values ranging from 5.38 to 16.74 nM. Additionally, it inhibits the transport activity of MATE1, MATE2K, P-gp, and BCRP. Iruplinalkib is under investigation for the treatment of non-small cell lung cancer (NSCLC). -
Endoplasmic Reticulum Stress Inhibitor
Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an inhibitor of endoplasmic reticulum (ER) stress that significantly downregulates pro-apoptotic molecules, including caspase-3 and caspase-12. Additionally, it suppresses ERK signaling, contributing to its cytoprotective and anti-apoptotic effects. -
Hsp90/HSV inhibitor
AT-533 is a potent inhibitor of heat shock protein 90 (Hsp90) and herpes simplex virus (HSV), exhibiting strong antitumor and antiviral activities. It suppresses tumor growth and angiogenesis by disrupting the HIF-1α/VEGF/VEGFR-2 signaling axis, a critical pathway in tumor vascularization and progression. Additionally, AT-533 inhibits key downstream signaling cascades, including Akt/mTOR/p70S6K, ERK1/2, and FAK pathways. In endothelial cells, specifically human umbilical vein endothelial cells (HUVECs), AT-533 effectively inhibits tube formation, cell migration, and invasion, highlighting its anti-angiogenic properties. These combined effects position AT-533 as a promising candidate for cancer therapy and angiogenesis-related disease research. -
Akt Inhibitor
2-Chlorophenoxazine is an Akt inhibitor with an IC50 value of 2-5 μM in vitro. This compound has been shown to induce apoptosis in various cancer cell lines. It is a valuable tool for research into cancerpathways and therapeutic strategies targeting Akt signaling. -
CIP2A and p-Akt Inhibitor
PP2A Cancerous-IN-1 is a strong and potent CIP2A (Cancerous inhibitor of PP2A) and p-Akt inhibitor. PP2A Cancerous-IN-1 shows the most potent antiproliferative activities. PP2A Cancerous-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. -
AKT Inhibitor
AKT-IN-14 free base is a highly potent inhibitor of the AKT family of serine/threonine kinases, demonstrating IC50 values of less than 0.01 nM, 1.06 nM, and 0.66 nM for AKT1, AKT2, and AKT3, respectively. This compound is valuable for research applications focused on cancer biology, particularly in studies investigating the role of AKT signaling in tumor progression and therapeutic resistance. -
Akt Inhibitor
DETD-35 is a potent inhibitor of the Akt signaling pathway, with additional effects on MEK-ERK and STAT3 pathways. It induces apoptosis in cancer cells and decreases their resistance to Vemurafenib. DETD-35 demonstrates effective inhibitory activity against various melanoma cell lines, with IC50 values of 2.5 to 6.0 μM across wild-type and mutant strains. This compound is a valuable tool for investigating mechanisms of anti-melanoma therapies. -
PI3K/AKT Pathways Inhibitor
Isocucurbitacin B selectively inhibits the PI3K/AKT signaling pathways, along with the MAPK and STAT3 pathways, demonstrating notable anti-cancer properties. This natural terpenoid, derived from Pedicellus melo, effectively suppresses cancer cell proliferation, migration, and invasion. Additionally, Isocucurbitacin B induces apoptosis and facilitates G2/M phase cell cycle arrest, while altering intracellular cholesterol and pH levels, and elevating intracellular calcium levels. It serves as a valuable reagent for research applications in cancer biology, particularly in the study of glioma. -
Akt Inhibitor
AM-9635 is a selective Akt inhibitor that targets the PI3Kδ pathway. It demonstrates significant in vitro and in vivo efficacy, effectively inhibiting PI3Kδ-dependent B cell receptor-mediated AKT phosphorylation. This compound has been shown to suppress the production of specific IgG and IgM antibodies in a rat model immunized with Aplysia leocyanin (KLH), making it useful for research applications in immunology and cancer biology. -
Akt Inhibitor
CCT129254 is a selective inhibitor of the Akt pathway, targeting the serine/threonine kinase Akt. This compound demonstrates significant reduction in melanoma cell motility in vivo, highlighting its potential utility in cancer research. CCT129254 may serve as a valuable tool for studying the role of Akt in tumor progression and therapeutic resistance. -
TrkA/Akt Inhibitor
HS-345 is a selective inhibitor of the TrkA/Akt signaling pathway, demonstrating significant anti-cancer effects in pancreatic cancer models. It inhibits the growth and proliferation of pancreatic cancer cells while inducing apoptosis. Moreover, HS-345 disrupts angiogenesis by downregulating the expression of HIF-1α and VEGF. This compound shows potential as a valuable tool for research into pancreatic cancer therapies. -
