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Catalog No.
Product Name
Application
Product Information
Citations
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PI3Kα Inhibitor
PI3Kα-IN-22 is a potent and selective inhibitor of the PI3KαH1047R mutant, demonstrating an IC50 of 1 nM in the pAKT T47D AlphaLISA assay. This orally active compound has shown the ability to induce tumor regressions in the HCC1954 mouse model, making it a valuable tool for studying PI3Kα-related pathways in cancer research and therapeutic development. Its specificity and efficacy support its use in investigations aimed at targeting PI3Kα-driven malignancies. -
PI3Kβ Inhibitor
TGX-155 is a selective inhibitor of PI3Kβ, a key enzyme involved in the phosphoinositide 3-kinase signaling pathway. This compound exhibits significant antithrombotic activity, making it a potential therapeutic agent for the treatment of thrombotic disorders. Its application in research may enhance the understanding of PI3Kβ-related mechanisms in cardiovascular biology and drug development. -
PI3K Inhibitor
PI3K-IN-51 is a potent inhibitor of the phosphoinositide 3-kinase (PI3K) pathway, exhibiting IC50 values below 500 nM for the p120γ and p110δ/p85α isoforms. This compound is crucial for investigating the role of PI3K in cellular processes such as growth, proliferation, and survival. It has applications in cancer research and other fields where PI3K signaling plays a significant role in disease progression. -
PI3K Inhibitor
PF-376304 is an orally active, non-specific class I phosphoinositide 3-kinase (PI3K) inhibitor, exhibiting an IC50 of 0.197 μM against PI3Kγ. This compound is shown to induce dose-dependent metabolic disorders related to glucose and lipid metabolism in animal models, with rapid lethality observed at elevated doses. Additionally, metabolic abnormalities induced at lower doses demonstrate self-reversibility. PF-376304 is valuable for research into metabolic and inflammatory diseases, providing insights into PI3K involvement in these pathological conditions. -
PI3Kδ Inhibitor
(R)-IHMT-PI3Kδ-372 is a selective inhibitor of the phosphoinositide 3-kinase delta (PI3Kδ) pathway, exhibiting an IC50 of 19 nM. This compound is primarily utilized in research related to chronic obstructive pulmonary disease (COPD), where modulation of the PI3Kδ signaling pathway may provide therapeutic insights. Its potency and specificity make it a valuable tool for investigating PI3Kδ's role in inflammatory and immune responses. -
PI3K Inhibitor
FD2056 is a potent, orally active inhibitor of the phosphoinositide 3-kinase (PI3K) family, with specific inhibition of PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, exhibiting IC50 values of 0.30, 0.80, 1.10, and 0.42 nM, respectively. This compound also targets cyclin-dependent kinases, inhibiting CDK2-CyclinA2 and CDK4-CyclinD3 with IC50 values of 115.95 nM and 2782.15 nM. FD2056 demonstrates significant antiproliferative effects in breast cancer cell lines, with IC50 values of 1.06 μM for MDA-MB-231, 0.04 μM for MDA-MB-468, and 1.40 μM for MCF-7 cells. Additionally, FD2056 promotes apoptosis in cancer cells and effectively inhibits tumor growth. -
PI3Kδ Inhibitor
PI3Kδ-IN-3 is a selective inhibitor of the PI3Kδ isoform, exhibiting an IC50 of 9 nM. This compound effectively inhibits B cell function, making it a valuable tool for studying immune responses and related disorders. With favorable pharmacokinetic properties, PI3Kδ-IN-3 is suitable for in vitro and in vivo research applications in the field of immunology and cancer therapeutics. -
PI3Kα Inhibitor
