Shop By
Catalog No.
Product Name
Application
Product Information
Citations
-
PI3Kδ inhibitor
CAL-130 Racemate is the racemate of CAL-130. CAL-130 Racemate is a PI3Kδ inhibitor. -
PI3Kα inhibitor
Alpelisib hydrochloride (BYL-719 hydrochloride) is a potent, orally active, and selective PI3Kα inhibitor with IC50s of 5 nM, 250 nM, 290 nM and 1200 nM for p110α, p110γ, p110δ, and p110β, respectively. -
multi-kinase inhibitor
Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle. -
multi-kinase inhibitor
Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle. -
PI3Kδ inhibitor
Umbralisib R-enantiomer (TGR-1202 R-enantiomer) is a PI3Kδ inhibitor, which is the less active enantiomer of TGR-1202. -
lysosomal exocytosis inhibitor
Vacuolin-1 is a potent and cell-permeable lysosomal exocytosis inhibitor. -
PI3Kδ inhibitor
Nemiralisib (GSK2269557 free base) is a potent and highly selective PI3Kδ inhibitor with a pKi of 9.9. -
PI3Kδ inhibitor
Selective PI3Kδ Inhibitor 1 (compound 7n) is an inhibitor of PI3Kδ with an IC50 of 0.9 nM and >1000-fold selectivity against other class I PI3K isoforms [PI3K α/γ/β=3670/1460/21300 nM]. -
PI3Kβ inhibitor
AZD6482 (S-isomer), CAS#1173900-37-2, is an isomer of AZD6482 (MedKoo Cat#406268) with S-configuration. AZD6482 is a potent, selective and ATP competitive PI3Kβ inhibitor (IC(50) 0.01 μm). -
PI3Kα Inhibitor
Tersolisib is a selective allosteric inhibitor of PI3Kα, specifically designed to target mutant forms of the enzyme. This compound exhibits significant anti-tumor activity, demonstrating robust and durable regression in various cancer models. Tersolisib is valuable in cancer research, particularly for studies focusing on PI3K pathway alterations and their therapeutic implications. -
PI3K/Akt/mTOR Inhibitor
Veratramine is a selective inhibitor of the PI3K/Akt/mTOR signaling pathway and serves as a modulator of SIGMAR1. This compound facilitates autophagic apoptosis in tumor cells, effectively induces G0/G1 cell cycle arrest, and diminishes epithelial-mesenchymal transition (EMT) markers, thereby reducing tumor migration. Additionally, Veratramine exhibits neuroprotective effects by inhibiting SIGMAR1 interactions with NMDAR and the phosphorylation of NMDAR Ser896, resulting in reduced neurological damage in neuropathy models. Its diverse biological activities make it suitable for research on liver cancer, osteosarcoma, and diabetic peripheral neuropathy. -
PI3Kα Inhibitor
BBO-10203 is a potent PI3Kα inhibitor that selectively and covalently binds to Cys242 in the RAS-Binding Domain. It inhibits both the GTP-bound and GDP-bound states of KRASG12C with an IC50 of 0.031 nM and an EC50 of 0.02 nM. By disrupting the interaction between RAS isoforms and PI3Kα, BBO-10203 effectively reduces pERK expression, suppresses cell growth, and induces G1 arrest and apoptosis. This compound is valuable for research into breast cancer, colorectal cancer, and non-small cell lung cancer. -
PI3K/AKT Inhibitor
PI3K/AKT-IN-1 is a potent dual inhibitor of the PI3K/AKT signaling pathway, exhibiting IC50 values of 6.99 μM for PI3Kγ, 4.01 μM for PI3Kδ, and 3.36 μM for AKT. This compound demonstrates significant anticancer activity by disrupting the PI3K/AKT axis, leading to the induction of caspase-3 dependent apoptosis. It serves as a valuable tool for research in cancer biology and therapeutic development targeting the PI3K/AKT pathway. -
PI3K/MDK Inhibitor
