Catalog No.
Product Name
Application
Product Information
Citations
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PI3Kδ Inhibitor
Roginolisib hemifumarate is a selective inhibitor of the PI3Kδ isoform with an IC50 of 145 nM. This compound demonstrates significant selectivity across a broad panel of 278 additional kinases, making it a valuable tool for the study of signaling pathways involving PI3Kδ. Its potency and specificity facilitate research applications in cancer biology and immune modulation. -
PI3Kβ/δ Inhibitor
PI3K-IN-2 is a potent and orally bioavailable inhibitor of PI3Kβ and PI3Kδ, exhibiting IC50 values of 7.1 nM and 8.6 nM, respectively. This compound demonstrates excellent selectivity over other isoforms, such as PI3Kσ and PI3Kγ, with IC50 values of 13 nM and 190 nM. Due to its specificity and potency, PI3K-IN-2 is suitable for research applications focusing on cancer, inflammation, and other diseases associated with dysregulated PI3K signaling pathways. -
PI3K Inhibitor
PI3K-IN-18 dihydrochloride is a selective inhibitor of the PI3K p110α isoform, derived from a 4-morpholino-2-phenylquinazoline structure. This compound demonstrates significant biological activity in attenuating the PI3K signaling pathway, which plays a crucial role in cell growth, proliferation, and survival. Research applications include cancer biology, where modulation of PI3K activity can provide insights into tumor progression and therapeutic responses. -
PI4K/PI3K Inhibitor
(S)-GSK-F1 is a potent inhibitor of type III phosphatidylinositol 4-kinase α (PI4KIIIα). It demonstrates inhibitory activity against various kinases, including PI4Kα, PI4Kβ, PI4Kγ, PI3Kα, PI3Kβ, and PI3Kδ, with pIC50 values of 8.3, 6.0, 5.6, 5.6, 5.1, and 5.6, respectively. (S)-GSK-F1 has been shown to effectively inhibit hepatitis C virus (HCV) replication, making it a valuable tool for research in viral infections and signaling pathways. Its moderate pharmacokinetic profiles in rat models support its potential for in vivo studies. -
PI3K Inhibitor
(S)-PI3K-IN-2 is a selective inhibitor of phosphoinositide 3-kinase (PI3K) isoforms β and δ, exhibiting IC50 values of 0.198 μM and 0.282 μM, respectively. This compound effectively inhibits phosphorylation of AKT at serine 473 in MDA-MB-468 cancer cells, demonstrating an IC50 of 27 nM. (S)-PI3K-IN-2 is a valuable tool for investigating PI3K signaling pathways and their implications in cancer research. -
PI3Kδ Inhibitor
PI3Kδ-IN-15 is a highly selective inhibitor of the PI3Kδ isoform, demonstrating an IC50 of 0.5 nM specifically for the p110δ subunit. This compound exhibits over 30-fold greater potency against PI3Kδ compared to other isoforms including PI3Kγ, PI3Kβ, and PI3Kα. PI3Kδ-IN-15 is valuable for research applications targeting immune cell signaling and cancer biology, aiding in the exploration of therapeutic strategies for diseases associated with aberrant PI3Kδ activity. -
PI3K Inhibitor
PI3Kδ-IN-9 is a selective inhibitor of the phosphoinositide 3-kinase delta (PI3Kδ) with an IC50 value of 3.8 nM. It effectively modulates signaling pathways related to immune responses and inflammation. This compound is utilized in research applications focused on cancer, autoimmune diseases, and other conditions where PI3Kδ plays a critical role in cellular processes. -
PI3K Inhibitor
Vps34-IN-3 is a selective inhibitor of the VPS34 kinase, a key component of the phosphoinositide 3-kinase (PI3K) signaling pathway. This compound exhibits potent activity, making it suitable for research applications aimed at understanding lipid metabolism, autophagy, and cellular signaling processes. Its oral bioavailability enhances its utility in preclinical studies. -
PI3K Inhibitor
Nemiralisib hydrochloride is a potent and highly selective inhibitor of the phosphoinositide 3-kinase delta (PI3Kδ) pathway, exhibiting a pKi of 9.9. This compound demonstrates significant biological activity in modulating immune responses and is primarily utilized in research related to cancer and autoimmune diseases. Its selective inhibition of PI3Kδ makes it a valuable tool for investigating the roles of this pathway in various cellular processes and therapeutic interventions. -
BTK/PI3Kδ Inhibitor
MDVN1003 is a dual inhibitor of Bruton's tyrosine kinase (BTK) and phosphatidylinositol-3-kinase delta (PI3Kδ). This compound effectively inhibits B cell activation and blocks the phosphorylation of protein kinase B (AKT) as well as extracellular signal-regulated kinases 1 and 2 (ERK 1/2). MDVN1003 is primarily utilized in research related to non-Hodgkin’s lymphoma (NHL), offering insights into the underlying mechanisms of lymphocyte-driven malignancies. -
PI3Kδ Inhibitor
PI3Kδ-IN-8 is a selective inhibitor of phosphoinositide 3-kinase delta (PI3Kδ) with an IC50 value of 3.3 nM. It demonstrates a pronounced selectivity for PI3Kδ compared to PI3Kα, PI3Kβ, and PI3Kγ, exhibiting IC50 values of 377.2 nM, 241.6 nM, and 17.9 nM, respectively. This compound has shown significant anti-tumor activity, making it a valuable tool for research in cancer therapeutics and cellular signaling pathways involving PI3Kδ. -
PI3K Inhibitor
GSK251 is a potent and selective inhibitor of the phosphoinositide 3-kinase delta (PI3Kδ) isoform, exhibiting a novel binding mechanism. It demonstrates significant biological activity by effectively impeding PI3Kδ signaling pathways, which are crucial in various immune responses and hematological malignancies. GSK251 is utilized in research applications focused on understanding the role of PI3Kδ in cancer therapy and immune modulation. -
PI3Kδ Inhibitor
CHF-6523 is a selective inhibitor of PI3Kδ, which plays a crucial role in cellular signaling pathways. This compound exhibits potent biological activity in modulating immune responses and has been employed in research focused on chronic obstructive pulmonary disease (COPD). Its ability to inhibit PI3Kδ makes it a valuable tool for investigating therapeutic strategies targeting immune and inflammatory processes associated with COPD. -
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.