PI3Kα-IN-13 is a selective inhibitor of PI3Kα, demonstrating an IC50 value of 2.5 nM. This compound effectively induces apoptosis in tumor cells, significantly inhibiting cancer cell proliferation across various cell lines, including MCF-7 (IC50: 0.75 μM), HCT-116 (IC50: 3.79 μM), MDA-MB-231 (IC50: 13.71 μM), and SW620 (IC50: 9.85 μM). Additionally, PI3Kα-IN-13 reduces tumor cell colony formation, migration, and invasion, making it a valuable tool for cancer research and therapeutic development. -
PI3Kγ Inhibitor
PI3Kγ Inhibitor 6 is a selective inhibitor of the phosphoinositide 3-kinase gamma (PI3Kγ) enzyme. This compound demonstrates significant anti-inflammatory activity, making it a valuable tool for research into inflammatory and autoimmune diseases. Its inhibition of PI3Kγ can help elucidate the signaling pathways involved in various pathological conditions, providing insights into potential therapeutic strategies. -
PI3K/Proliferation Inhibitor
PI3Kδ-IN-17 is a highly selective inhibitor of PI3Kδ, exhibiting an IC50 of 2.82 nM. This compound demonstrates significant anti-proliferative effects in SU-DHL-6 cells, with an IC50 value of 0.035 μM. PI3Kδ-IN-17 is valuable for research applications focusing on cancer biology and the modulation of cell proliferation pathways. -
Pan-isoform PI3K Inhibitor
PX-866-17OH is a pan-isoform inhibitor of phosphoinositide 3-kinases (PI3K) that exhibits IC50 values of 14, 57, 131, and 148 nM against PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively. Its primary action as a metabolite of PX-866 (Sonolisib) makes it a valuable tool in the study of PI3K signaling pathways. PX-866-17OH has potential applications in cancer research and therapeutic development, particularly in contexts where PI3K signaling contributes to tumor growth and survival. -
PI3K Inhibitor
IMM-H012 is a selective inhibitor of phosphoinositide 3-kinase (PI3K), exhibiting an IC50 of 0.80 nM for PI3Kα. This compound demonstrates significant antitumor activity when used in combination with [177Lu]Lu-P4, showing synergistic effects against stomach and lung cancers. It is a valuable tool for researchers investigating PI3K signaling pathways and their implications in cancer therapeutics. -
PI3K Inhibitor
PI3K-IN-50 is a selective inhibitor of phosphoinositide 3-kinase (PI3K), known for its ability to interfere with key signaling pathways involved in cell growth and metabolism. This compound demonstrates potent inhibitory activity against PI3K, making it valuable for research focused on cancer, metabolic disorders, and other diseases associated with dysregulated PI3K signaling. Its utility in studying PI3K-related biological processes makes it an important tool for investigating therapeutic strategies targeting this pathway. -
PI3Kδ/γ Inhibitor
HM5023507 is a selective inhibitor of PI3Kδ and PI3Kγ, exhibiting IC50 values of 4 μM and 5 μM, respectively, while showing minimal activity against PI3Kα and PI3Kβ. This compound effectively attenuates PI3Kδ/γ signaling in human basophils and suppresses the activation, function, and cytokine production of human B and T cells, impacting Th17 differentiation in CD4 T cells. In vivo studies demonstrate that HM5023507 can inhibit collagen-induced inflammatory responses in rat models, making it a valuable tool for research into inflammatory diseases, particularly rheumatoid arthritis. -
PI3Kα Inhibitor
PI3Kα-IN-11 is a selective inhibitor of phosphoinositide 3-kinase alpha (PI3Kα), demonstrating significant efficacy in interrupting the PI3K signaling pathway. This compound exhibits potent anticancer activity, making it a valuable tool for research on tumorigenesis and cancer therapy. Its application spans in vitro studies to evaluate the role of PI3Kα in cancer proliferation and progression, contributing to the development of targeted cancer treatments. -
PI3Kγ Inhibitor
