Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
PI3K/AKT/BMP-2/p38/ERK 1/2 Modulator
Asperosaponin V is an indirect modulator of key signaling pathways, including PI3K/AKT, BMP-2/p38, and ERK 1/2. This compound stimulates the proliferation of marrow stromal cells and promotes differentiation into osteoblasts, making it valuable for studying bone metabolism. Asperosaponin V holds potential for applications in osteoporosis research and fracture healing studies. -
PI3K/AKT/mTOR Modulator
Anticancer agent 235 is a modulator of the PI3K/AKT/mTOR signaling pathway. It promotes reactive oxygen species (ROS) generation and decreases mitochondrial membrane potential, leading to reduced proliferation of cancer cell lines including HCT116, Caco-2, AGS, and SMMC-772 with IC50 values ranging from 0.35 to 26.9 μM. Furthermore, Anticancer agent 235 effectively induces G2/M cell cycle arrest and apoptosis in HCT116 cells, making it a valuable tool for cancer research applications. -
PI3K/AKT Activator
Monomethyl lithospermate serves as a PI3K/AKT pathway activator, which is crucial for neuroprotection following nerve injury. This compound enhances the viability of SH-SY5Y neuroblastoma cells by preserving mitochondrial membrane potential and inhibiting apoptosis. Additionally, monomethyl lithospermate reduces oxidative stress in brain tissue of rats subjected to middle cerebral artery occlusion, demonstrating efficacy in mitigating nerve damage associated with ischemic stroke. -
PI3Kδ Inhibitor
PI3Kδ-IN-24 is a highly selective inhibitor of the phosphoinositide 3-kinase delta (PI3Kδ) with an IC50 of 0.1 nM. This compound demonstrates notable antiproliferative effects in cancer cell lines with elevated PI3Kδ expression. By inhibiting PI3Kδ, PI3Kδ-IN-24 effectively lowers phosphorylated AKT levels and promotes cell cycle arrest and apoptosis in tumor cells. Its applications are particularly relevant in cancer research, including studies involving diffuse large B-cell lymphoma (DLBCL). -
PI3Kδ Inhibitor
X-370 is a PI3Kδ inhibitor (IC50 = 7 nM). X-370 inhibits the survival of leukemia cells, inducing G1 arrest and apoptosis. X-370 blocks PDK1 binding and phosphorylation of MEK1/2, eliminating Akt and Erk1/2 signaling. X-370 can be used in research on B-cell acute lymphoblastic leukemia (B-ALL). -
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. -
PI3K Inhibitor
PI3K-IN-4 is a potent Pan-PI3K inhibitor. PI3K-IN-4 has high activity for three PI3K isoforms with the IC50 values of picomole. PI3K-IN-4 shows superior inhibitory activity against PI3Kα (IC50 = 0.20 nM), PI3Kβ (IC50 = 2.99 nM), PI3Kδ (IC50 = 0.48 nM) and PI3Kγ (IC50 = 0.58 nM) and has no significant activity against EGFR. PI3K-IN-4 inhibits cancer cell growth though PI3K/Akt signaling pathway, leading to the inhibition of colony formation and the induction of apoptosis. PI3K-IN-4 can be used for lung, colon and breast cancer research. -
PI3K Inhibitor
PI3K-IN-29 is a potent inhibitor of Phosphoinositide 3-kinase (PI3K), effectively disrupting the PI3K/Akt signaling pathway. It demonstrates significant cytotoxic activity against various cancer cell lines, including U87MG, HeLa, and HL60, with IC50 values of 0.264 µM, 2.04 µM, and 1.14 µM, respectively. This compound is valuable for research applications involving cancer biology and therapeutic interventions targeting the PI3K pathway. -
PI3K/Akt Inhibitor
Acetyl-Exenatide is an acetylated derivative of Exenatide, targeting the PI3K/Akt signaling pathway. This compound exhibits insulin-mimetic properties and is instrumental in type 2 diabetes research. Acetyl-Exenatide promotes Th17 differentiation while inhibiting Treg differentiation, and downregulates the phosphorylation of PI3K/Akt/FoxO1, making it a valuable tool for elucidating mechanisms underlying metabolic disorders. -
PI3K p110α Inhibitor
VVD-484 is a selective inhibitor targeting PI3K p110α, exhibiting an IC50 of 0.59 μM against human targets. Classified as a "silent ligand," it forms a covalent bond with Cys242 of PI3K p110α, maintaining the p110α-KRASG12C interaction. VVD-484 effectively inhibits AKT phosphorylation at S473 via a RAS-independent pathway, making it a valuable tool in the research of HER2-overexpressing cancers. -
PI3K Inhibitor
PI3K-IN-56 is a potent and selective irreversible inhibitor of phosphoinositide 3-kinase (PI3K), exhibiting oral bioavailability. This compound effectively blocks the production of phosphatidylinositol-3,4,5-triphosphate (PIP3) and disrupts downstream AKT signaling pathways. Its potential applications in cancer research make PI3K-IN-56 particularly valuable for studies focusing on PI3Kα-driven malignancies, including breast and ovarian cancers. -
PI3K/Akt/mTOR Inhibitor、MAPK Inhibitor、NF-κB Inhibitor
