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Catalog No.
Product Name
Application
Product Information
Citations
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PI3Kδ Inhibitor
PI3Kδ-IN-11 is a potent and selective inhibitor of the PI3Kδ isoform, exhibiting an IC50 value of 27.5 nM. This compound effectively blocks the PI3K/Akt signaling pathway in a dose-dependent manner. PI3Kδ-IN-11 is particularly useful for studying B and T cell-related malignancies, providing valuable insights into therapeutic strategies targeting this pathway. -
AKT1 Inhibitor
AKT1-IN-10 is a non-covalent allosteric inhibitor of AKT1, exhibiting an IC50 of less than 500 μM. This compound demonstrates oral bioavailability, making it a viable candidate for in vivo studies. AKT1-IN-10 is primarily utilized in cancer research, providing insights into the modulation of AKT signaling pathways and their implications in tumor progression. -
AKT Inhibitor
AKT-IN-8 is a potent inhibitor of AKT, exhibiting IC50 values of 4.46 nM for AKT1, 2.44 nM for AKT2, and 9.47 nM for AKT3. This compound demonstrates significant inhibitory activity, making it a valuable tool for studying AKT signaling pathways. It is applicable in cancer research and investigations into the role of AKT in various cellular processes, including metabolism, proliferation, and survival. -
AKT Inhibitor
AKT-IN-10 is a selective inhibitor of AKT (Protein Kinase B), a crucial component of the PI3K/AKT/mTOR signaling pathway that regulates cell growth, survival, differentiation, and metabolism. This compound demonstrates significant potential for applications in cancer research, particularly in breast and prostate cancer studies, by effectively modulating AKT activity. Its ability to interfere with AKT signaling positions AKT-IN-10 as a valuable tool for investigating therapeutic strategies targeting these malignancies. -
PI3K-AKT Inhibitor
Alborixin is a potent inhibitor of the PI3K-AKT signaling pathway that promotes autophagy. It facilitates the clearance of intracellular and extracellular amyloid-β by upregulating key autophagy-related proteins such as BECN1, ATG5, and ATG7, while enhancing lysosomal activity. This mechanism yields a reduction in amyloid-β-mediated neurotoxicity, positioning Alborixin as a valuable tool for research related to Alzheimer's disease and other neurodegenerative conditions. -
APN/AKT Inhibitor
APN/AKT-IN-1 is a potent dual inhibitor targeting aminopeptidase N (APN) and protein kinase B (AKT), exhibiting IC50 values of 0.21 μM and 0.27 μM, respectively. This compound effectively blocks the phosphorylation of glycogen synthase kinase 3 beta (GSK3β), a critical substrate of AKT, thereby modulating key signaling pathways involved in cell growth, survival, and metabolism. APN/AKT-IN-1 is valuable for research applications focusing on cancer biology and therapeutic interventions targeting the APN/AKT pathway. -
Akt Inhibitor
TCL1(10-24) is a specific Akt inhibitor that targets the PH domain of Akt, disrupting its interaction with phosphoinositides. This inhibition prevents Akt's membrane translocation and subsequent activation, thereby hindering cellular proliferation and promoting apoptosis. TCL1(10-24) demonstrates significant antitumor activity in vivo, making it a valuable reagent for cancer research and studies focused on cell survival mechanisms. -
AKT1 Inhibitor
Akt1-IN-3 is a selective inhibitor of AKT1, demonstrating potent inhibition with an IC50 value of less than 15 nM against the AKT1-E17K mutant. This compound is valuable for research applications exploring the role of AKT signaling in various cancers and other diseases. Its potency and specificity make it an essential tool for studies aimed at understanding AKT1-related pathways and developing targeted therapies. -
PI3K/BRD4 Inhibitor
PI3Kα-IN-28 is a potent dual-target inhibitor of PI3K and BRD4. This compound effectively suppresses cell proliferation in various cancer cell lines, including KYSE180 and KYSE450, while also inhibiting migration and colony formation. Additionally, PI3Kα-IN-28 induces G0/G1 phase cell cycle arrest and promotes cellular senescence by enhancing the proportion of senescent cells. Mechanistically, it decreases the levels of p-AKT and c-Myc, while activating the AMPK-p27 pathway, making it a valuable tool for cancer research, particularly in esophageal cancer studies. -
Akt Phosphorylation Inhibitor
Antiangiogenic agent 4 is an Akt phosphorylation inhibitor that effectively disrupts the Akt signaling pathway in human foreskin fibroblast (HFF) and human umbilical vein endothelial cells (HUVEC). This compound demonstrates notable antiangiogenic activity, making it a valuable tool in cancer research aimed at understanding tumor growth and vascularization mechanisms. -
PI3K/AKT Inhibitor
PI3K/AKT-IN-2 is a selective inhibitor of the phosphoinositide 3-kinase (PI3K) and AKT signaling pathways. This compound effectively prevents epithelial-mesenchymal transition (EMT) and promotes apoptosis in various cancer cell lines. Additionally, PI3K/AKT-IN-2 has been shown to inhibit tubulin polymerization, making it a valuable tool for research into cancer metastasis and cell proliferation. -
PDK1/Akt/Flt Pathway Inhibitor
PDK1/Akt/Flt dual pathway inhibitor selectively targets the PDK1/Akt/Flt signaling pathways, crucial for cell survival and proliferation. This compound demonstrates significant inhibitory activity, making it a valuable tool for research in cancer biology and therapeutic development. It can be utilized to explore the roles of these pathways in oncogenesis and to assess potential therapeutic strategies against malignancies driven by aberrant PDK1/Akt/Flt signaling. -
Akt/PKA Inhibitor
Akt1&PKA-IN-1 is a potent dual inhibitor targeting both Akt and Protein Kinase A (PKA), exhibiting IC50 values of 0.03 μM for PKAα and 0.11 μM for Akt, with a higher IC50 of 9.8 μM for cyclin-dependent kinase 2 (CDK2). This compound demonstrates selective inhibition of CDK2, making it a valuable tool for research in cancer biology and cellular signaling pathways. Akt1&PKA-IN-1 is useful for studying the regulatory role of these kinases in cellular processes and potential therapeutic applications. -
PI3Kγ Inhibitor
TASP0415914 is a potent and orally active inhibitor of PI3Kγ, exhibiting an IC50 of 29 nM. In addition, it demonstrates significant inhibitory activity against Akt with an IC50 of 294 nM. This compound is applicable in research focused on inflammatory diseases and may provide insights into the modulation of signaling pathways involved in inflammation. -
PIM/PI3K/AKT/mTOR Inhibitor
IBL-302 is an orally available dual inhibitor targeting PIM and the PI3K/AKT/mTOR pathways. It exhibits significant antitumor activity against breast cancer and neuroblastoma, showing in vivo efficacy in nude mouse xenograft models by overcoming trastuzumab resistance. Additionally, IBL-302 enhances the cytotoxic effects of commonly used chemotherapeutic agents, including cisplatin, doxorubicin, and etoposide, making it a valuable compound for cancer research applications. -
Akt/mTOR Inhibitor
MKC-1 is an orally active and potent inhibitor targeting the Akt/mTOR signaling pathway. This compound exhibits broad antitumor activity by arresting cellular mitosis and inducing apoptosis. MKC-1 interacts with various cellular proteins, including tubulin and members of the importin β family, making it valuable for research in cancer cell cycle regulation and therapeutic mechanisms. -
Akt1 Inhibitor
24-Methylenecycloartanyl ferulate is identified as a potential ATP-competitive inhibitor of Akt1, with an EC50 value of 33.3 μM. This compound has been shown to promote the expression of parvin-beta in human breast cancer cells, suggesting its role in modulating important signaling pathways. As a research tool, it may be valuable for studying Akt1-related biological processes and their implications in cancer research. -
Src/Akt Inhibitor
