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Catalog No.
Product Name
Application
Product Information
Citations
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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 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. -
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. -
PI3Kδ Inhibitor
LAS195319 is a potent and orally active inhibitor of PI3Kδ, exhibiting an IC50 of 0.5 nM. This compound demonstrates high selectivity against a wide array of proteins, lipid kinases, and GPCRs. LAS195319 effectively inhibits the infiltration of neutrophils and eosinophils, making it a valuable tool for research into respiratory diseases, including asthma and chronic obstructive pulmonary disease (COPD). -
PI3Kδ Inhibitor
IHMT-PI3Kδ-372 is a highly selective inhibitor of PI3Kδ, exhibiting an IC50 of 14 nM. This compound demonstrates significant selectivity over other class I PI3Ks, with 56 to 83-fold differences, as well as over various protein kinases. IHMT-PI3Kδ-372 is suitable for research applications related to chronic obstructive pulmonary disease (COPD), enabling investigations into therapeutic strategies targeting this pathway. -
PI3K Inhibitor
Isopsoralidin is a phosphatidylinositol 3-kinase (PI3K) inhibitor that demonstrates potentially hepatotoxic properties and exhibits inhibitory activity on CYP2D6. This compound plays a significant role in research focused on cell signaling pathways related to cancer and metabolic disorders. Its unique mechanism of action makes it a valuable tool for studying PI3K-related biological processes and evaluating therapeutic approaches involving PI3K modulation. -
Dual PI3K/mTOR Inhibitor
PKI-179 is a highly effective dual inhibitor of PI3K and mTOR, exhibiting IC50 values of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ, and mTOR, respectively. It demonstrates significant activity against E545K and H1047R mutant isoforms, with IC50 values of 14 nM and 11 nM. PKI-179 is utilized in cancer research due to its proven anti-tumor efficacy in vivo, making it a valuable tool for investigating the PI3K/mTOR signaling pathway in various cancer models. -
PI3K/mTOR Inhibitor
PI3K/mTOR Inhibitor-4 is a potent orally active pan-class I PI3K/mTOR inhibitor. It demonstrates enzymatic inhibition across PI3Kα, PI3Kγ, PI3Kδ, and mTOR with IC50 values of 0.63 nM, 22 nM, 9.2 nM, and 13.85 nM, respectively. This reagent is primarily utilized in cancer research to investigate the role of the PI3K/mTOR signaling pathway in tumorigenesis and therapeutic responses. -
PI3K/mTOR Inhibitor
PI3K/mTOR Inhibitor-11 is a potent oral inhibitor of the PI3K/mTOR signaling pathway, exhibiting IC50 values of 3.5 nM, 4.6 nM, and 21.3 nM for PI3Kα, PI3Kδ, and mTOR, respectively. This compound effectively impairs the phosphorylation of AKT and S6 proteins, thereby modulating critical cellular processes. PI3K/mTOR Inhibitor-11 is valuable for cancer research, offering insights into therapeutic strategies targeting aberrant signaling in tumors. -
PI3K/mTOR Inhibitor
DS-7423 is a potent dual inhibitor of PI3K and mTOR, exhibiting IC50 values of 15.6 nM for PI3Kα and 34.9 nM for mTOR. This compound demonstrates significant anti-tumor activity, making it a valuable tool for research into cancer biology and potential therapeutic strategies. Its ability to inhibit key signaling pathways involved in cell growth and survival positions DS-7423 as a promising candidate for further exploration in oncology studies. -
PI3K/mTOR Inhibitor
PI3K-IN-37 is a potent inhibitor of the PI3K family, specifically targeting PI3K α, β, and δ isoforms with IC50 values of 6, 8, and 4 nM, respectively. Additionally, PI3K-IN-37 demonstrates strong inhibition of mTOR with an IC50 of 4 nM. This compound is valuable for research applications involving cancer biology, metabolic disorders, and signaling pathways related to cell growth and survival. -
PI3Kα/mTOR Kinase Inhibitor