Calebin A is a potent inhibitor of the PI3K/Akt/mTOR pathway, as well as MAPK and NF-κB signaling pathways. It exhibits significant anti-tumor activity through epigenetic regulation and can suppress apoptosis while inhibiting autophagy. Additionally, Calebin A modulates adipogenesis, enhances thermogenic processes, and supports gut microbiota. This compound is suitable for research in various domains, including osteoarthritis, Alzheimer's disease, type 2 diabetes, malignant peripheral nerve sheath tumors, and colorectal cancer. -
PI3Kδ Inhibitor
PI3Kδ-IN-10 is a potent and orally bioavailable inhibitor of the PI3Kδ enzyme, exhibiting an IC50 value of 2 nM. This compound effectively inhibits the downstream AKT signaling pathway, leading to the induction of apoptosis in hepatocellular carcinoma models. Due to its mechanism of action, PI3Kδ-IN-10 is valuable for investigating the role of PI3Kδ in cancer biology and therapeutic development. -
PI3K/Akt/FoxO3a Inhibitor
RLX (PD 139530) is a potent inhibitor of the PI3K/Akt/FoxO3a signaling pathway, exhibiting significant therapeutic potential in colon cancer models. This compound can effectively modulate the tumor microenvironment, thereby enhancing the efficacy of cancer immunotherapy. Additionally, RLX improves the retention time of therapeutic agents in tumors through advanced nanoparticle delivery systems and can be combined with various treatment modalities, such as chemotherapy and radiotherapy, to synergistically enhance cancer treatment outcomes. -
Dual PI3K/mTOR Inhibitor
DHW-221 is a potent dual inhibitor of PI3K and mTOR, demonstrating low nanomolar potency across all four Class I PI3K isoforms (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM) and mTOR (IC50 = 3.9 nM). This compound exhibits significant antitumor activity by disrupting the PI3K/Akt/mTOR signaling pathway, promoting mitochondrial apoptosis and paraptosis via endoplasmic reticulum stress and MAPK signaling, while also hindering cell cycle progression, migration, invasion, and angiogenesis. DHW-221 serves as a valuable tool in research related to non-small cell lung cancer (NSCLC), colon cancer, and breast cancer. -
PI3K Inhibitor
Zandelisib hydrochloride is a selective, non-covalent inhibitor of PI3Kδ, known for its oral bioavailability. By effectively inhibiting AKT phosphorylation, Zandelisib hydrochloride disrupts downstream signaling pathways, making it a valuable tool for investigating the role of the PI3K pathway in various malignancies. This compound is particularly relevant in research focused on relapsed and refractory B-cell lymphoma, enabling studies on tumor behavior and therapeutic responses. -
PI3K/AKT Inhibitor
PI3K/AKT-IN-5 is a selective inhibitor of the PI3K/AKT signaling pathway. It demonstrates potent anti-cancer activity, particularly in colorectal cancer models, by significantly inhibiting cell colony formation, inducing G2/M phase cell cycle arrest, and promoting apoptosis. This compound serves as a valuable tool for research into the mechanisms of colorectal cancer progression and treatment. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
PI3K/Akt Activator
Hydroxy celecoxib is a derivative of Celecoxib that functions as a PI3K/Akt signaling activator, facilitating epithelial repair processes. Its activation of the PI3K/Akt pathway supports cellular survival and proliferation, making it a valuable tool for investigating mechanisms of tissue regeneration. Hydroxy celecoxib is particularly relevant in asthma research, where it may contribute to understanding airway epithelial function and repair. -
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. -
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. -
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. -
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. -
PI3K/mTOR Inhibitor
Dactolisib hydrochloride is a potent dual inhibitor of class I phosphoinositide 3-kinases (PI3K) and the mammalian target of rapamycin (mTOR), specifically targeting p110α, p110γ, p110δ, and p110β with IC50 values of 4 nM, 5 nM, 7 nM, 75 nM, and 20.7 nM, respectively. This compound effectively inhibits both mTORC1 and mTORC2, making it a valuable tool for studying the PI3K/mTOR signaling pathway. Its applications include cancer research, drug development, and exploring therapeutic strategies for various diseases associated with dysregulated PI3K/mTOR signaling. -
PI3Kδ/BET Inhibitor
PI3Kδ/BET-IN-1 is a selective inhibitor targeting both PI3Kδ and the bromodomain BRD4-BD1. With an IC50 of 112 nM for PI3Kδ and 19 nM for BRD4-BD1, this compound demonstrates potent antiproliferative effects in diffuse large B-cell lymphoma (DLBCL) cells. Its dual inhibition mechanism makes it a valuable tool for research into cancer biology and therapeutic development. -
PI3K/Akt Inhibitor, MAPK Inhibitor, NF-κB Inhibitor, Nrf2/ARE Activator
