Catalog No.
Product Name
Application
Product Information
Citations
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PI3Kδ Inhibitor
PI3K-IN-9 is a potent and selective inhibitor of PI3Kδ, demonstrating an IC50 of 8.9 nM. This compound effectively modulates PI3K signaling pathways, making it a valuable tool in research focused on cancer and immune responses. It is applicable in studies evaluating the role of PI3Kδ in various diseases, including hematological malignancies and inflammatory disorders. -
PI3Kγ Inhibitor
PI3Kγ Inhibitor 4 is a selective, orally bioavailable inhibitor targeting the phosphoinositide 3-kinase gamma (PI3Kγ) enzyme, demonstrating an IC50 of 40 nM. It exhibits notable selectivity ratios of approximately 7-fold, 43-fold, and 18-fold against the α, β, and δ isoforms, respectively. This compound is valuable for studying airway inflammation and may contribute to understanding associated pathological conditions. -
PI3Kα Inhibitor
PI3K-IN-63 is a potent inhibitor of PI3Kα, exhibiting a Ki of 0.35 nM against human targets. This compound effectively inhibits the phosphorylation of AKT at the S473 site in cellular assays, demonstrating its capacity to interfere with critical signaling pathways. PI3K-IN-63 has shown efficacy in reducing the viability of non-small cell lung cancer cell lines harboring PIK3CA mutations, making it a valuable tool for research related to this type of cancer. -
PI3K Inhibitor
Amdizalisib is a selective inhibitor of the phosphoinositide 3-kinase (PI3K) pathway, which plays a crucial role in various cellular functions, including metabolism, growth, and survival. This compound demonstrates significant anti-proliferative effects in cancer cells and modulates immune responses, making it a valuable reagent for research applications focused on inflammatory diseases, autoimmune disorders, and oncology. Amdizalisib serves as an important tool for advancing the understanding of PI3K-related mechanisms in both disease states and therapeutic development. -
PI3Kδ Inhibitor
AM-8508 is a potent PI3Kδ inhibitor, demonstrating an IC50 of 0.016 μM. It selectively targets PI3Kδ, effectively blocking AKT phosphorylation associated with B cell receptor signaling. Research has shown that AM-8508 suppresses the production of antigen-specific IgG and IgM in immunized rats, highlighting its potential applications in the study of inflammatory diseases. This compound serves as a valuable tool for investigating the role of PI3Kδ in immune responses. -
PI3Kδ Inhibitor
AM-1430 is a highly selective and orally active inhibitor of the phosphoinositide 3-kinase delta (PI3Kδ) enzyme, with an IC50 value of 4.6 nM. This compound demonstrates significantly higher IC50 values for PI3Kα, PI3Kβ, and PI3Kγ, at 14.18 μM, 2.2 μM, and 3.22 μM, respectively. AM-1430 effectively inhibits B cell proliferation and shows strong in vivo activity, particularly in models of pAKT inhibition and hemoglobin (KLH) immune response. This reagent is suitable for research focused on inflammation and autoimmune diseases. -
PI3K Inhibitor
PI3Kα-IN-12 is a highly selective inhibitor of phosphoinositide 3-kinase alpha (PI3Kα) with an IC50 of 1.2 nM. It demonstrates significant antiproliferative activity against HCT-116 and U87-MG cell lines, with IC50 values of 0.83 μM and 1.25 μM, respectively. In vivo, PI3Kα-IN-12 induces tumor regression in a U87-MG xenograft model at a dosage of 40 mg/kg administered intraperitoneally, making it a valuable tool for research on cancer therapy targeting the PI3K signaling pathway. -
PI3Kα Inhibitor
PI3Kα-IN-19 is a selective inhibitor of PI3Kα, targeting the p110α catalytic subunit. This compound demonstrates significant biological activity in inhibiting the PI3Kα pathway, which is frequently dysregulated in various cancers. PI3Kα-IN-19 is valuable for researching cancer biology and evaluating therapeutic strategies that involve modulation of the PI3Kα signaling pathway. -
FAP-PI3K Inhibitor