Chrysotoxine is a dual inhibitor of the Src and Akt signaling pathways. It effectively suppresses cancer stem cell phenotypes by down-regulating the Src/Akt pathway, leading to reduced cell viability and increased apoptosis in H460 and H23 cancer cell lines, while sparing non-tumor cell lines. Due to its rapid excretion and low bioavailability in animal studies, Chrysotoxine serves as a valuable tool in cancer research, particularly for investigating therapies targeting cancer stem cells. -
AKT/mTOR Inhibitor
Dehydrovomifoliol is a dual inhibitor of the AKT/mTOR signaling pathway. It effectively reduces lipid accumulation and lipogenesis, making it a valuable reagent in the study of nonalcoholic fatty liver disease (NAFLD). The compound's targeted inhibition of AKT and mTOR provides insights into metabolic regulation and potential therapeutic strategies for liver-related disorders. -
PI3K/Akt/mTOR signaling pathway Inhibitor, TLR4 signaling Inhibitor
25(R,S)-Ruscogenin is a potent inhibitor of the PI3K/Akt/mTOR and TLR4 signaling pathways. This compound effectively suppresses hepatocellular carcinoma (HCC) metastasis by decreasing the expression of matrix metalloproteinases (MMP-2 and MMP-9), uPA, VEGF, and HIF-1α. Additionally, 25(R,S)-Ruscogenin mitigates LPS-induced apoptosis in pulmonary endothelial cells, highlighting its potential for applications in cancer research and inflammatory disease studies. -
p70S6K/Akt Inhibitor
M2698 is a selective inhibitor targeting p70S6K and Akt, functioning through an ATP-competitive mechanism. With IC50 values of 1 nM for both p70S6K and Akt1/Akt3, M2698 demonstrates potent inhibitory effects on these kinases. This compound is capable of crossing the blood-brain barrier, making it a valuable tool for research in cancer biology and potential therapeutic applications in neurologic conditions. -
Akt Inhibitor
AKT Kinase Inhibitor hydrochloride is a selective inhibitor of AKT kinase, primarily known for its anti-tumor properties. This compound demonstrates significant potential in cancer research by disrupting the AKT signaling pathway, which is often activated in various malignancies. Additionally, it features an alkyne functional group, facilitating its use in click chemistry applications, particularly in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with azide-containing molecules. -
Akt Inhibitor
AKT-IN-6 is a potent inhibitor of the AKT family of serine/threonine kinases, specifically targeting Akt1, Akt2, and Akt3 with IC50 values of less than 500 nM. This compound is widely utilized in biochemical research to elucidate the role of AKT signaling in various cellular processes, including cell growth, metabolism, and apoptosis. AKT-IN-6 serves as a valuable tool for investigating therapeutic approaches in cancer, diabetes, and neurodegenerative diseases where AKT activity is dysregulated. -
Akt Inhibitor
FPA-124 is a selective Akt inhibitor that operates by targeting both the pleckstrin homology (PH) and kinase domains of Akt. With an IC50 of 0.1 μM, FPA-124 demonstrates significant biological activity in promoting apoptosis. This compound is primarily utilized in research applications focused on cancer biology and signaling pathways associated with the Akt protein. -
Akt1 Inhibitor
A-674563 hydrochloride is a selective inhibitor of Akt1, exhibiting a Ki value of 11 nM. This compound effectively disrupts Akt1 signaling, making it a valuable tool for investigating the role of this kinase in cellular processes such as metabolism, survival, and proliferation. A-674563 hydrochloride is suitable for use in various research applications, including cancer research and studies focused on metabolic disorders. -
PI3K-Akt Inhibitor
(E)-Akt inhibitor-IV is a potent PI3K-Akt inhibitor that selectively targets the Akt signaling pathway. It demonstrates significant cytotoxic activity against various cancer cell lines, making it a valuable tool for studying tumor biology and therapeutic resistance. Research applications include investigating the role of Akt in cell proliferation, survival, and apoptosis in cancer models. -