Akt Inhibitor
Uprosertib hydrochloride is a potent and selective pan-Akt inhibitor, characterized by IC50 values of 180 nM for Akt1, 328 nM for Akt2, and 38 nM for Akt3. This compound effectively modulates Akt signaling pathways, which are crucial in regulating cell growth, proliferation, and survival. Uprosertib hydrochloride is widely utilized in cancer research and therapeutic studies to explore potential treatments targeting the Akt pathway. -
Akt inhibitor
PX-316 is a selective Akt inhibitor that demonstrates the ability to phosphorylate Akt while leaving PDK1 and PKC phosphorylation unaffected. Notably, PX-316 also enhances the expression of various mitochondrial-related genes. This compound serves as a valuable tool for investigating pathways involved in colon and breast cancer research. -
PI3K/Akt/Ras/Raf/MAPK Inhibitor
Erufosine is a potent inhibitor of the PI3K/Akt and Ras/Raf/MAPK signaling pathways. It demonstrates significant cytotoxic activity against breast cancer cell lines, specifically MCF-7 and MDA-MB-231, with IC50 values of 40.95 μM and 40.8 μM, respectively. By reducing the phosphorylation levels of PI3K (p85), Akt (PKB), and cRaf, Erufosine serves as a valuable tool in the research of breast cancer and myeloid leukemia. -
PI3K/AKT/mTOR Inhibitor
PI3K/Akt/mTOR-IN-3 is a potent inhibitor targeting the PI3K/AKT/mTOR signaling pathway. It demonstrates significant biological activity, exhibiting IC50 values of 0.77 μM, 1.23 μM, and 4.57 μM in MCF-7, HeLa, and HepG2 cells, respectively. Additionally, this compound effectively inhibits the migration of MCF-7 and HeLa cells at a concentration of 4 μM, while also inducing apoptosis and causing cell cycle arrest in the S phase. This makes PI3K/Akt/mTOR-IN-3 a valuable tool for research in cancer biology and therapeutic development. -
AKT1 Inhibitor
Akt1-IN-8 is a selective inhibitor of AKT1 kinase, demonstrating high potency with an IC50 of 8.8 nM. This compound exhibits significant antiproliferative activity against PC-3 prostate cancer cells, with an IC50 of 3.0 μM. Akt1-IN-8 effectively reduces levels of phosphorylated GSK3β, making it a valuable tool for studying AKT signaling pathways in cancer research and therapeutic development. -
Akt Inhibitor
WF-10129 is a cytotoxic steroidal compound isolated from the plant Physalis. WF-10129 inhibits liver cancer cell proliferation, induces apoptosis, interferes with metabolism, and significantly reduces lactate production in vitro and in vivo. WF-10129 can also exert anti-tumor activity by regulating the expression of related genes and proteins through the AKT-p53 pathway. -
PI3K/AKT Inhibitor
PI3K/AKT-IN-3 is a selective inhibitor of the PI3K/AKT signaling pathway, known to induce both autophagy and apoptosis in various cell types. This compound is primarily utilized in cancer research to study the effects of PI3K/AKT inhibition on tumor growth and cell survival mechanisms. Its application extends to exploring therapeutic strategies targeting this critical signaling pathway in cancer treatment. -
Akt1 Inhibitor
Akt1-IN-6 is a potent Akt1 inhibitor with an IC50 of less than 15 nM. This compound selectively targets the Akt1 kinase, disrupting downstream signaling pathways involved in cell survival and metabolism. It is primarily used in research applications focused on cancer biology, metabolism, and other Akt-related pathways. Its high specificity for Akt1 makes it a valuable tool for studying the roles of this kinase in various disease processes. -
Akt Inhibitor
5,4'-Dihydroxy-6,8-dimethoxy-7-O-rhamnosyl flavone is a potent Akt inhibitor derived from Indigofera ovata. This compound effectively disrupts the PI3K/AKT and NF-κB signaling pathways, leading to the inhibition of cancer cell invasion and migration. Its biological activity supports research applications in cancer therapeutics and molecular signaling studies. -
Akt3 Inhibitor
Akt3 ligand-1 is a potent inhibitor of Akt3, exhibiting an IC50 of 0.1 nM. This compound serves as a ligand for the development of PROTAC strategies targeting Akt3, facilitating targeted protein degradation. Akt3 ligand-1 is invaluable for research into cancer biology and cellular signaling pathways where Akt3 plays a pivotal role. Additionally, it can be utilized to synthesize PROTAC Akt3 Degrader-1, enabling further exploration of therapeutic potentials in oncological studies. -