PI3Kγ inhibitor 7 is a selective inhibitor targeting the phosphoinositide 3-kinase gamma isoform (PI3Kγ), exhibiting an IC50 value of 3.42 nM for this target, while showing significantly higher IC50 values for PI3Kα, PI3Kβ, and PI3Kδ. This compound demonstrates notable antitumor activity, making it suitable for cancer research applications. Additionally, PI3Kγ inhibitor 7 contains an alkyne functional group, enabling its use in click chemistry reactions, specifically copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. -
PI3K Inhibitor
17β-Hydroxywortmannin is a potent inhibitor of phosphatidylinositol-3-kinase (PI3K) with an impressive IC50 of 0.5 nM. This compound effectively suppresses osteoclast resorption, displaying an IC50 of 10 nM, and exhibits notable antitumor activity. It is valuable in research applications focused on cancer biology and bone metabolism. -
PI3K Inhibitor
PI3K-IN-49 is a selective phosphoinositide 3-kinase (PI3K) inhibitor. It exhibits significant antiproliferative effects in T-47D and SKBR3 cell lines, making it a valuable tool for cancer research. This compound can be utilized to investigate PI3K signaling pathways and their role in tumor growth and progression. -
PI3Kβ Inhibitor
PI3Kβ-IN-1 is a selective inhibitor of phosphoinositide 3-kinase beta (PI3Kβ) with an IC50 value of 2 nM, demonstrating potent activity against this target. This compound is suitable for in vitro and in vivo research applications aimed at investigating the role of PI3Kβ in various signaling pathways and disease models, including cancer and metabolic disorders. Its oral bioavailability enhances its potential for therapeutic development and translational studies. -
PI3K Inhibitor
PI3Kγ inhibitor 5 is a selective inhibitor of phosphoinositide 3-kinase γ (PI3Kγ), exhibiting an IC50 value of 34 nM. This compound is vital for studying the role of PI3Kγ in cellular signaling pathways, including immune response and cancer progression. It serves as a valuable tool in research focused on targeting PI3K signaling in various disease models. -
PI3Kγ/δ Inhibitor
IHMT-PI3K-455 is a selective, orally active dual inhibitor of PI3Kγ and PI3Kδ, exhibiting IC50 values of 7.1 nM and 0.57 nM for each isoform, respectively. This compound effectively suppresses AKT phosphorylation, leading to documented inhibition of tumor growth through the recruitment and activation of CD8+ cytotoxic T cells. IHMT-PI3K-455 is primarily utilized in cancer research to explore its therapeutic potential and mechanisms in tumor biology. -
PI3Kδ Inhibitor
RV-1729 is a potent inhibitor of phosphatidylinositol 3-kinase-delta (PI3Kδ), with an IC50 value of 12 nM for the release of phosphatidylinositol 3,4,5-triphosphate (PIP3). This compound exhibits significant selectivity, being twice as selective for PI3Kδ compared to PI3Kγ and 16 times more selective for PI3Kα. RV-1729 modulates immune and inflammatory responses, making it a valuable tool in research applications related to asthma and chronic obstructive pulmonary disease (COPD). -
PI3K/PIKK Inhibitor
PI3K/PIKK-IN-2 is a potent inhibitor of the phosphoinositide 3-kinase (PI3K) and phosphoinositide-dependent kinase (PIKK) pathways. This compound demonstrates significant biological activity by modulating signaling pathways involved in cell growth, metabolism, and survival. PI3K/PIKK-IN-2 is suitable for use in research applications focused on targeted therapies, including the development of antibody-drug conjugates (ADCs). -
PI3K Inhibitor
Nemiralisib succinate is a potent and selective inhibitor of phosphoinositide 3-kinase delta (PI3Kδ), exhibiting a pKi of 9.9. This compound demonstrates significant anti-inflammatory effects and is utilized in research applications focusing on immune response modulation and cancer therapy. Its specificity for PI3Kδ makes it an important tool for investigating pathways involved in various diseases, particularly those associated with hematological malignancies and autoimmune disorders. -
PI3Kδ Inhibitor