PI3K-IN-22 is a potent dual inhibitor of the PI3Kα and mTOR kinases, with IC50 values of 0.9 nM and 0.6 nM, respectively. This compound exhibits substantial biological activity, making it valuable for investigating the roles of these pathways in cancer research. PI3K-IN-22 can facilitate the study of tumor growth and response to therapy, contributing to the understanding of oncogenic signaling and potential treatment strategies. -
Dual PI3K/mTOR Inhibitor
PKI-179 hydrochloride is a potent dual inhibitor of the PI3K and mTOR signaling pathways, demonstrating IC50 values of 8 nM for PI3K-α, 24 nM for PI3K-β, 74 nM for PI3K-γ, 77 nM for PI3K-δ, and 0.42 nM for mTOR. This compound is effective against mutant variants E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride has been shown to exhibit significant anti-tumor activity in vivo, making it a valuable tool for cancer research and therapeutic development targeting PI3K/mTOR pathways. -
PI3K/mTOR Inhibitor
SN32976 is a potent and selective inhibitor of class I phosphoinositide 3-kinases (PI3K) and mTOR, exhibiting IC50 values of 15.1 nM for PI3Kα, 461 nM for PI3Kβ, 110 nM for PI3Kγ, 134 nM for PI3Kδ, and 194 nM for mTOR. This compound demonstrates significant selectivity against a wide panel of 442 kinases. SN32976 is primarily utilized in cancer research, showcasing notable anticancer activity that makes it a valuable tool for studying PI3K/mTOR pathway modulation. -
PI3K/mTOR Inhibitor
PI3K/mTOR Inhibitor-13 sodium is a dual inhibitor targeting phosphoinositide 3-kinase (PI3K) and mTOR kinase, demonstrating oral bioavailability. This compound exhibits significant biological activity in the modulation of cellular growth and metabolism, making it a valuable tool in research related to sexual dysfunction, solid tumors, and idiopathic pulmonary fibrosis (IPF). Its dual inhibition profile presents opportunities for therapeutic exploration in various disease contexts. -
PI3K/mTOR inhibitor
PI3K-IN-18 is a potent inhibitor of the PI3K/mTOR signaling pathway, selectively targeting PI3K-α and mTOR with IC50 values of 41 nM and 49 nM, respectively. This compound exhibits significant biological activity by disrupting key signaling processes involved in cell growth and proliferation. PI3K-IN-18 is valuable for research applications focused on cancer biology, metabolism, and therapeutic strategies targeting the PI3K/mTOR axis. -
PI3K Inhibitor
PI3Kα/mTOR-IN-1 is a selective dual inhibitor targeting PI3Kα and mTOR, exhibiting an IC50 of 7 nM for PI3Kα in cellular assays. It demonstrates Kis of 10.6 nM and 12.5 nM for mTOR and PI3Kα in cell-free assays, respectively. This compound is instrumental in studies related to cancer biology and signal transduction, making it valuable for research involving the modulation of PI3K/mTOR pathways. -
PI3K/mTOR Inhibitor
PI3K/mTOR Inhibitor-9 is a potent inhibitor targeting both the PI3K and mTOR pathways, exhibiting IC50 values of 38 nM for mTOR (in phospho-S6 cellular assays) and 6.6 μM, 6.6 μM, and 0.8 μM for PI3Kα, PI3Kγ, and PI3Kδ, respectively. This compound demonstrates significant biological activity in modulating cellular growth and metabolism, making it a valuable tool for research on cancer and other diseases characterized by dysregulated PI3K/mTOR signaling. Its application in various cellular models facilitates the exploration of therapeutic strategies in oncology and other fields of biomedical research. -
PI3K/mTOR Inhibitor
PI3K/mTOR Inhibitor-5 selectively targets both phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR), demonstrating IC50 values of 86.9 nM for PI3K and 14.6 nM for mTOR. This dual inhibition has significant implications for cancer research, as it can effectively impede cell proliferation and survival in tumor cells. PI3K/mTOR Inhibitor-5 is suitable for studies investigating the PI3K/mTOR signaling pathway and its role in various diseases, particularly in the contexts of oncology and metabolic disorders. -
PI3K/mTOR Inhibitor
PI3K/mTOR Inhibitor-3 is a potent dual inhibitor of phosphoinositide 3-kinase (PI3K) and mechanistic target of rapamycin (mTOR). This imidazoline derivative exhibits significant anti-cancer activity, making it a valuable tool for cancer research. Its ability to modulate key signaling pathways related to cell growth and survival enhances its utility in studying tumor biology and therapeutic strategies. -
