PI3K Inhibitor

Fenitrothion (Standard) is the analytical standard of Fenitrothion (HY-B1885). This product is intended for research and analytical applications. Fenitrothion is a broad-spectrum and orally active insecticide/acaricide. Fenitrothion inhibits cholinesterase, AMPKα and IRS1/PI3K/AKT. Fenitrothion causes Apoptosis, reduces SOD activity. Fenitrothion shows insecticidal effect against Rhyzopertha dominica and Tribolium castaneum adults. Fenitrothion is widely used in cotton crops, vegetable crops, fruit crops and field crops, especially rice. Fenitrothion can be used for brain and spleen toxicology studies.

Ethalfluralin is a dinitroaniline herbicide and microtubule inhibitor. Ethalfluralin blocks nuclear division and cytokinesis of parasites by inhibiting intranuclear spindle formation. Ethalfluralin activates the phosphorylation levels of NF-κB and P38 MAPK, inhibits the PI3K/AKT signaling pathway, impairs mitochondrial function, and induces apoptosis, endoplasmic reticulum stress, autophagy, and ROS production. Ethalfluralin is applicable to research related to toxoplasmosis.

DFX117 is a selective, orally active inhibitor for PI3Kα and c-Met tyrosine kinase. DFX117 inhibits PI3K/Akt/mTOR pathway, inhibits the proliferation of NCI-H1975, NCI-H1993, and HCC827 with IC₅₀s 0.02-0.08 µM. DFX117 arrests cell cycle at G0/G1 phase, induces apoptosis in A549 and NCI-H1975. DFX117 exhibits antitumor efficacy in mice.

mTOR inhibitor-10 (Compound 9c) is a selective inhibitor for mTOR. mTOR inhibitor-10 inhibits mTOR and PI3K-α, with IC₅₀ of 0.7 and 825 nM. mTOR inhibitor-10 inhibits proliferation of LNCaP with IC₅₀ of 87 nM.

Trilinolein (Standard) is the analytical standard of Trilinolein (HY-128393). This product is intended for research and analytical applications. Trilinolein is an orally active triglyceride that inhibits the PI3K/Akt, Ras/MEK/ERK signaling pathways, and MMP-2. Trilinolein can reduce oxidative stress, induce apoptosis, and inhibit cell migration. Trilinolein can be used in the research fields of cardiovascular disease, cerebrovascular disease (such as cerebral ischemia), and non-small cell lung cancer.

IC-87114 (Standard) is the analytical standard of IC-87114. This product is intended for research and analytical applications. IC-87114 is a potent and selective PI3Kδ inhibitor with IC50 of 0.5 μM.

PI3Kγ inhibitor AZ2 (Standard) is the analytical standard of PI3Kγ inhibitor AZ2 (HY-111570). This product is intended for research and analytical applications. PI3Kγ inhibitor AZ2 is a highly selective PI3Kγ inhibitor (The pIC₅₀ value for PI3Kγ is 9.3). PI3Kγ inhibitor AZ2 can be used for the research of inflammatory and immune diseases.

PK_i-179 hydrochloride (Standard) is the analytical standard of PK_i-179 (hydrochloride) (HY-11080A). This product is intended for research and analytical applications. PK_i-179 hydrochloride is a potent and orally active dual PI3K/mTOR inhibitor, with IC₅₀s 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. PK_i-179 hydrochloride also exhibits activity over E545K and H1047R, with IC₅₀s of 14 nM and 11 nM, respectively. PK_i-179 hydrochloride shows anti-tumor activity in vivo.

Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities. Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1). Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes.

Kuwanon G (Standard) is the analytical standard of Kuwanon G (HY-N4247). This product is intended for research and analytical applications. Kuwanon G is a flavonoid compound and an antagonist of the bombesin receptor. Kuwanon G has multiple activities such as bactericidal, anti-tumor, anti-inflammatory, antioxidant, anti-atherosclerotic, and neuroprotective effects. Kuwanon G exhibits strong antibacterial activity against oral pathogens, especially cariogenic bacteria and periodontal pathogens. Kuwanon G can induce apoptosis and inhibit proliferation, migration, and invasion of tumor cells. Kuwanon G can be used in the research of diseases such as gastric cancer and atherosclerosis.

CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC₅₀s of 1.3 and 6.1 nM, respectively.

Taurolithocholic Acid-d₅ (sodium) is the deuterium labeled Taurolithocholic acid sodium salt. Taurolithocholic Acid sodium salt is an orally active bile acid and antiviral agent. Taurolithocholic Acid sodium salt upregulates FADS2 by activating the TGR5-PI3K/AKT-SREBP2 signaling axis, inhibits SFTSV-induced ferroptosis, viral replication and viral entry of HBV/HDV, while reducing the release of IL-1β, lipid ROS and LDH. While exerting antiviral protective effects, Taurolithocholic Acid sodium salt also stimulates the recycling of hepatocellular membrane transporters, impairs canalicular bile acid secretion function, and induces hepatocyte cholestasis, apoptosis and acute hepatocellular injury. Taurolithocholic Acid sodium salt serves as an experimental model compound for hepatocellular cholestasis. At concentrations ≤200 μM, Taurolithocholic Acid sodium salt shows no cytotoxicity and does not activate the interferon pathway. Taurolithocholic Acid sodium salt not only protects mice from lethal SFTSV infection but also is suitable for studies related to severe fever with thrombocytopenia syndrome and cholestasis.

Zandelisib (Standard) is the analytical standard of Zandelisib (HY-109198). This product is intended for research and analytical applications. Zandelisib (ME-401) is a selective, orally active, non-covalent inhibitor of PI3Kδ. Zandelisib can sustainably inhibit AKT phosphorylation and downstream signaling pathways. Zandelisib can be used in the study of malignancies such as relapsed/refractory B-cell lymphoma.

Ginkgolic Acid (C13:0) (Standard) is the analytical standard of Ginkgolic Acid (C13:0) (HY-N0078). This product is intended for research and analytical applications. Ginkgolic Acid (C13:0) (Ginkgoneolic Acid) is an anti-cariogenic agent and a PI3Kδ inhibitor (IC₅₀: 2.49 μM). Ginkgolic Acid (C13:0) exhibits antibacterial and anti-parasitic activities. Ginkgolic Acid (C13:0) can also inhibit mast cell degranulation (IC₅₀: 2.40 μM).

AZD 6482 (Standard) is the analytical standard of AZD 6482 (HY-10344). This product is intended for research and analytical applications. AZD 6482 (KIN-193) is a potent and selective p110β inhibitor with an IC₅₀ of 0.69 nM.

Thymoquinone (Standard) is the analytical standard of Thymoquinone. This product is intended for research and analytical applications. 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 .

Vitexin-2"-O-rhamnoside (Standard) is the analytical standard of Vitexin-2"-O-rhamnoside (HY-N0534). This product is intended for research and analytical applications. Vitexin-2"-O-rhamnoside is an orally active flavonoid glycoside. Vitexin-2"-O-rhamnoside inhibits Apoptosis, increases the phosphorylation levels of PI3K/Akt, inhibits caspase-3, SOD activity, and promotes cytokine (IL-2, IL-6, and IL-12) secretion. Vitexin-2"-O-rhamnoside strongly inhibits DNA synthesis in MCF-7 cells with an IC₅₀ of 17.5 μM. Vitexin-2"-O-rhamnoside enhances immune function and improves the absorption of active compounds. Vitexin-2"-O-rhamnoside has antioxidant activity. Vitexin-2"-O-rhamnoside is used in the study of cardiovascular disease and immune-related diseases.

Apitolisib (Standard) is the analytical standard of Apitolisib. This product is intended for research and analytical applications. Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a Ki of 17 nM for mTOR.

Itacnosertib hydrochloride (Standard) is the analytical standard of Itacnosertib (hydrochloride) (HY-109179A). This product is intended for research and analytical applications. Itacnosertib hydrochloride (TP-0184 hydrochloride) is the inhibitor for FLT3, ACVR1 (ALK2, IC₅₀=8 nM) and JAK2 (IC₅₀=8540 nM). Itacnosertib hydrochloride exhibits anti-leukemic activity.

Pilaralisib (Standard) is the analytical standard of Pilaralisib. This product is intended for research and analytical applications. Pilaralisib (XL147; SAR245408) is a potent and highly selective class I PI3Ks inhibitor with IC50s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ.