Catalog No.
Product Name
Application
Product Information
Citations
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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 Activator
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 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
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. -
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. -
mTORC2 Inhibitor
JR-AB2-011 is a selective inhibitor of the mTORC2 complex, exhibiting an IC50 value of 0.36 μM. This compound disrupts the association between Rictor and mTOR (Ki: 0.19 μM), leading to reduced phosphorylation of Akt and decreased MMP2 activity. Consequently, JR-AB2-011 inhibits the migratory and invasive capabilities of tumor cells while also triggering non-apoptotic cell death. It serves as a valuable tool for research into cancer treatment and the regulation of cellular signaling pathways. -
mTORC1 Inhibitor
RMC-5552 is a potent and selective inhibitor of the mTORC1 pathway. It effectively inhibits the phosphorylation of S6K and 4EBP1 with IC50 values of 0.14 nM and 0.48 nM, respectively. RMC-5552 demonstrates significantly lower inhibition of AKT (IC50 of 19 nM), conferring a selectivity ratio for mTORC1 over mTORC2 of nearly 40-fold. This compound exhibits anti-cancer activity, making it a valuable tool for cancer research and therapeutic development targeting mTOR signaling. -
Rheb/mTORC1 Inhibitor
Rheb inhibitor NR1 is a selective Rheb/mTORC1 inhibitor with an IC50 of 2.1 µM in the Rheb-IVK assay. This compound directly binds to the switch II domain of Rheb, effectively inhibiting the activation of the mechanistic target of rapamycin complex 1 (mTORC1). Rheb inhibitor NR1 attenuates phosphorylation of T389pS6K1 while enhancing phosphorylation of S473pAKT in a dose-dependent manner, with no effect on mTORC2 activity. It serves as a valuable tool for investigating the mTOR signaling pathway and its implications in various diseases. -
PIP4K2C-mTOR Activator
C24-Ceramide is a competitive binding agonist of PIP4K2C, a key regulator of the mTOR signaling pathway. This compound facilitates cellular processes such as enhanced keratinocyte proliferation and migration, thereby promoting skin wound healing. Moreover, C24-Ceramide has been implicated in the proliferation and metastasis of gallbladder cancer cells, indicating its potential as a therapeutic target. Additionally, C24-Ceramide levels in serum may serve as a diagnostic marker for gallbladder cancer. -
mTORC1 Activator
Mefluleucine hydrochloride is a selective and orally active activator of mTORC1, functioning primarily through its interaction with Sestrin2. This leucine analog plays a critical role in neurobiology and has been utilized in research studies focused on antidepressant mechanisms. Its distinct properties make it a valuable tool for investigating mTORC1 signaling pathways and their implications in mood disorders. -
mTORC1-Selective Inhibitor
RMC-6272 is a bi-steric inhibitor selectively targeting mTORC1. It demonstrates potent inhibition of mTORC1 with over 10-fold selectivity compared to mTORC2, outperforming Rapamycin in its ability to inhibit mTORC1 and induce cell death in TSC2 null tumors. This compound is valuable for research applications focusing on cancer biology and therapeutic strategies targeting the mTOR signaling pathway. -
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. -
mTOR Inhibitor
PQR626 is a selective mTOR inhibitor that demonstrates potent activity with an IC50 of 5 nM and a Ki of 3.6 nM. This orally active compound is designed for effective brain penetration, making it suitable for investigating neurological disorders. Research applications include studying the role of mTOR in neurodegenerative diseases and evaluating potential therapeutic strategies targeting this pathway. -
mTORC1/mTORC2 Inhibitor
MTI-31 is a potent inhibitor of mTORC1 and mTORC2, demonstrating high selectivity for mTOR with a Kd of 0.20 nM and over 5,000-fold selectivity against PIK3CA, PIK3CB, and PIK3G. It exhibits an IC50 of 39 nM in the LANCE assay for mTOR substrate phosphorylation in the presence of 100 μM ATP. This compound is valuable for research into breast cancer and other diseases involving aberrant mTOR signaling pathways. -
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. -
mTOR Inhibitor
WYE-23 is a selective mTOR inhibitor with a reported IC50 of 0.45 nM against mTOR and 661 nM against PI3Kα. This compound exhibits significant antitumor activity, making it a valuable reagent for cancer research. It is particularly useful for studies investigating the role of mTOR signaling in tumorigenesis and therapeutic interventions targeting this pathway. -
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. -
mTORC1 Inhibitor