iMDK is a potent inhibitor of phosphoinositide 3-kinase (PI3K) and midkine (MDK), a growth factor associated with tumorigenesis. This compound has demonstrated the ability to effectively suppress non-small cell lung cancer (NSCLC) growth, particularly in combination with MEK inhibitors, while exhibiting minimal toxicity to normal cells and healthy mouse models. iMDK is a valuable tool for researchers studying cancer biology and potential therapeutic strategies targeting the PI3K/MDK signaling pathway. -
PI3Ka Inhibitor
Zovegalisib is an orally active allosteric inhibitor that selectively targets mutant forms of PI3Kα, exhibiting significant anti-tumor activity. This compound has demonstrated efficacy in inhibiting tumor growth in PIK3CA-mutant xenograft mouse models while exhibiting minimal effects on insulin levels. It is valuable for research into targeted cancer therapies and the exploration of PI3K signaling pathways. -
MEK/PI3K Inhibitor
ST-168 is an orally bioavailable inhibitor of MEK and PI3K, exhibiting IC50 values of 182 nM for MEK1 and showing varying potency against PI3K isoforms with values of 69.2 nM, 41.7 nM, 1482 nM, and 2293 nM for PI3Kα, PI3Kδ, PI3Kβ, and PI3Kγ, respectively. It effectively inhibits ERK1/2 and AKT phosphorylation, inducing apoptosis in cancer cells within a 3D tumor sphere model. In vivo studies demonstrate its substantial antitumor efficacy in A375 melanoma mouse models. Additionally, ST-168 displays an improved ocular safety profile compared to conventional MEK inhibitors, evidenced by reduced caspase activation and apoptosis levels, making it a valuable tool for melanoma research. -
DK/PI3K/BRD4 Inhibitor
SRX3177 is a potent triple inhibitor targeting CDK4/6, PI3K, and BRD4, with IC50 values of <2.5 nM for CDK4, 3.3 nM for CDK6, 79 nM for PI3Kα, 83 nM for PI3Kδ, 3.18 μM for PI3Kγ, and 33 nM and 89 nM for BRD4 BD1 and BD2, respectively. It exhibits broad cytotoxic activity against cancer cells while sparing normal epithelial cells, highlighting its potential as a targeted cancer therapeutic with reduced toxicity. -
PI3K/Akt/mTOR inhibitor
PI3K/Akt/mTOR-IN-2 is an inhibitor of the PI3K/AKT/mTOR signaling pathway with demonstrated anticancer activity. It selectively inhibits the proliferation of MDA-MB-231 cells with an IC50 of 2.29 μM and induces cell cycle arrest and apoptosis, making it a promising candidate for cancer research. -
EGFR/PI3K Inhibitor
MTX-531 is an orally active small molecule that inhibits EGFR (IC50 = 14.7 nM) and multiple PI3K isoforms, with IC50 values of 6.4 nM (PI3Kα), 233 nM (PI3Kβ), 8.3 nM (PI3Kγ), and 1.1 nM (PI3Kδ), demonstrating potent antitumor activity. Additionally, MTX-531 functions as a weak PPARγ agonist (IC50 = 2.5 µM), which may mitigate PI3K inhibitor-induced hyperglycemia. -
PI3K/AKT Pathways Inhibitor
Isocucurbitacin B selectively inhibits the PI3K/AKT signaling pathways, along with the MAPK and STAT3 pathways, demonstrating notable anti-cancer properties. This natural terpenoid, derived from Pedicellus melo, effectively suppresses cancer cell proliferation, migration, and invasion. Additionally, Isocucurbitacin B induces apoptosis and facilitates G2/M phase cell cycle arrest, while altering intracellular cholesterol and pH levels, and elevating intracellular calcium levels. It serves as a valuable reagent for research applications in cancer biology, particularly in the study of glioma. -
PI3K Inhibitor
PI3K-IN-7 is a selective inhibitor of phosphoinositide 3-kinase (PI3K) that effectively inhibits the phosphorylation of AKT, thereby disrupting downstream signaling pathways essential for cell survival. This compound promotes apoptosis in tumor cells while exhibiting low toxicity towards normal cells. PI3K-IN-7 is suitable for research applications focused on acute and chronic leukemia, multiple myeloma, and lymphoma. -