Akt1 Inhibitor
Akt1-IN-7 is a potent Akt1 inhibitor with an IC50 value of less than 15 nM. It effectively hinders the activity of Akt1, a key player in cell survival and growth signaling pathways. This compound is utilized in research focused on cancer biology, metabolic disorders, and other conditions where Akt1 signaling is implicated. Its selective inhibition of Akt1 makes it a valuable tool for elucidating the role of this kinase in various biological processes. -
Akt Inhibitor
Monosialoganglioside GM3 (bovine) is a ganglioside that functions as an Akt inhibitor, impacting both VEGFR2 and Akt signaling pathways. At a concentration of 20 μM, it effectively inhibits angiogenesis and decreases the proliferation and migration of human umbilical vein endothelial cells (HUVECs). Additionally, it protects against ferroptosis, which is relevant in the context of abdominal aortic aneurysm formation, and impairs insulin signaling by disrupting the insulin receptor-Caveolin-1 complex, contributing to insulin resistance in adipocytes. This reagent is applicable in cancer and metabolic disease research. -
AKT1-E17K Inhibitor
Akt1-IN-4 is a selective inhibitor of the AKT1-E17K mutant with an IC50 value of less than 15 nM. This compound effectively disrupts the activity of the AKT signaling pathway, which is implicated in various cancers. Akt1-IN-4 is suitable for research applications focused on studying the role of AKT1 mutations in tumorigenesis and therapeutic resistance. -
Akt Inhibitor
Puquitinib is a selective Akt inhibitor that effectively disrupts the PI3K/AKT/mTOR signaling pathway, promoting autophagy in nasopharyngeal carcinoma cells. This compound demonstrates a dose-dependent antiproliferative effect on CNE-2 cells, which is accompanied by increased autophagosome and autolysosome formation as confirmed by fluorescence and electron microscopy. Puquitinib enhances the conversion of LC3-I to LC3-II and elevates beclin 1 levels while decreasing p62 expression. Additionally, it induces apoptosis in CNE-2 cells, highlighting the interplay between autophagy and apoptosis in mediating cell death processes relevant to cancer research. -
Akt Inhibitor
TAT-TCL1-Akt-in is an Akt inhibitor that selectively modulates the Akt signaling pathway, which is crucial for cell proliferation and survival. By inhibiting Akt activity, this compound can effectively impact various cellular processes linked to tumorigenesis and cancer progression. TAT-TCL1-Akt-in is useful for research applications focused on cancer biology, signaling pathways, and therapeutic interventions targeting the Akt pathway. -
AKT Inhibitor
BI-69A11 is a selective AKT inhibitor that effectively suppresses the phosphorylation of AKT, disrupting the signaling pathways associated with cell survival and proliferation. This compound demonstrates significant anticancer activity, promoting apoptosis in melanoma and prostate tumor cells. It serves as a valuable tool for research in cancer biology and therapeutic development targeting the AKT pathway. -
mTOR/PI3/AKT Inhibitor
Royleanone, a diterpenoid isolated from plants, inhibits the proliferation of cancer cells by inducing cell cycle arrest and mitochondria-mediated apoptosis, also inhibits cell migration potential, inhibits mTOR/PI3/AKT signaling pathway in LNCaP prostate cancer cells. -
PI3K/Akt/FoxO3a Inhibitor
RLX hydrochloride is a potent inhibitor of the PI3K/Akt/FoxO3a signaling pathway, which plays a critical role in cellular growth and survival. This compound demonstrates significant therapeutic potential in experimental colon cancer by modulating the tumor microenvironment and enhancing the efficacy of cancer immunotherapy. Additionally, RLX hydrochloride can improve the retention of therapeutic agents within tumors when utilized with advanced nanoparticle delivery systems. It may also be effectively combined with other treatment modalities, such as chemotherapy and radiotherapy, to optimize overall cancer therapy outcomes. -
AKT Inhibitor
AKT-IN-9 is a potent inhibitor of AKT (Protein Kinase B), a key regulator of the PI3K/AKT/mTOR signaling pathway. This compound plays a critical role in processes such as cell growth, survival, differentiation, and metabolism. AKT-IN-9 is valuable for research applications focusing on breast and prostate cancer, contributing to a better understanding of tumor biology and potential therapeutic strategies.