PI3Kδ-IN-13 is a selective inhibitor of phosphoinositide 3-kinase delta (PI3Kδ) with an IC50 of 2.6 nM. This compound demonstrates significant activity in modulating cell proliferation and has potential applications in researching various diseases, including cancer, infections, inflammation, and autoimmune disorders. Its specificity towards PI3Kδ makes it a valuable tool for dissecting the biological pathways involved in these conditions. -
PI3K Inhibitor
PI3K-IN-19 hydrochloride is a potent inhibitor of phosphatidylinositol-3-kinase (PI3K), targeting the PI3K signaling pathway involved in cellular growth and survival. This compound demonstrates significant biological activity in modulating PI3K-mediated processes, making it valuable for studying cancer and metabolic disorders. Its application extends to research on drug development and mechanistic studies of PI3K-related pathways. -
PI3K Inhibitor
PI3Kδ-IN-18 is a highly selective inhibitor of the phosphoinositide 3-kinase delta (PI3Kδ) with an IC50 value below 0.1 nM. This compound demonstrates potent inhibitory activity, making it a valuable tool for research applications focused on autoimmune diseases and related signaling pathways. Its ability to modulate PI3Kδ activity allows for the exploration of therapeutic strategies targeting immune cell functionality and inflammation. -
PI3Kα Inhibitor
Hit20 is a selective inhibitor of PI3Kα, effectively inhibiting PI3Kα kinase activity and reducing phosphorylation of this target. This compound demonstrates significant biological activity by suppressing proliferation, colony formation, migration, and invasion in colon cancer cells. Hit20 is a valuable tool for investigating the role of PI3Kα in colon cancer research and therapeutic development. -
PI3Kα Inhibitor
PI3Kα-IN-15 is a highly selective inhibitor of the phosphoinositide 3-kinase alpha (PI3Kα) with an IC50 of 0.15 μM. It demonstrates significant anti-proliferative effects against various cancer cell lines, including SKOV-3, T47D, NCI-H1975, NCI-H460, and MCF-7, with IC50 values of 26.6 μM, 7.9 μM, 32.1 μM, 17.7 μM, and 9.4 μM, respectively. PI3Kα-IN-15 is valuable for investigations into cancer biology and potential therapeutic strategies targeting the PI3K pathway. -
PI3Kγ Inhibitor
PI3K-IN-60 is a highly selective inhibitor targeting phosphatidylinositol 3-kinase gamma (PI3Kγ). This compound demonstrates significant biological activity in modulating immune responses and exhibits potential applications in the study of autoimmune diseases, such as multiple sclerosis, as well as various cancer types including breast cancer and pancreatic ductal adenocarcinoma. -
PI3K/ERK Inhibitor
CXJ-2 is a cyclic peptide that serves as a potent inhibitor of the PI3K/ERK signaling pathway. It significantly reduces the proliferation and migration of hepatic stellate cells, demonstrating strong antifibrotic properties. This compound is valuable for research in fibrosis and related hepatic disorders, providing insights into cellular processes influenced by the PI3K/ERK pathway. -
PI3K Inhibitor
PI3K-IN-12 is a potent inhibitor of phosphoinositide 3-kinase (PI3K) with a primary mechanism of disrupting PI3K signaling pathways. It demonstrates significant biological activity in modulating cell survival and proliferation, making it a valuable tool for cancer research and studies investigating metabolic disorders. Researchers can utilize PI3K-IN-12 to explore the role of PI3K in various cellular processes and therapeutic interventions. -
PI3Kα Inhibitor
PI3Kα-IN-20 is a selective inhibitor of phosphoinositide 3-kinase alpha (PI3Kα). It effectively disrupts the PI3K signaling pathway, leading to the modulation of cellular functions such as growth, proliferation, and survival. This compound is valuable for research applications focused on cancer biology, metabolic disorders, and other conditions associated with aberrant PI3Kα activity. -