PI3Kα/c-Met Inhibitor
DFX117 is a selective, orally active inhibitor targeting PI3Kα and c-Met tyrosine kinase. This compound effectively inhibits the PI3K/Akt/mTOR pathway, demonstrating significant antiproliferative activity against cancer cell lines such as NCI-H1975, NCI-H1993, and HCC827, with IC50 values ranging from 0.02 to 0.08 µM. DFX117 induces cell cycle arrest at the G0/G1 phase and promotes apoptosis in A549 and NCI-H1975 cells. Additionally, DFX117 exhibits notable antitumor efficacy in murine models, making it a valuable tool for cancer research. -
PI3K/Akt/Ras/Raf/MAPK Inhibitor
Erufosine is a potent inhibitor of the PI3K/Akt and Ras/Raf/MAPK signaling pathways. It demonstrates significant cytotoxic activity against breast cancer cell lines, specifically MCF-7 and MDA-MB-231, with IC50 values of 40.95 μM and 40.8 μM, respectively. By reducing the phosphorylation levels of PI3K (p85), Akt (PKB), and cRaf, Erufosine serves as a valuable tool in the research of breast cancer and myeloid leukemia. -
PI3K/AKT/mTOR Inhibitor
PI3K/Akt/mTOR-IN-3 is a potent inhibitor targeting the PI3K/AKT/mTOR signaling pathway. It demonstrates significant biological activity, exhibiting IC50 values of 0.77 μM, 1.23 μM, and 4.57 μM in MCF-7, HeLa, and HepG2 cells, respectively. Additionally, this compound effectively inhibits the migration of MCF-7 and HeLa cells at a concentration of 4 μM, while also inducing apoptosis and causing cell cycle arrest in the S phase. This makes PI3K/Akt/mTOR-IN-3 a valuable tool for research in cancer biology and therapeutic development. -
PI3K/AKT Inhibitor
PI3K/AKT-IN-3 is a selective inhibitor of the PI3K/AKT signaling pathway, known to induce both autophagy and apoptosis in various cell types. This compound is primarily utilized in cancer research to study the effects of PI3K/AKT inhibition on tumor growth and cell survival mechanisms. Its application extends to exploring therapeutic strategies targeting this critical signaling pathway in cancer treatment. -
PI3Kδ Inhibitor
PI3Kδ-IN-24 is a highly selective inhibitor of the phosphoinositide 3-kinase delta (PI3Kδ) with an IC50 of 0.1 nM. This compound demonstrates notable antiproliferative effects in cancer cell lines with elevated PI3Kδ expression. By inhibiting PI3Kδ, PI3Kδ-IN-24 effectively lowers phosphorylated AKT levels and promotes cell cycle arrest and apoptosis in tumor cells. Its applications are particularly relevant in cancer research, including studies involving diffuse large B-cell lymphoma (DLBCL). -
PI3Kδ Inhibitor
X-370 is a PI3Kδ inhibitor (IC50 = 7 nM). X-370 inhibits the survival of leukemia cells, inducing G1 arrest and apoptosis. X-370 blocks PDK1 binding and phosphorylation of MEK1/2, eliminating Akt and Erk1/2 signaling. X-370 can be used in research on B-cell acute lymphoblastic leukemia (B-ALL). -
PI3K/Akt/FoxO3a Inhibitor
RLX hydrochloride is a potent inhibitor of the PI3K/Akt/FoxO3a signaling pathway, which plays a critical role in cellular growth and survival. This compound demonstrates significant therapeutic potential in experimental colon cancer by modulating the tumor microenvironment and enhancing the efficacy of cancer immunotherapy. Additionally, RLX hydrochloride can improve the retention of therapeutic agents within tumors when utilized with advanced nanoparticle delivery systems. It may also be effectively combined with other treatment modalities, such as chemotherapy and radiotherapy, to optimize overall cancer therapy outcomes. -
PI3K Inhibitor