AKT1 Inhibitor
Tanerasertib is an inhibitor of AKT1, specifically targeting the AKT1E17K mutant with an EC50 range of 15-60 nM. This compound exhibits significant biological activity that may be leveraged in cancer research, particularly in studies focusing on the role of the AKT signaling pathway in tumorigenesis and treatment resistance. Its application in preclinical models can provide insights into therapeutic strategies for cancers harboring AKT1 mutations. -
Akt Inhibitor
K-80003 is a potent Akt inhibitor that specifically targets and inhibits tRXRα-dependent Akt activation. This compound exhibits significant biological activity in suppressing cancer cell growth, making it valuable in cancer research. K-80003 is useful for studies investigating Akt signaling pathways and therapeutic strategies against malignancies. -
Akt Inhibitor
1-Formyl-beta-carboline is an alkaloid that functions as an Akt inhibitor, disrupting key signaling pathways. It demonstrates significant inhibitory activity against Newcastle disease virus (NDV), with IC50 values below 10 μM and over 90% inhibition at 20 μM concentration. The compound primarily targets the adsorption and entry phases of the NDV life cycle by directly interacting with the NDV hemagglutinin-neuraminidase (HN) protein. Additionally, 1-Formyl-beta-carboline affects viral entry through modulation of the PI3K/Akt signaling pathway. -
Akt Inhibitor
Hu7691 is a selective Akt inhibitor that exhibits potent inhibitory activity with IC50 values of 4.0 nM, 97.5 nM, and 28 nM against Akt1, Akt2, and Akt3, respectively. This compound has been shown to inhibit tumor growth while reducing cutaneous toxicity in mouse models, making it a valuable tool for cancer research. Its specificity and efficacy position Hu7691 as a promising reagent for studies focused on the Akt signaling pathway and its role in tumorigenesis. -
pan-AKT Inhibitor
Vevorisertib is a potent and selective pan-AKT serine/threonine kinase inhibitor, effectively targeting AKT1 (IC50=0.55 nM), AKT2 (IC50=0.81 nM), and AKT3 (IC50=1.31 nM). This orally active compound demonstrates significant biological activity in inhibiting AKT pathways and is applicable in the study of solid tumors harboring PIK3CA, AKT, or PTEN mutations. Vevorisertib can be utilized as a monotherapy or in combination with other anti-cancer agents for enhanced therapeutic efficacy in cancer research. -
PI3K Inhibitor
HL-8 is a potent PI3Kα degrader that functions through the targeted protein degradation mechanism of PROTAC technology. By promoting the ubiquitination and subsequent degradation of PI3Kα, HL-8 effectively reduces phospho-AKT levels, thereby interfering with key signaling pathways associated with cancer progression. This compound exhibits significant anticancer activity against colon and cervical cancer, making it a valuable tool for research in cancer biology and therapeutic development. -
Pan-PI3K Inhibitor
KTC1101 is a potent oral pan-PI3K inhibitor targeting the phosphoinositide 3-kinase (PI3K) signaling pathway. It effectively reduces downstream phosphorylation of AKT and mTOR, leading to decreased expression of Ki67. KTC1101 exhibits dual anti-tumor mechanisms by directly inhibiting tumor cell proliferation and enhancing the immune response, making it a valuable tool for cancer research and therapeutic applications. -
Akt Inhibitor
GSK2110183 analog 1 hydrochloride is a structural analogue designed to inhibit Akt, a critical signaling protein involved in various cellular processes such as growth, survival, and metabolism. This compound demonstrates potent Akt inhibitory activity, making it a valuable tool for studying the role of Akt in cancer progression and treatment. Its applications extend to exploring therapeutic strategies targeting the Akt pathway in various disease models. -
PI3K-Akt Inhibitor
