PI3K Inhibitor

PI3K/Akt/mTOR-IN-5 (compound D3) is a derivative of Pseudolaric Acid B (HY-N6939) with anti-tumor activity. PI3K/Akt/mTOR-IN-5 inhibits excessive proliferation of tumor cells through the PI3K/AKT/mTOR and STAT3/GPX4 pathways. PI3K/Akt/mTOR-IN-5 effectively inhibits EDU positivity, reduces colony formation, places HCT-116 cells in the S phase and G2/M phase, and induces apoptosis.

PI3K/PIKK-IN-1 is a PI3K and PIKK inhibitor that serves as a payload for antibody-drug conjugates (ADC) to prepare ADC. PI3K/PIKK-IN-1 is applicable to research related to breast cancer, multiple myeloma, Burkitt lymphoma, diffuse large B-cell lymphoma, and non-small cell lung cancer.

PI3Kα-IN-12 (compound 13) is a highly selective PI3Kα inhibitor (IC₅₀: 1.2 nM). PI3Kα-IN-12 inhibits HCT-116 and U87-MG with IC₅₀s values of 0.83 and 1.25 μM, respectively. PI3Kα-IN-12 (40 mg/kg; IP) causes tumor regression in a U87-MG cell line xenograft mouse model.

Oroselol is a coumarin commonly found in a variety of plants, especially in the roots of angelica plants and the bark of cinnamon trees. Oroselol has potential medicinal properties, including anti-inflammatory, antioxidant and anti-tumor effects. Oroselol can be used in the production of fragrances, flavors and medicines

EGFR-IN-196 is an EGFR inhibitor with an IC₅₀ of 105.96 nM. EGFR-IN-196 inhibits EGFR enzymatic activity, reduces phosphorylated PI3K levels, and suppresses downstream EGFR-AKT signaling. EGFR-IN-196 increases intracellular ROS generation, induces mitochondrial depolarisation, and induces apoptosis in cancer cells. EGFR-IN-196 can be used for the research of lung cancer.

Jujuboside B (Standard) is the analytical standard of Jujuboside B. This product is intended for research and analytical applications. Jujuboside B is a bioactive saponin component isolated from Ziziphi Spinosae Semen (sour jujube seed), with oral efficacy and blood-brain barrier permeability. Jujuboside B induces acute leukemia cell death and drives necroptosis apoptosis by activating the RIPK1/RIPK3/MLKL pathway. Jujuboside B upregulates the expression of NOXA, PARP and caspase-3, activates AMPK, inhibits the proliferation of breast cancer cells, and induces cell apoptosis and autophagy. Jujuboside B inhibits angiogenesis and tumor growth by blocking the VEGFR-2 signaling pathway. Jujuboside B alleviates liver injury in mice by regulating the Nrf2-STING signaling pathway. Jujuboside B alleviates liver injury by regulating anti-inflammatory responses and downregulating the expression of 11β-HSD2. Jujuboside B induces ferroptosis and overcomes radioresistance in non-small cell lung cancer via the PPARγ-ATF3-Gpx4 signaling pathway. Jujuboside B exerts inhibitory effects on platelet aggregation. Jujuboside B inhibits febrile seizures by suppressing the activity of AMPA receptors. Jujuboside B reverses chronic unpredictable mild stress-promoted tumor progression by blocking the PI3K/Akt and MAPK/ERK pathways and dephosphorylating CREB signaling. Jujuboside B is applicable to related studies on acute leukemia, breast cancer, PM_2.5-induced lung injury, hepatotoxicity, liver injury, colorectal cancer, non-small cell lung cancer, thromboembolic diseases, cardiovascular diseases associated with high platelet aggregation, febrile seizures, and depressive-like phenotypes.

Anticancer agent 137 (8q) is a potent PI3k inhibitor. Anticancer agent 137 has broad-spectrum anticancer activity. Anticancer agent 137 induces G2/M cell cycle arrest and apoptosis. Anticancer agent 137 increases cleaved PARP, caspase 3, and 7. Anticancer agent 137 can be used in research of cancer.

PI3K/mTOR Inhibitor-5 (compound 19a) is a potent and dual PI3K and mTOR inhibitor, with IC₅₀ values of 86.9 nM and 14.6 nM, respectively.

(±)-10-Gingerol is the racemic form of 10-Gingerol (HY-N0448). 10-Gingerol is an AMPK agonist, which is found in the ginger oleoresin from fresh rhizome with anti-inflammatory, antioxidant and anti-proliferative activities. 10-Gingerol suppresses neointimal hyperplasia and inhibits vascular smooth muscle cell proliferation. 10-Gingerol exhibits substantial scavenging activities with an IC₅₀ value of 10.47 μM against DPPH radical, an IC₅₀ value of 1.68 μM against superoxide radical and an IC₅₀ value of 1.35 μM against hydroxyl radical. 10-Gingerol inhibits the proliferation of MDA-MB-231 tumor cell line with an IC₅₀ of 12.1 μM. 10-Gingerol suppresses the proliferation, migration, invasion, and induced apoptosis through targeting the PI3K/Akt signaling pathway in MDA-MB-231/IR cells. 10-Gingerol can be used in research on various common cancers such as ovarian cancer and colon cancer, as well as colitis and neurodegenerative diseases.

EGFR/PI3Kα-IN-1 (compound 30k) is a dual EGFR/PI3Kα inhibitor with IC₅₀ values of 3.6 nM (EGFRL858R/T790M) and 30 nM (PI3Kα), respectively. EGFR/PI3Kα-IN-1 can inhibit tumor cell proliferation and has anticancer activity.

EGFR-IN-192 is an anticancer agent. EGFR-IN-192 inhibits EGFR (IC₅₀: 0.12 μM), downregulates the HIF-VEGF and PI3K/AKT/mTOR pathways, upregulates the tumor suppressor gene PTEN, and induces cell cycle arrest and apoptosis in tumor cells. EGFR-IN-192 exhibits antitumor activity and can be used in tumor research.

Penetratin-PI3Kγ(126-150) is a peptide inhibitor of ΡI3Κγ that plays an important role in respiratory system diseases.

RLX (PD 139530) is a PI3K/Akt/FoxO3a signaling inhibitor, possessing significant therapeutic potential in experimental colon cancer. RLX can effectively modulate the tumor microenvironment, enhancing the efficacy of cancer immunotherapy. RLX demonstrates the ability to improve the retention time of therapeutic agents within the tumor microenvironment by utilizing advanced nanoparticle delivery systems. RLX can be integrated with various treatment modalities, such as chemotherapy and radiotherapy, to enhance overall tumor therapy effectiveness.

Zandelisib (ME-401) hydrochloride is a selective, orally active, non-covalent inhibitor of PI3Kδ. Zandelisib hydrochloride can sustainably inhibit AKT phosphorylation and downstream signaling pathways. Zandelisib hydrochloride can be used in the study of malignancies such as relapsed/refractory B-cell lymphoma.

Antiproliferative agent-67 (Compound 5g) is a PI3K inhibitor with a selectivity index SI of 7.72 for breast cancer cells (MCF-7). Antiproliferative agent-67 inhibits the activity of PI3K protein by forming hydrogen bonds and intermolecular hydrophobic forces with it, exerting anti - proliferative activity against breast cancer cells (MCF-7), and can be used in the research of breast cancer.

FAP-PI3KI1 is a fibroblast-activated protein (FAP)-targeted PI3K inhibitor that selectively targets FAP-expressing human idiopathic pulmonary fibrosis (IPF) cells and effectively inhibits collagen synthesis and reduces collagen deposition.

PI3K/AKT-IN-5 (Compound 3h) is a PI3K/AKT inhibitor. PI3K/AKT-IN-5 exhibits outstanding broad-spectrum anti-cancer activity, especially being sensitive to colorectal cancer. PI3K/AKT-IN-5 significantly reduces cell colony formation, induces G2/M phase cell cycle arrest and cell apoptosis. PI3K/AKT-IN-5 can be used for research on colorectal cancer.

PI3K-IN-28 (Compound 6c) is a potent inhibitor of PI3K. PI3K-IN-28 displays the most potent activity with lower toxic effects on MCF-10a. PI3K-IN-28 displays half-maximal inhibitory concentration (IC₅₀, μM) values of 5.8, 2.3, and 7.9. PI3K-IN-28 is the most potent one with a selectivity index (SI) of 39 and is considered as a latent lead for further optimization of anticancer agents.

Myrislignan-13C,d2 is the ¹³C, d₂ deuterated-labeled Myrislignan (HY-N0608). Myrislignan is a PI3K/AKT/NF-κB inhibitor that can cross the blood-brain barrier. Myrislignan exerts anticancer activity by inducing apoptosis and ferroptosis. Myrislignan inhibits the replication and invasion of Toxoplasma gondii; it induces reactive oxygen species (ROS) imbalance, autophagy, and the death of Toxoplasma gondii tachyzoites. Myrislignan inhibits mitochondrial function and ERK1/2 phosphorylation to improve ovariectomy-induced osteoporosis. Myrislignan can be used in studies related to gastric cancer, glioblastoma, osteoporosis, and toxoplasmosis.

Dezapelisib (NCB040093) is a potent inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ). Dezapelisib is a promising research strategy for select R/R B-cell lymphomas.