RMC-4627 is a selective inhibitor of the mechanistic target of rapamycin complex 1 (mTORC1), a key regulator of cell growth and proliferation. This compound has been shown to activate 4EBP1, leading to the downregulation of protein synthesis and subsequently inhibiting tumor growth. RMC-4627 is valuable for research applications focused on cancer biology and the elucidation of mTOR signaling pathways. -
mTOR Complex 1 Inhibitor
WRX606 is a selective inhibitor of the mTOR complex 1 (mTORC1), which effectively disrupts the phosphorylation of key mTORC1 substrates, including S6 kinase 1 (S6K1) and eukaryotic translation initiation factor 4E binding protein (4E-BP1), with IC50 values of 10 nM and 0.27 μM, respectively. This compound demonstrates significant antitumor activity by suppressing tumor growth in mouse models without promoting metastasis. WRX606 is a valuable tool for research focused on exploring therapeutic strategies against cancer through mTORC1 inhibition. -
mTOR Inhibitor
mTOR inhibitor WYE-28 selectively targets the mammalian target of rapamycin (mTOR), exhibiting an IC50 of 0.08 nM. Additionally, it inhibits PI3Kα with an IC50 of 6 nM, demonstrating its potential for broader applications in cancer therapy and metabolic research. WYE-28 has a metabolic half-life (T1/2) of 13 minutes in nude mouse microsomes, making it a valuable reagent for studying mTOR signaling pathways and their implications in disease models. -
mTOR Inhibitor
(32-Carbonyl)-RMC-5552 is a potent inhibitor of the mechanistic target of rapamycin (mTOR), effectively blocking mTORC1 and mTORC2 signaling pathways. This compound impedes the phosphorylation of key substrates including p-P70S6K-(T389), p-4E-BP1-(T37/36), and p-AKT1/2/3-(S473), with pIC50 values greater than 9 for the first two and between 8 and 9 for the latter. (32-Carbonyl)-RMC-5552 is valuable for studies investigating mTOR-related cellular processes and the development of therapies targeting mTOR in various diseases. -
mTORC1/2 Inhibitor
AZD3147 is a potent, orally bioavailable dual inhibitor of mTORC1 and mTORC2, exhibiting an IC50 value of 1.5 nM. This compound selectively targets both complexes, while also having a specific inhibitory effect on PI3K. AZD3147 is primarily utilized in research related to cancer therapeutics and metabolic disorders, where modulation of the mTOR signaling pathway is of significant interest. -
mTOR Inhibitor
WYE-687 dihydrochloride is an ATP-competitive inhibitor of the mechanistic target of rapamycin (mTOR), demonstrating an IC50 of 7 nM. This compound effectively inhibits the activation of both mTORC1 and mTORC2, making it a valuable tool for studying mTOR signaling pathways. Additionally, WYE-687 modulates PI3Kα and PI3Kγ activity with IC50 values of 81 nM and 3.11 μM, respectively, supporting its role in cancer and metabolic research. -
Akt Kinase Activator
Thyroglobulin is a 660 kDa dimeric glycoprotein that serves as a substrate in the synthesis of thyroid hormones, thyroxine (T4) and triiodothyronine (T3). Primarily produced by follicular cells of the thyroid, it also functions in the storage of inactive thyroid hormone forms and iodine in the follicular lumen. In research applications, thyroglobulin has been shown to activate Akt kinase activity in FRTL-5 thyroid cells, making it valuable for studies related to thyroid function and signaling pathways. -
Nrf2/AMPK/mTOR Activator
Hydroxycitric acid (tripotassium) is a potent activator of the Nrf2, AMPK, and mTOR signaling pathways. It enhances the expression of antioxidant enzymes, elevates glutathione levels, and inhibits ferroptosis, thereby providing protection against oxidative stress and promoting cellular health. This compound is actively engaged in regulating renal and pulmonary vascular functions and is also implicated in the induction of apoptosis in cancer cells through cell cycle arrest and DNA fragmentation. Its multi-target bioactivity makes it a valuable tool in research focused on oxidative stress, cancer biology, and metabolic regulation. -
AKT1/SRC/STAT3/EGFR Binder
(+)−Theta-cypermethrin is a stereoisomer of cypermethrin that functions as a selective binder to AKT1, SRC, STAT3, and epidermal growth factor receptor (EGFR). This compound is known to penetrate the blood-brain barrier, leading to alterations in the amplitude of delayed rectifier potassium channel currents and significant shifts in the activation and inactivation curves at elevated concentrations. Additionally, (+)-Theta-cypermethrin induces abnormal electrical activity in rat hippocampal neurons and is associated with chronic respiratory system damage and neurotoxicity. It serves as a valuable tool for research into signal transduction pathways and neuropharmacology. -
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. -
PI3K Inhibitor
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. -
PI3Kα/δ Ligand
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.