FAP-PI3KI1 is a fibroblast-activated protein (FAP) inhibitor that selectively targets the phosphoinositide 3-kinase (PI3K) pathway in FAP-expressing human cells. This compound effectively inhibits collagen synthesis and reduces collagen deposition, making it a valuable tool for research in idiopathic pulmonary fibrosis (IPF) and related fibrotic conditions. Its targeted action facilitates investigating the role of the PI3K signaling pathway in fibrosis and offers potential insights into therapeutic strategies for IPF. -
PI3K Inhibitor
PI3K-IN-27 is a targeted inhibitor of phosphoinositide 3-kinase (PI3K), a critical component in cellular signaling pathways that govern processes such as cell growth, differentiation, migration, and apoptosis. This compound exhibits potent inhibitory activity against PI3K, making it valuable for investigating hyper-proliferative diseases, including cancer and inflammation, as well as immune and autoimmune disorders. Its role in modulating PI3K activity underscores its potential utility in preclinical research settings. -
PI3K Inhibitor
PI3K-IN-28 is a selective inhibitor of phosphoinositide 3-kinase (PI3K), showcasing significant potency in inhibiting its activity. With half-maximal inhibitory concentration (IC50) values of 5.8, 2.3, and 7.9 µM, PI3K-IN-28 demonstrates reduced toxicity in MCF-10a cell lines and a selectivity index (SI) of 39, highlighting its potential for anticancer applications. This compound serves as a promising lead for further development of targeted therapeutics in cancer research. -
PI3Kδ Inhibitor
Dezapelisib is a potent inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ) that demonstrates significant antitumor activity. This compound is primarily utilized in research focused on relapsed or refractory B-cell lymphomas, making it a valuable tool for understanding the therapeutic potential of targeted PI3Kδ inhibition in hematological malignancies. Its mechanism of action contributes to the modulation of cell proliferation and survival pathways, offering insights into cancer treatment strategies. -
PI3K Inhibitor
PI3K-IN-38 is an orally active inhibitor of phosphoinositide 3-kinase (PI3K), with an IC50 of 0.541 µM for PI3K-α. This compound demonstrates significant anticancer and anti-inflammatory properties, effectively inhibiting tumor growth in vivo. Its selective modulation of the PI3K pathway makes it a valuable tool for research into cancer therapies and inflammatory diseases. -
Pan-class I PI3K Inhibitor
NVP-CLR457 is a potent pan-class I PI3K inhibitor that exhibits oral bioavailability and a favorable pharmacokinetic/pharmacodynamic relationship. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. NVP-CLR457 is suitable for studies focused on the roles of PI3K signaling in various cancer types and therapeutic resistance mechanisms. -
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. -
PI3K/110β PROTAC Degrader
PROTAC PI3K/110β degrader-1 is a targeted protein degradation tool designed to selectively degrade the PI3K/110β protein. This reagent employs a PROTAC mechanism, linking an inhibitor of PI3K/110β with an E3 ligase ligand to facilitate ubiquitination and degradation. Its primary biological activity is to reduce levels of PI3K/110β, making it a valuable resource for studies exploring PI3K-related signaling pathways and their implications in cancer research and other diseases. -
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 Modulator
ML-220 is a selective PI3K modulator that plays a crucial role in the regulation of cellular signaling pathways. This compound has demonstrated significant biological activity in the context of neoplasms and infectious diseases, making it a valuable tool for research applications aimed at understanding tumor biology and host-pathogen interactions. Its mechanism of action on the PI3K pathway positions ML-220 as a promising candidate for further investigation in therapeutic development. -
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 Activator
PI3K-IN-23 is a selective PI3K activator that enhances glucose uptake with an EC50 value of 7.00 μM. This compound serves as a versatile click chemistry reagent due to its alkyne functionality, enabling efficient copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. Its applications extend to metabolic research and biochemical studies exploring PI3K pathways. -
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.