PI3K-IN-4 is a potent Pan-PI3K inhibitor. PI3K-IN-4 has high activity for three PI3K isoforms with the IC50 values of picomole. PI3K-IN-4 shows superior inhibitory activity against PI3Kα (IC50 = 0.20 nM), PI3Kβ (IC50 = 2.99 nM), PI3Kδ (IC50 = 0.48 nM) and PI3Kγ (IC50 = 0.58 nM) and has no significant activity against EGFR. PI3K-IN-4 inhibits cancer cell growth though PI3K/Akt signaling pathway, leading to the inhibition of colony formation and the induction of apoptosis. PI3K-IN-4 can be used for lung, colon and breast cancer research. -
PI3K Inhibitor
PI3K-IN-29 is a potent inhibitor of Phosphoinositide 3-kinase (PI3K), effectively disrupting the PI3K/Akt signaling pathway. It demonstrates significant cytotoxic activity against various cancer cell lines, including U87MG, HeLa, and HL60, with IC50 values of 0.264 µM, 2.04 µM, and 1.14 µM, respectively. This compound is valuable for research applications involving cancer biology and therapeutic interventions targeting the PI3K pathway. -
PI3K/Akt Inhibitor
Acetyl-Exenatide is an acetylated derivative of Exenatide, targeting the PI3K/Akt signaling pathway. This compound exhibits insulin-mimetic properties and is instrumental in type 2 diabetes research. Acetyl-Exenatide promotes Th17 differentiation while inhibiting Treg differentiation, and downregulates the phosphorylation of PI3K/Akt/FoxO1, making it a valuable tool for elucidating mechanisms underlying metabolic disorders. -
PI3K p110α Inhibitor
VVD-484 is a selective inhibitor targeting PI3K p110α, exhibiting an IC50 of 0.59 μM against human targets. Classified as a "silent ligand," it forms a covalent bond with Cys242 of PI3K p110α, maintaining the p110α-KRASG12C interaction. VVD-484 effectively inhibits AKT phosphorylation at S473 via a RAS-independent pathway, making it a valuable tool in the research of HER2-overexpressing cancers. -
PI3K Inhibitor
PI3K-IN-56 is a potent and selective irreversible inhibitor of phosphoinositide 3-kinase (PI3K), exhibiting oral bioavailability. This compound effectively blocks the production of phosphatidylinositol-3,4,5-triphosphate (PIP3) and disrupts downstream AKT signaling pathways. Its potential applications in cancer research make PI3K-IN-56 particularly valuable for studies focusing on PI3Kα-driven malignancies, including breast and ovarian cancers. -
PI3K/Akt/mTOR Inhibitor、MAPK Inhibitor、NF-κB Inhibitor
Calebin A is a potent inhibitor of the PI3K/Akt/mTOR pathway, as well as MAPK and NF-κB signaling pathways. It exhibits significant anti-tumor activity through epigenetic regulation and can suppress apoptosis while inhibiting autophagy. Additionally, Calebin A modulates adipogenesis, enhances thermogenic processes, and supports gut microbiota. This compound is suitable for research in various domains, including osteoarthritis, Alzheimer's disease, type 2 diabetes, malignant peripheral nerve sheath tumors, and colorectal cancer. -
PI3Kδ Inhibitor
PI3Kδ-IN-10 is a potent and orally bioavailable inhibitor of the PI3Kδ enzyme, exhibiting an IC50 value of 2 nM. This compound effectively inhibits the downstream AKT signaling pathway, leading to the induction of apoptosis in hepatocellular carcinoma models. Due to its mechanism of action, PI3Kδ-IN-10 is valuable for investigating the role of PI3Kδ in cancer biology and therapeutic development. -
PI3K/Akt/FoxO3a Inhibitor
RLX (PD 139530) is a potent inhibitor of the PI3K/Akt/FoxO3a signaling pathway, exhibiting significant therapeutic potential in colon cancer models. This compound can effectively modulate the tumor microenvironment, thereby enhancing the efficacy of cancer immunotherapy. Additionally, RLX improves the retention time of therapeutic agents in tumors through advanced nanoparticle delivery systems and can be combined with various treatment modalities, such as chemotherapy and radiotherapy, to synergistically enhance cancer treatment outcomes. -