AKT Inhibitor IV is a potent PI3K-Akt pathway inhibitor that selectively targets the E isomer. This compound exhibits significant cytotoxic effects, making it valuable for research applications focusing on cell proliferation, survival, and apoptosis. It is ideal for studies investigating the role of the PI3K-Akt signaling pathway in cancer and other diseases. -
AKT Inhibitor
CCT128930 hydrochloride is a selective inhibitor of AKT, demonstrating an IC50 of 6 nM. It exhibits significant selectivity, being 28-fold more potent against AKT than the closely related PKA kinase (IC50 of 168 nM) and 20-fold more effective than p70S6K (IC50 of 120 nM). CCT128930 hydrochloride is recognized for its ability to induce cell cycle arrest, promote DNA damage, and stimulate autophagy, enabling its application in cancer research and potential antitumor strategies. -
Allosteric Akt Inhibitor
Pifusertib is a selective, orally active allosteric inhibitor of Akt, exhibiting IC50 values of 4.8, 1.6, and 44 nM for Akt1, Akt2, and Akt3, respectively. This compound demonstrates significant anti-myeloma activity and intensifies lethal endoplasmic reticulum (ER) stress resulting from proteasome inhibition. In addition, Pifusertib promotes both apoptosis and autophagy, making it a useful tool for research in cancer biology and therapeutic development. -
Allosteric Akt Inhibitor
MK-2206 is a highly potent and selective allosteric inhibitor of the Akt signaling pathway, exhibiting IC50 values of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. This compound demonstrates significant anticancer activity, particularly in breast cancer cell lines and those harboring PIK3CA mutations or loss of PTEN function. MK-2206 is valuable for research investigating Akt's role in cancer progression and therapeutic resistance. -
AKT1/2 Inhibitor
Engasertib is a potent and selective inhibitor of AKT1 and AKT2, displaying IC50 values of 0.13 µM and 0.09 µM, respectively, with a slightly lower potency against AKT3 at 2.75 µM. This compound effectively inhibits AKT phosphorylation, leading to modulation of downstream signaling pathways in vitro. Due to its ability to suppress cancer cell proliferation and tumor growth, Engasertib serves as a valuable tool for cancer research and therapeutic development. -
PI3K/AKT/mTOR Inhibitor
Notoginsenoside Ft1 is a potent PI3K/AKT/mTOR inhibitor with significant bioactive properties. This compound induces apoptosis and lysosomal cell death in various cancer cell types by modulating key signaling pathways, such as p38 MAPK and ERK1/2, while promoting angiogenesis. Additionally, Notoginsenoside Ft1 enhances CD8+ T cell populations and exerts vasodilatory effects through glucocorticoid and estrogen receptor beta activation in endothelial cells. By acting as a TGR5 agonist and FXR antagonist, it may provide protective effects against renal injury and contribute to the management of obesity and insulin resistance through the modulation of intracellular calcium and cAMP levels. -
pan-AKT/AKT1-E17K Mutant Inhibitor
Vevorisertib trihydrochloride is a selective, allosteric inhibitor targeting pan-AKT and the AKT1-E17K mutant. It effectively inhibits AKT phosphorylation, demonstrating Kd values of 1.2 nM for AKT1 and 8.6 nM for AKT1-E17K, along with IC50 values of 0.55 nM, 0.81 nM, and 1.3 nM for AKT1, AKT2, and AKT3, respectively. This compound is valuable for cancer research, aiding in the exploration of therapeutic strategies targeting the AKT signaling pathway. -
Allosteric Akt Inhibitor
Pifusertib hydrochloride is a selective allosteric inhibitor of Akt, exhibiting IC50 values of 4.8 nM, 1.6 nM, and 44 nM for Akt1, Akt2, and Akt3, respectively. This compound demonstrates significant anti-myeloma activity by enhancing endoplasmic reticulum stress in the context of proteasome inhibition. Additionally, Pifusertib hydrochloride induces both apoptosis and autophagy, making it a valuable tool for research into cancer therapies and the modulation of cellular stress responses. -
PI3K/HDAC Inhibitor