PI3Kδ/γ Inhibitor
PI3Kδ/γ-IN-2 is a potent dual inhibitor of phosphoinositide 3-kinase delta (PI3Kδ) and gamma (PI3Kγ), demonstrating IC50 values of 1 nM and 4.3 nM, respectively. With favorable oral bioavailability, this compound shows promise in the treatment of B-cell malignancies, making it a valuable tool for research in cancer biology and therapeutic development targeting the PI3K signaling pathway. -
PI3K Inhibitor
PI3K-IN-26 is a potent inhibitor of phosphoinositide 3-kinase (PI3K), exhibiting an IC50 of 36 nM in SU-DHL-6 cells. This compound is useful in research focused on the PI3K signaling pathway, which plays a critical role in cell growth, proliferation, and survival. The inhibition of PI3K by PI3K-IN-26 allows for the investigation of its effects on cancer cell metabolism and identification of potential therapeutic targets. -
PI3K Inhibitor
PI3K-IN-10 is a potent pan-PI3K inhibitor derived from benzimidazole. This compound selectively targets the phosphoinositide 3-kinase (PI3K) pathway, demonstrating significant inhibitory activity across various PI3K isoforms. Its key biological activity makes it a valuable tool for investigating PI3K-related signaling mechanisms and potential therapeutic applications in cancer and metabolic disorders. -
PI3Kδ Inhibitor
PI3Kδ-IN-23 is a highly selective inhibitor of the PI3Kδ isoform, exhibiting an exceptional binding affinity with an IC50 value of 0.27 nM. This compound forms covalent bonds with the Lys779 residue on PI3Kδ, effectively blocking its activity. Its potent inhibition profile makes PI3Kδ-IN-23 a valuable tool for cancer research, particularly in studies focused on therapeutic strategies targeting PI3K signaling pathways. -
PI3Kα Inhibitor
PI3Kα-IN-1 is a potent inhibitor of the phosphoinositide 3-kinase alpha (PI3Kα) with an IC50 value of less than 0.5 nM. Additionally, it exhibits inhibitory activity against mTOR with an IC50 of 104 nM. This compound is valuable for studying the PI3K/mTOR signaling pathway, which is implicated in various diseases, including cancer and metabolic disorders. Research applications include evaluating the effects of PI3Kα inhibition on cell proliferation, survival, and signaling. -
PI3Kδ Inhibitor
PI3Kδ-IN-26 is a selective and orally active inhibitor of the PI3Kδ isoform, exhibiting an IC50 of 14 nM. This compound has demonstrated significant efficacy in attenuating inflammatory responses in house dust mite-induced chronic asthma models in mice. Due to its potent anti-inflammatory properties, PI3Kδ-IN-26 is a valuable tool for research into inflammatory, autoimmune, and hyperproliferative diseases. -
PI3K Inhibitor
LTURM 36 is a potent inhibitor of phosphoinositide 3-kinase (PI3K), exhibiting IC50 values of 0.64 μM for PI3Kδ and 5.0 μM for PI3Kβ. This compound serves as a valuable tool in cancer research by modulating PI3K signaling pathways, which are frequently implicated in tumorigenesis and cancer progression. Its selective inhibition profile positions LTURM 36 as an important reagent for studying the roles of PI3K isoforms in various cancer types. -
PI3Kα Inhibitor
PI3Kα-IN-24 is a potent inhibitor of PI3Kα, exhibiting an IC50 of 0.025 μM. This compound effectively suppresses phosphorylated Akt at serine 473, demonstrating significant impact in cellular signaling pathways. It is a valuable tool for cancer research, allowing for the exploration of PI3Kα-mediated mechanisms and therapeutic strategies. -
PI3Kα Inhibitor
PI3Kα-IN-17 is a selective inhibitor of phosphoinositide 3-kinase alpha (PI3Kα), a critical enzyme in the PI3K signaling pathway. This compound demonstrates potent inhibitory activity, making it valuable for research focused on cancer biology and other diseases linked to dysregulated PI3Kα activity. It can be utilized to explore the role of PI3Kα in cancer cell proliferation, survival, and metabolism. -