Dual PI3K/mTOR Inhibitor
DHW-221 is a potent dual inhibitor of PI3K and mTOR, demonstrating low nanomolar potency across all four Class I PI3K isoforms (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM) and mTOR (IC50 = 3.9 nM). This compound exhibits significant antitumor activity by disrupting the PI3K/Akt/mTOR signaling pathway, promoting mitochondrial apoptosis and paraptosis via endoplasmic reticulum stress and MAPK signaling, while also hindering cell cycle progression, migration, invasion, and angiogenesis. DHW-221 serves as a valuable tool in research related to non-small cell lung cancer (NSCLC), colon cancer, and breast cancer. -
PI3K Inhibitor
Zandelisib hydrochloride is a selective, non-covalent inhibitor of PI3Kδ, known for its oral bioavailability. By effectively inhibiting AKT phosphorylation, Zandelisib hydrochloride disrupts downstream signaling pathways, making it a valuable tool for investigating the role of the PI3K pathway in various malignancies. This compound is particularly relevant in research focused on relapsed and refractory B-cell lymphoma, enabling studies on tumor behavior and therapeutic responses. -
PI3K/AKT Inhibitor
PI3K/AKT-IN-5 is a selective inhibitor of the PI3K/AKT signaling pathway. It demonstrates potent anti-cancer activity, particularly in colorectal cancer models, by significantly inhibiting cell colony formation, inducing G2/M phase cell cycle arrest, and promoting apoptosis. This compound serves as a valuable tool for research into the mechanisms of colorectal cancer progression and treatment. -
PI3Kδ Inhibitor
PI3Kδ-IN-11 is a potent and selective inhibitor of the PI3Kδ isoform, exhibiting an IC50 value of 27.5 nM. This compound effectively blocks the PI3K/Akt signaling pathway in a dose-dependent manner. PI3Kδ-IN-11 is particularly useful for studying B and T cell-related malignancies, providing valuable insights into therapeutic strategies targeting this pathway. -
PI3K-AKT Inhibitor
Alborixin is a potent inhibitor of the PI3K-AKT signaling pathway that promotes autophagy. It facilitates the clearance of intracellular and extracellular amyloid-β by upregulating key autophagy-related proteins such as BECN1, ATG5, and ATG7, while enhancing lysosomal activity. This mechanism yields a reduction in amyloid-β-mediated neurotoxicity, positioning Alborixin as a valuable tool for research related to Alzheimer's disease and other neurodegenerative conditions. -
PI3K/BRD4 Inhibitor
PI3Kα-IN-28 is a potent dual-target inhibitor of PI3K and BRD4. This compound effectively suppresses cell proliferation in various cancer cell lines, including KYSE180 and KYSE450, while also inhibiting migration and colony formation. Additionally, PI3Kα-IN-28 induces G0/G1 phase cell cycle arrest and promotes cellular senescence by enhancing the proportion of senescent cells. Mechanistically, it decreases the levels of p-AKT and c-Myc, while activating the AMPK-p27 pathway, making it a valuable tool for cancer research, particularly in esophageal cancer studies. -
PI3K/AKT Inhibitor
PI3K/AKT-IN-2 is a selective inhibitor of the phosphoinositide 3-kinase (PI3K) and AKT signaling pathways. This compound effectively prevents epithelial-mesenchymal transition (EMT) and promotes apoptosis in various cancer cell lines. Additionally, PI3K/AKT-IN-2 has been shown to inhibit tubulin polymerization, making it a valuable tool for research into cancer metastasis and cell proliferation.