PI3K/HDAC-IN-3 is a dual inhibitor targeting PI3K and HDAC, with IC50 values of 0.23 nM for PI3Kα and 172 nM for HDAC1. It effectively suppresses AKT phosphorylation while enhancing H3 acetylation in MV4-11 cells. Additionally, PI3K/HDAC-IN-3 demonstrates notable anticancer efficacy in a dose-dependent manner within an MV4-11 xenograft model, making it a valuable tool for studying cancer biology and potential therapeutic interventions. -
PI3Kα/HDAC6 Inhibitor
PI3Kα/HDAC6-IN-1 is a dual inhibitor targeting PI3Kα and HDAC6, exhibiting IC50 values of 2.9 nM and 26 nM, respectively. This compound effectively inhibits AKT (Ser473) phosphorylation and promotes the accumulation of acetylated α-tubulin, while not influencing acetylated histones H3 and H4. Its potent anti-cancer activity is demonstrated in the L-363 cell line with an IC50 of 0.17 μM, highlighting its potential for therapeutic applications in cancer research. -
PI3K Inhibitor
PI3K/HDAC-IN-1 is a potent dual inhibitor targeting phosphoinositide 3-kinase (PI3K) and histone deacetylase (HDAC). It effectively inhibits PI3Kδ and HDAC1 with IC50 values of 8.1 nM and 1.4 nM, respectively. This compound is valuable for studying the roles of PI3K and HDAC in various cellular processes and can aid in cancer research by exploring the therapeutic potential of dual inhibition in tumor models. -
PI3Kδ Inhibitor
FD223 is a potent and selective inhibitor of phosphoinositide 3-kinase delta (PI3Kδ), demonstrating an IC50 of 1 nM. It shows significant selectivity over other isoforms, with IC50 values of 51 nM, 29 nM, and 37 nM for α, β, and γ, respectively. FD223 effectively inhibits the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473, leading to G1 phase arrest in the cell cycle. This compound holds potential for research into leukemia, particularly AML. -
mTOR Inhibitor
2,6-Dihydroxyacetophenone primarily functions as an mTOR inhibitor. This polyphenolic derivative exhibits significant antioxidant activity and effectively inhibits cell growth and proliferation in colorectal cancer (CRC) cells by inducing apoptosis and arresting the cell cycle at the G0/G1 phase, while also suppressing cell migration. Additionally, 2,6-Dihydroxyacetophenone inhibits xanthine oxidase with an IC50 of 1.24 mM and enhances uric acid metabolism in hyperuricemic models. It further reduces plasma cholesterol levels in hypercholesterolemic rats and mitigates lipid accumulation in mice subjected to a high-fat diet. This compound is valuable for research into CRC, hyperuricemia, and hypercholesterolemia. -
mTORC1/2 Inhibitor
(+)–Usnic acid is a potent mTORC1/2 inhibitor derived from lichens, acting by binding to the ATP-binding pocket of mTOR. It effectively inhibits the phosphorylation of downstream effectors such as Akt (Ser473), 4EBP1, and S6K, thereby promoting autophagy and exhibiting both anti-cancer and anti-inflammatory properties. Additionally, (+)-Usnic acid demonstrates antimicrobial activity against several planktonic gram-positive bacteria, including Staphylococcus aureus, Enterococcus faecalis, and Enterococcus faecium, making it a valuable tool for various biological research applications. -
PI3K/HDAC Inhibitor
PI3K/HDAC-IN-2 is a potent dual inhibitor of phosphoinositide 3-kinase (PI3K) and histone deacetylase (HDAC), demonstrating IC50 values of 226 nM for PI3Kα, 279 nM for PI3Kβ, 467 nM for PI3Kγ, and 29 nM for PI3Kδ. It also exhibits selective inhibition with IC50 values of 1.3 nM for HDAC1, 3.4 nM for HDAC2, 972 nM for HDAC4, 17 nM for HDAC6, and 12 nM for HDAC8. Due to its significant anticancer properties, PI3K/HDAC-IN-2 is valuable for research applications in cancer biology and therapeutic development. -
mTOR/HDAC Inhibitor
mTOR/HDAC-IN-1 is a dual inhibitor targeting mTOR and HDAC, exhibiting IC50 values of 0.49 nM and 0.91 nM for mTOR and HDAC1, respectively. This compound demonstrates significant anti-cancer activity, making it a valuable tool for research in cancer therapeutics and signaling pathways. Its selective inhibition profile offers potential for elucidating the roles of mTOR and HDAC in tumorigenesis and for developing novel cancer treatment strategies.
