PI3K

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.

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-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).

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-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-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.

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.

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-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.

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.

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-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-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-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-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-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-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-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-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.

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-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-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.

PI(3,4)P2 (18:1) ammonium salt is a potent activator of phosphatidylinositol 3-kinase (PI3K). This polyphosphorylated phosphatidylinositol effectively promotes the activation of AKT (protein kinase B), thereby influencing key cellular processes such as metabolism, growth, and survival. Additionally, PI(3,4)P2 (18:1) ammonium salt plays a crucial role in regulating cytoskeletal dynamics, impacting cell morphology and movement. It is applicable in studies related to cancer, diabetes, and cardiovascular disease.

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.

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.

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-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.

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.

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.

mTOR inhibitor-25 is a selective inhibitor of the mechanistic target of rapamycin (mTOR), demonstrating significant anticancer activity. It exhibits strong inhibitory effects on mTOR while having a comparatively weaker impact on phosphoinositide 3-kinase (PI3K). This compound is valuable for research applications focused on various cancers, including leukemia, skin cancer, breast cancer, lung cancer, and colon cancer, and has shown excellent efficacy in cell proliferation assays.

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.

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-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-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.

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.

Zandelisib is a selective, orally active, non-covalent inhibitor of PI3Kδ. It effectively inhibits AKT phosphorylation and suppresses downstream signaling pathways, making it a valuable tool in cancer research. Zandelisib is particularly relevant for studying malignancies such as relapsed or refractory B-cell lymphoma, providing insights into tumor behavior and therapeutic response.

Copanlisib-NH is a selective ligand for the PI3Kα/δ isoforms, making it a valuable tool in targeted protein degradation studies. This compound serves as a ligand in the development of PROTACs aimed at degrading PI3Kα/δ proteins, facilitating research on mechanisms of resistance and cellular pathways in oncology. Notably, Copanlisib-NH is applicable in breast cancer research, offering insights into therapeutic strategies that exploit the PI3K signaling pathway.