PI3K Inhibitor
PI3K-IN-54 is a potent pan-PI3K inhibitor that targets the p110α, p110β, and p110δ isoforms with IC50 values of 0.22 nM, 1.4 nM, and 0.38 nM, respectively. This compound is valuable for investigating the role of PI3K signaling in various cancers. Its ability to inhibit multiple isoforms makes PI3K-IN-54 a useful tool for studying cancer progression and therapy resistance. -
PI3Kδ Inhibitor
GNE-293 is a selective inhibitor of phosphoinositide 3-kinase delta (PI3Kδ), demonstrating an IC50 of 4.38 nM. This compound exhibits favorable pharmacokinetic properties, making it suitable for in vitro and in vivo studies. GNE-293 is particularly relevant for research into asthma, rheumatoid arthritis, and various inflammatory disorders. -
PI3Kδ Inhibitor
AS2541019 is a selective inhibitor of the PI3Kδ (p110δ) isoform, effectively targeting the phosphoinositide 3-kinase pathway. This compound demonstrates notable inhibitory effects on B cell activation and proliferation, making it useful for evaluating immune responses. Additionally, AS2541019 has been shown to suppress antibody production in xenograft models, contributing to its potential applications in immunological research. -
PI3K Inhibitor
PI3K-IN-11 is a selective inhibitor of phosphoinositide 3-kinases (PI3K), targeting PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ with IC50 values of 6.4, 13, 8, and 11 nM, respectively, while showing significantly lower affinity for mTOR (IC50=2.9 μM). This compound demonstrates over 420-fold selectivity for PI3K in a comprehensive panel of 20 lipid and protein kinases. In PTEN-negative U87MG cells, PI3K-IN-11 effectively inhibits the phosphorylation of Akt and S6 kinase (S6K) at concentrations between 0.03 and 1 μg/mL. Additionally, it has shown potential in reducing tumor growth in U87MG mouse xenograft models at doses ranging from 2.5 to 10 mg/kg, making it a valuable tool for cancer research. -
PI3Kδ Inhibitor
AM-0687 is a selective inhibitor of phosphoinositide 3-kinase delta (PI3Kδ), exhibiting an IC50 of 2.9 nM. This compound effectively reduces levels of IgG and IgM specific antibodies and inhibits the proliferation of human B cells induced by anti-IgM/CD40L with an IC50 of 0.8 nM. Additionally, AM-0687 decreases AKT phosphorylation with an IC50 of 0.7 nM, demonstrating its potential as an anti-inflammatory agent in various research applications. -
PI3Kβ Inhibitor
GSK2636771 methyl is a selective inhibitor of PI3Kβ, a key lipid kinase involved in cellular signaling pathways regulating growth and survival. This compound is primarily utilized in cancer research, where it can be combined with other agents, such as VT-464, to explore potential therapeutic strategies. Its role in modulating PI3Kβ activity aids in the investigation of cancer metabolism and treatment resistance mechanisms. -
PI3K Inhibitor
NIBR-17 is a pan-class I PI3K inhibitor that targets phosphoinositide 3-kinases, key regulators in various signaling pathways. This compound demonstrates significant antitumor activity by effectively inhibiting cell proliferation and survival in cancer models. It is suitable for research applications focused on cancer biology and drug discovery targeting the PI3K/Akt signaling pathway. -
PI3K/mTOR Inhibitor
NVP-BBD130 is a potent dual inhibitor of PI3K and mTOR, functioning through ATP-competitive mechanisms. This compound demonstrates significant stability and provides effective oral bioavailability. Additionally, NVP-BBD130 serves as a click chemistry reagent due to its alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. Its versatility makes it suitable for various research applications in cancer therapy and biochemical signaling pathways.
