PI3K Inhibitor

mTOR inhibitor-13 (compound 9g), an aryl ureido compound, is a potent and selective mTOR inhibitor with an IC₅₀ of 0.29 nM. mTOR inhibitor-13 also inhibits PI3K-α with an IC₅₀ of 119 nM.

PIK-75 (Standard) is the analytical standard of PIK-75 (HY-107834). This product is intended for research and analytical applications. PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC₅₀s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC₅₀=1.3 μM). PIK-75 induces apoptosis.

Leupeptin hydrochloride is a broad-spectrum protease inhibitor. By inhibiting the activation of the PTEN/PI3K/Akt/NF-κB/ERK1/2/p38 signaling pathway, Leupeptin hydrochloride significantly reduces LPS-induced NO and ROS production, mitochondrial membrane potential hyperpolarization, phagocytic activity, pro-inflammatory cytokine release, and M1 polarization in mouse peritoneal macrophages, and reverses autophagic flux impairment. It also decreases Concanavalin A (HY-P2149)-induced proliferation index of mouse splenic lymphocytes and the Th1/IL-10 and Th2/IL-10 cytokine ratios, thereby modulating innate and adaptive immune responses. Leupeptin hydrochloride inhibits blood coagulation and tumorigenesis in mouse skin. Leupeptin hydrochloride can be used in research on chronic inflammatory diseases and skin tumorigenesis.

PI3Kα-IN-24 (WR23) is a PI3Kα inhibitor with an IC₅₀ of 0.025 μM and exhibits a significant pAkt^Ser473 suppression effect. PI3Kα-IN-24 can be utilized in cancer research.

BMS-554417 is an orally active inhibitor of insulin receptor and insulin-like growth factor-I receptor (IGF-1R) kinases, with IC₅₀ values of 50.6 nM and 67.9 nM, respectively. BMS-554417 blocks downstream signal transduction via the ERK and PI3K/Akt pathways. BMS-554417 induces G0-G1 cell cycle arrest, prevents cyclin D1 accumulation in the nucleus, triggers mitochondrial pathway-mediated apoptosis, promotes HER2 phosphorylation, and inhibits the proliferation and growth of cancer cells. BMS-554417 can be used in research related to colon cancer, ovarian cancer, and breast cancer.

PK_i-179 (Standard) is the analytical standard of PK_i-179 (HY-11080). This product is intended for research and analytical applications. PK_i-179 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 also exhibits activity over E545K and H1047R, with IC₅₀s of 14 nM and 11 nM, respectively. PK_i-179 shows anti-tumor activity in vivo.

Liriodendrin is an orally effective lignan compound with anti-inflammatory, antioxidant, and anti-platelet aggregation activities. Liriodendrin is isolated and extracted from Sargentodoxae caulis and Linaria vulgaris. Liriodendrin regulates the expression of genes related to inflammation and cellular metabolism by inhibiting the NF-κB, PI3K/Akt, and TLR4 signaling pathways, or by activating the PI3K-DDX18 pathway. Liriodendrin increases the expression of HSF1 and HSP27 without cytotoxicity. Liriodendrin is used in studies on ulcerative colitis, myocardial ischemia-reperfusion injury, sepsis-induced acute lung injury, and chronic endometritis.

PI3Kα-IN-17 (example 4) is a potent inhibitor of PI3Kα.

Pilaralisib analogue (Standard) is the analytical standard of Pilaralisib analogue (HY-11105). This product is intended for research and analytical applications. Pilaralisib analogue (XL147 analogue) is a representative and selective PI3Kα inhibitor extracted from patent WO2012006552A1, Compound 147 in Table 1.

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

Bruceoside B is a PI3K/Akt/NF-κB inhibitor. Bruceoside B reduces LPS (HY-D1056)-induced nitric oxide release and the secretion of TNF-α, IL-6 and IL-1β, and decreases the activation level of apoptosis. Bruceoside B inhibits the replication, coat protein accumulation and local lesion formation of tobacco mosaic virus (TMV), and enhances the anti-infection ability of plants. Bruceoside B can be used in studies related to acute lung injury and tobacco mosaic virus infection.

mTOR inhibitor-17 (Compound 9e) is a selective inhibitor for mTOR. mTOR inhibitor-10 inhibits mTOR and PI3K-α, with IC₅₀ of 0.68 and 1359 nM. mTOR inhibitor-10 inhibits proliferation of LNCaP with IC₅₀ of 40 nM.

PIK-108 (Standard) is the analytical standard of PIK-108 (HY-111184). This product is intended for research and analytical applications. PIK-108 is a non-ATP competitive, allosteric p110β/p110δ selective inhibitor.

Idelalisib (Standard) is the analytical standard of Idelalisib. This product is intended for research and analytical applications. Idelalisib (CAL-101; GS-1101) is a highly selective and orally bioavailable p110δ inhibitor with an IC50 of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.

PI3Kδ-IN-1 (Standard) is the analytical standard of PI3Kδ-IN-1 (HY-101921). This product is intended for research and analytical applications. PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC₅₀ of 1.7 nM.

RV-6153 is a potent and selective dual inhibitor of PI3Kδ and PI3Kγ, with IC₅₀ values of 2.5 nM and 28 nM, respectively. RV-6153 dually inhibits PI3Kδ and PI3Kγ, blocking Akt phosphorylation, thereby inhibiting ROS production and cytokine release at the cellular level, and reducing neutrophil and macrophage accumulation in the airways in vivo. RV-6153 can be used in research on chronic obstructive pulmonary disease, asthma, and other inflammatory diseases.

SF2523 (Standard) is the analytical standard of SF2523 (HY-101146). This product is intended for research and analytical applications. SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.

PI4K-IN-3 (Compound 27) is an orally active PI4K inhibitor with an IC₅₀ of 1.9  nM for Plasmodium vivax PI4K. PI4K-IN-3 has no hERG channel inhibition and mammalian cytotoxicity. PI4K-IN-3 has significant selectivity against the human MINK1 and MAP4K4 kinases but with low selectivity against human PI3Kα and PI4Kβ. PI4K-IN-3 has potent antimalarial activity and significantly reduces parasitaemia in NSG mice mouse models of Plasmodium falciparum malaria.

Molephantin is a blood-brain barrier permeable anti-glioblastoma compound. Molephantin induces ROS generation, leading to mitochondrial damage, Mitophagy flux blockage and Apoptosis induction. Molephantin can suppress the PI3K/Akt/mTOR signaling pathway. Molephantin demonstrates antitumor effects against glioblastoma.

2C07 is a mutant Ras (K-Ras^M72C, H-Ras^M72C) inhibitor. 2C07 blocks the activation of PI3K through allosteric Ras modification. 2C07 binds to the modified switch II pocket (S-IIG) of Ras in both GDP- and GTP-bound states, stabilizes the GDP-bound state, disrupts the polar interactions of the canonical GTP-bound state, and inhibits SOS binding and nucleotide exchange. 2C07 can be used in cancer-related research.