PI3K Inhibitor

Wortmannin (SL-2052; KY-12420) is a potent, selective and irreversible PI3K inhibitor with an IC₅₀ of 3 nM. Wortmannin also blocks autophagy formation, and potently inhibits Polo-like kinase 1 (PlK1) and Plk3 with IC₅₀s of 5.8 and 48 nM, respectively.

α-Linolenic acid (ALA (free base); C18:3 (9Z,12Z,15Z) (free base); C18:3 n-3 (free base)) is an essential fatty acid that cannot be synthesized by humans. α-Linolenic acid can affect the process of thrombotic through the modulation of PI3K/Akt signaling. α-Linolenic acid possess the anti-arrhythmic properties and is related to cardiovascular disease and cancer.

Quercetin hydrate, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC₅₀ of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.

Isorhamnetin is a flavonoid compound extracted from the Chinese herb Hippophae rhamnoides L.. Isorhamnetin suppresses skin cancer through direct inhibition of MEK1 and PI3K.

STX-478 (compound 80) is an oral CNS-penetrant allosteric mutant-selective PI3Kα inhibitor. STX-478 shows robust and durable tumor regression and can be used in cancer research.

D-GsMTx4 is a spider peptide and the D enantiomer of GsMTx4 (HY-P1410). D-GsMTx4 inhibits the mechanosensitive ion channel Piezo2. D-GsMTx4 inhibits [Ca²⁺]_i elevation. D-GsMTx4 inhibits mTOR and PI3K-Akt signaling pathways. D-GsMTx4 inhibits mechanical allodynia and thermal hyperalgesia. D-GsMTx4 can be used in researches of mechanical stress, chronic pain and idiopathic pulmonary fibrosis.

iMDK is a potent PI3K inhibitor and inhibits the growth factor MDK (also known as midkine or MK). iMDK suppresses non-small cell lung cancer (NSCLC) cooperatively with A MEK inhibitor without harming normal cells and mice.

Zovegalisib (RLY-2608) is an orally active first-in-class allosteric mutant-selective inhibitor of PI3Ka with anti-tumor activity. Zovegalisib inhibits tumor growth in PIK3CA-mutant xenograft mice models with minimal impact on insulin.

Liensinine is a bisbenzylisoquinoline alkaloid. By inhibiting the PI3K/AKT and JNK/p38-MAPK signaling pathways, Liensinine suppresses autophagy and apoptosis, clears Aβ, and exerts anti-inflammatory, antioxidant and neuroprotective effects. Liensinine activates AMPK and inhibits the expression of HIF-1α and VEGF, thereby suppressing angiogenesis. Liensinine exerts anti-tumor effects through ROS-mediated inhibition of the JAK2/STAT3 signaling pathway. Liensinine can be used for the research of diseases such as Alzheimer's disease, hepatocellular carcinoma, osteosarcoma, sepsis-induced organ injury and stroke.

Ononin is an orally active isoflavone. Ononin inhibits the ERK/JNK/p38 and PI3K/Akt/mTOR pathways. Ononin regulates Apoptosis. Ononin has anti-tumor effects on laryngeal cancer and lung cancer. Ononin has neuroprotective effects. Ononin alleviates endoplasmic reticulum stress and diabetic nephropathy.

Isoacteoside is a natural product that can significantly inhibit the formation of glycation end products. Isoacteoside regulates the AKT/PI3K/m-TOR/NF-κB signaling pathway, induces apoptosis in OVCAR-3 cell. Isoacteoside exhibits antitumor, anti-inflammatory, anti-obesity and neuroprotective activities.

Thymoquinone is an orally active natural product isolated from N. sativa Thymoquinone down-regulates the VEGFR2-PI3K-Akt pathway. Thymoquinone has antioxidant, anti-inflammatory, anticancer, antiviral, anticonvulsant, antifungal, antiviral, antiangiogenic activity and hepatoprotective effects. Thymoquinone can be used to study Alzheimer's disease, cancer, cardiovascular disease, infectious disease and inflammation .

