Catalog No.
Product Name
Application
Product Information
Citations
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mTOR/PI3K Inhibitor,
GSK2126458 is a highly potent, orally bioavailable inhibitor of PI3Kα and mTOR with in vivo activity in both pharmacodynamic and tumor growth efficacy models. -
p110β inhibitor
Rac)-AZD 6482 ((Rac)-KIN-193) is a less active racemate of AZD 6482. AZD 6482 is a potent and selective p110β inhibitor with an IC50 of 0.69 nM. -
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]. -
anti-tumor agent
Sophocarpine (monohydrate) is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. -
monounsaturated fatty acid
Erucic acid, a monounsaturated fatty acid (MUFA), is isolated from the seed of Raphanus sativus L. Erucic acid can readily cross the blood-brain barrier (BBB), it has been reported to normalize the accumulation of very long-chain fatty acids in the brain. Erucic acid can improve cognitive impairment and be effective against dementia . -
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). -
PI3K Activator
UCL-TRO-1938 is a potent allosteric activator of phosphoinositide 3-kinase alpha (PI3Kα), exhibiting an EC50 value of approximately 60 μM. This compound promotes cell proliferation and demonstrates cardioprotective effects against ischemia-reperfusion injury. Additionally, UCL-TRO-1938 enhances nerve regeneration following nerve crush, making it a valuable tool in neuroprotection and regenerative medicine research. -
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/CREB Activator
PI3K/Akt/CREB activator 1 is a potent, orally active compound that stimulates the PI3K/Akt/CREB signaling pathway. This activator promotes neuronal proliferation, induces differentiation of Neuro-2a cells into neuron-like cells, and facilitates the axon-dendrite polarization in primary hippocampal neurons by upregulating brain-derived neurotrophic factor. It is particularly relevant for research into vascular dementia (VaD). -
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. -
Anti-Insect Agent
Methyl Eugenol is an anti-insect agent primarily effective against the oriental fruit fly (Bactrocera dorsalis). In addition to its insecticidal properties, Methyl Eugenol exhibits anti-cancer and anti-inflammatory activities, making it a versatile compound for biological research. It has been shown to induce autophagy in cells and can be utilized in studies related to intestinal ischemia/reperfusion injury. -
AMPK Agonist
10-Gingerol is an AMPK agonist derived from ginger oleoresin, exhibiting notable anti-inflammatory, antioxidant, and anti-proliferative properties. It effectively suppresses neointimal hyperplasia and inhibits the proliferation of vascular smooth muscle cells. Demonstrating significant radical scavenging activities, 10-Gingerol has IC50 values of 10.47 μM against DPPH, 1.68 μM against superoxide, and 1.35 μM against hydroxyl radicals. This compound also inhibits MDA-MB-231 tumor cell line proliferation with an IC50 of 12.1 μM, while targeting the PI3K/Akt signaling pathway to suppress proliferation, migration, invasion, and promote apoptosis. It holds potential for research applications in ulcerative colitis. -
Glycosaminoglycan
Hyaluronic acid sodium, also known as sodium hyaluronate, is a glycosaminoglycan that plays a crucial role in the extracellular matrix (ECM). This biopolymer is involved in key biological activities such as cell proliferation, tissue remodeling, and angiogenesis, particularly in the context of digestive cancers. Hyaluronic acid sodium is implicated in tumor cell growth and migration, and it activates the PI3K-Akt signaling pathway. This reagent can also be utilized in research related to joint diseases, wound healing, and as a drug delivery system to enhance the efficacy of therapeutics in cancer research. -
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. - Lipoteichoic acid is an orally active compound with anti-inflammatory and antitumor properties. It is a key immune molecule found in Gram-positive bacteria that activates the complement system by upregulating C3 and inhibiting CD55. Lipoteichoic acid modulates macrophage autophagy via the PI3K/Akt/mTOR pathway, induces lung injury in mouse models, and inhibits melanin production.
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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. - Hirsutenone is a bioactive diarylheptanoid derived from *Alnus* species, known for its anti-inflammatory, anti-tumor-promoting, and anti-atopic dermatitis properties. It attenuates adipogenesis by directly binding to PI3K and ERK1 in a non-ATP competitive manner. Hirsutenone is a valuable compound for research related to obesity and metabolic disorders.
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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. -
BMP receptor agonist
SY-LB-35 is a potent agonist of bone morphogenetic protein (BMP) receptors, capable of activating both canonical and non-canonical signaling pathways. In the C2C12 myoblast cell line, SY-LB-35 significantly enhances cell proliferation and viability, promoting cell cycle progression by increasing the proportion of cells in the S and G2/M phases. Mechanistically, it activates the canonical Smad pathway as well as non-canonical PI3K/Akt, ERK, p38, and JNK signaling cascades. These properties make SY-LB-35 a valuable tool for studying BMP-related cellular processes and a potential therapeutic candidate for tissue regeneration and muscle repair. -
PIK3CG PROTAC degrader
ARM165 is a heterobifunctional PROTAC molecule that targets and degrades PIK3CG (PI3Kγ), effectively inhibiting the PI3Kγ-Akt signaling pathway. It exhibits potent antileukemic activity, suppressing the proliferation of acute myeloid leukemia (AML) cells with an IC₅₀ of less than 1 μM. ARM165 is a promising tool for investigating PI3Kγ-driven signaling and developing targeted therapies for leukemia. -
PROTAC PIKfyve degrade
PIK5-12d is a potent PROTAC degrader targeting PIKfyve, with a DC₅₀ of 1.48 nM. It induces extensive cytoplasmic vacuolization, disrupts autophagic flux, and inhibits proliferation in multiple prostate cancer cell lines. PIK5-12d exhibits notable anti-tumor activity, supporting its use in cancer research. -
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.