PI3Kα/mTOR Inhibitor
PI3Kα-IN-5 is a potent inhibitor of the PI3Kα and mTOR pathways, exhibiting IC50 values of 0.7 nM and 3.3 nM, respectively. This compound is valuable for research focused on colorectal cancer, offering insights into the modulation of these critical signaling pathways. Its specificity and efficacy make it an important tool for investigating the roles of PI3Kα and mTOR in cancer biology. -
PI3K/mTOR Inhibitor
PI3K/mTOR Inhibitor-12 is a selective inhibitor targeting the phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) pathways, exhibiting IC50 values of 0.06 nM for PI3Kα and 3.12 nM for mTOR. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Additionally, PI3K/mTOR Inhibitor-12 has been shown to possess reduced liver toxicity, enhancing its potential for therapeutic applications in oncology. -
PI3K/mTOR Inhibitor
PI3K/mTOR Inhibitor-8 is a potent dual inhibitor of PI3K and mTOR, exhibiting IC50 values of 0.46 nM and 12 nM against PI3Kα and mTOR, respectively. This compound promotes apoptosis in HCT-116 cells and effectively induces cell cycle arrest at the G1/S phase. It serves as a valuable tool for researchers investigating the roles of PI3K and mTOR signaling in cancer biology and potential therapeutic interventions. -
PI3K Inhibitor
MCX 28 is a potent inhibitor of the phosphoinositide 3-kinase (PI3K) pathway, functioning as a triple inhibitor of PI3K, mTOR, and PIM kinases. It exhibits low nanomolar activity, making it a valuable tool for studying signaling pathways involved in cancer and other diseases. This compound is particularly useful for research applications focused on the modulation of cell proliferation, survival, and metabolic processes. -
PI3K/mTOR Inhibitor
PI3K/mTOR-IN-18 is a highly selective dual inhibitor targeting PI3Kα and mTOR, with binding affinities of Ki=0.130 nM and Ki=0.111 nM, respectively. This compound effectively blocks the PI3K/AKT/mTOR signaling pathway, resulting in significant inhibition of tumor cell proliferation (IC50=144 nM). PI3K/mTOR-IN-18 is suitable for research involving various solid tumors, including breast cancer and non-small cell lung cancer (NSCLC). -
PI3K/mTOR Inhibitor
PI3K/mTOR Inhibitor-14 is a dual inhibitor targeting phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR), exhibiting IC50 values of 171.4 nM and 10.1 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its inhibition of the PI3K/mTOR signaling pathway can be critical for studies focused on cell proliferation and survival in various cancer models. -
PI3K/mTOR Inhibitor
PI3K/mTOR Inhibitor-7 (Compound 19i) is a potent dual inhibitor targeting the PI3K and mTOR pathways. It demonstrates a 4.7-fold increased potency compared to the positive control gedatolisib, with an IC50 of 0.3 μM. At a concentration of 10 μM, PI3K/mTOR Inhibitor-7 effectively suppresses the PI3K/Akt/mTOR signaling pathway. This compound is valuable for research applications focused on cancer biology and related therapeutic development. -
PI3K/mTOR Inhibitor
PI3K/mTOR Inhibitor-6 is a potent dual inhibitor targeting the phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) pathways. This compound demonstrates enhanced stability in artificial gastric fluids compared to other PI3K/mTOR inhibitors. At a concentration of 10 μM, PI3K/mTOR Inhibitor-6 effectively suppresses the PI3K/Akt/mTOR signaling pathway, highlighting its potential for cancer research applications. -
PI3K inhibitor
PI-540 is a bicyclic thienopyrimidine derivative that functions as an orally active inhibitor of phosphoinositide 3-kinases (PI3K). Demonstrating potent anti-cancer cell proliferation activity, PI-540 selectively inhibits various PI3K isoforms with IC50 values of 10 nM for P110α, 3510 nM for P110β, 410 nM for P110δ, and 33110 nM for P110γ. In addition to its PI3K inhibition, PI-540 also targets mTOR and DNA-PK, with IC50 values of 61 nM and 525 nM, respectively, making it a valuable tool for cancer research and therapeutic development.