Oroxin B (OB) is a BBB-permeable flavonoid isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent. Oroxin B (OB) possesses obvious inhibitory effect and induces early apoptosis rather than late apoptosis on liver cancer cells through upregulation of PTEN, down regulation of COX-2, VEGF, PI3K, and p-AKT. Oroxin B (OB) selectively induces tumor-suppressive ER stress in malignant lymphoma cells.

Plantamajoside is an orally active phenylpropanoid glycoside. Plantamajoside can be isolated from Plantago asiatica L.(Plantaginaceae). Plantamajoside inactivates NF-κB, PI3K/akt, induces Apoptosis, and improves Autophagy. Plantamajoside regulates MAPK, integrin-linked kinase/c-Src. Plantamajoside inhibits multiple cancers, improves lung and kidney damage. Plantamajoside has neuroprotective and anti-inflammatory effects.

Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities.

Ginsenoside Rk1 is a unique component created by processing the ginseng plant (mainly Sung Ginseng, SG) at high temperatures. Ginsenoside Rk1 has anti-inflammatory effect, suppresses the activation of Jak2/Stat3 signaling pathway and NF-κB. Ginsenoside Rk1 has anti-tumor effect, antiplatelet aggregation activities, anti-insulin resistance, nephroprotective effect, antimicrobial effect, cognitive function enhancement, lipid accumulation reduction and prevents osteoporosis. Ginsenoside Rk1 induces cell apoptosis by triggering intracellular reactive oxygen species (ROS) generation and blocking PI3K/Akt pathway.

Quercetin (Standard) is the analytical standard of Quercetin. This product is intended for research and analytical applications. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.

GO-203 TFA is a potent MUC1-C oncoprotein inhibitor. GO-203 TFA is an all D-amino acid peptide that consists of a poly-R transduction domain linked to a CQCRRKN motif that binds to the MUC1-C cytoplasmic tail and blocks MUC1-C homodimerization. GO-203 TFA downregulates TIGAR (TP53-induced glycolysis and apoptosis regulator) protein synthesis by inhibiting the PI3K-AKT-S6K1 pathway. GO-203 TFA induces the production of ROS and loss of mitochondrial transmembrane potential. GO-203 TFA inhibits the growth of colon cancer cells in vitro and as xenografts in nude mice.

D-GsMTx4 TFA is a spider peptide and the D enantiomer of GsMTx4 (HY-P1410). D-GsMTx4 TFA inhibits the mechanosensitive ion channel Piezo2. D-GsMTx4 TFA inhibits [Ca²⁺]_i elevation. D-GsMTx4 TFA inhibits mTOR and PI3K-Akt signaling pathways. D-GsMTx4 TFA inhibits mechanical allodynia and thermal hyperalgesia. D-GsMTx4 TFA can be used in researches of mechanical stress, chronic pain and idiopathic pulmonary fibrosis.

Sophocarpine is a PTEN activator and an inhibitor of PI3K/Akt, MEK/ERK, and NF-κB signaling pathways. Sophocarpine upregulates PTEN expression and inhibits PI3K/Akt phosphorylation, arrests tumor cell cycle and induces apoptosis. Sophocarpine inhibits MEK/ERK phosphorylation and VEGF secretion, reducing tumor cell migration. Sophocarpine can also inhibit NF-κB activation and p38 and JNK phosphorylation, reduce the expression of inflammatory factors such as iNOS and COX-2, and activate the Nrf2/HO-1 pathway to reduce oxidative stress. Sophocarpine has anti-tumor, anti-inflammatory, antioxidant and anti-apoptotic effects, and can be used in the research of cancers such as glioblastoma and colorectal cancer, inflammation-related diseases, and Doxorubicin (HY-15142A)-induced cardiac damage.