JRN73958 is a potent inhibitor of the PI3K/Akt, MAPK, and NF-κB signaling pathways. This compound effectively reduces LPS/IFNγ-induced activation of these pathways, making it a valuable tool for investigating their roles in cancer biology, particularly in leukemia research. Additionally, JRN73958 acts as an Nrf2/ARE activator, further expanding its utility in studies related to oxidative stress and cell survival mechanisms. -
MAPK/PI3K Antagonist
ST-162 is a dual antagonist of the MAPK and PI3K signaling pathways. It demonstrates significant antitumor activity and has been shown to enhance the efficacy of immune checkpoint inhibitors. This compound is suitable for cancer research, particularly in the study of melanoma and other malignancies. -
PI3K/PIKK Inhibitor
PI3K/PIKK-IN-1 is a potent inhibitor of phosphoinositide 3-kinases (PI3K) and PI3-kinase-related kinases (PIKK). This compound is utilized in the development of antibody-drug conjugates (ADCs), making it valuable for therapeutic applications. It is particularly relevant in the research of various cancers, including breast cancer, multiple myeloma, Burkitt lymphoma, diffuse large B-cell lymphoma, and non-small cell lung cancer, aiding in the exploration of targeted cancer therapies. -
PI3Kα Inhibitor
PI3Kα-IN-16 is a selective PI3Kα inhibitor with an IC50 value of 4.28 μM. It effectively suppresses PI3K-mediated colorectal cancer growth and migration, demonstrating its potential as a therapeutic agent. Additionally, PI3Kα-IN-16 inhibits the Wnt signaling pathway, making it a valuable tool for research in cancer biology and signaling pathways. -
PI3K Inhibitor
ETP-45658 is a potent inhibitor of the phosphoinositide 3-kinase (PI3K) family, exhibiting IC50 values of 22.0 nM for PI3Kα, 39.8 nM for PI3Kδ, 129.0 nM for PI3Kβ, and 717.3 nM for PI3Kγ. Additionally, ETP-45658 demonstrates inhibitory effects on DNA-PK (IC50 = 70.6 nM) and mTOR (IC50 = 152.0 nM). This compound is valuable for cancer research, particularly in exploring the roles of PI3K signaling pathways in tumorigenesis and treatment resistance. -
PI3Kδ Inhibitor
PI3Kδ-IN-27 is a selective inhibitor of PI3Kδ, exhibiting an IC50 value of 355.3 nM. This compound demonstrates notable antiviral activity against SARS-CoV-2, making it a valuable tool for studying viral infections, particularly COVID-19. Researchers can utilize PI3Kδ-IN-27 to explore pathways related to immune response and infection mechanisms. -
PI3Kα Inhibitor
VVD-442 is a selective inhibitor of PI3Kα that covalently binds to cysteine 242 within the RAS-binding domain of the PI3K p110α subunit. This binding induces conformational changes that disrupt the interaction between PI3K p110α and RAS proteins, effectively blocking RAS-mediated activation of PI3K. VVD-442 is applicable in research focusing on RAS-mutant cancers and HER2-overexpressing tumors, providing valuable insights into therapeutic strategies targeting these pathways. -
MEK/PI3K Inhibitor
MEK/PI3K-IN-2 is a potent inhibitor targeting both MEK and PI3K pathways, exhibiting IC50 values of 352 nM for MEK1, 107 nM for PI3Kα, and 137 nM for PI3Kδ. This compound effectively reduces levels of phosphorylated AKT and ERK1/2, demonstrating significant anti-proliferative activity against various tumor cell lines. MEK/PI3K-IN-2 is valuable for research in cancer biology and therapeutic development aimed at disrupting these critical signaling pathways. -
MEK/PI3K Inhibitor
MEK/PI3K-IN-1 is a potent inhibitor targeting MEK and PI3K pathways, exhibiting IC50 values of 124 nM for MEK1, 130 nM for PI3Kα, and 236 nM for PI3Kδ. This compound effectively reduces levels of phosphorylated AKT (pAKT) and ERK1/2 (pERK1/2), demonstrating significant anti-proliferative effects in various tumor cell lines. MEK/PI3K-IN-1 serves as a valuable tool for research in cancer therapeutics and signaling pathway analysis. -
PI3Kγ Inhibitor
SH-273 is a potent dual-function compound that acts as a selective inhibitor of PI3Kγ with an IC50 of 7 nM while also stimulating STING function with an EC50 of 100 nM. This unique profile makes SH-273 a valuable tool for investigating signaling pathways involved in pancreatic cancer. Researchers can utilize SH-273 to explore the therapeutic potential of targeting PI3Kγ and enhancing STING-mediated immune responses in cancer models. -
COX-2/PI3K Inhibitor
COX-2/PI3K-IN-2 is a potent inhibitor targeting both COX-2 and PI3K pathways, exhibiting an IC50 value of 2.78 nM for PI3K and a Ki value of 3.02 nM for COX-2. This compound demonstrates significant anti-inflammatory and anti-cancer activities, making it valuable for research in oncology and inflammatory disease studies. Its dual-target mechanism provides insights into the therapeutic potential of modulating these critical pathways.
