PI3K Inhibitor

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.

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.

PI3K-IN-54 (compound 10w) is a pan-PI3K inhibitor. The IC₅₀ values of PI3K-IN-54 for p110α, p110β, and p110δ are 0.22 nM, 1.4 nM, and 0.38 nM, respectively. PI3K-IN-54 can be used in cancer research.

Voxtalisib (Standard) is the analytical standard of Voxtalisib. This product is intended for research and analytical applications. Voxtalisib (XL765) is a potent PI3K inhibitor, which has a similar activity toward class I PI3K (IC50s=39, 113, 9 and 43 nM for p110α, p110β, p110γ and p110δ, respectively), also inhibits DNA-PK (IC50=150 nM) and mTOR (IC50=157 nM). Voxtalisib (XL765) inhibits mTORC1 and mTORC2 with IC50s of 160 and 910 nM, respectively.

Nemiralisib (Standard) is the analytical standard of Nemiralisib. This product is intended for research and analytical applications. Nemiralisib (GSK2269557 free base) is a potent and highly selective PI3Kδ inhibitor with a pKi of 9.9.

TGX-221 (Standard) is the analytical standard of TGX-221. This product is intended for research and analytical applications. TGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, used for cancer treatment.

SAR405 (Standard) is the analytical standard of SAR405 (HY-12481). This product is intended for research and analytical applications. SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC₅₀=1.2 nM; K_d=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity.

mTOR inhibitor-24 (comounp 9d) is a mTOR inhibitor, with IC₅₀s of 0.34 nM (mTOR) and 324 nM (PI3K-α) respectively. mTOR inhibitor-24 inhibtis LNCaP cell proliferation (IC₅₀: 180 nM).

PI3K/mTOR Inhibitor-2 (Standard) is the analytical standard of PI3K/mTOR Inhibitor-2 (HY-111508). This product is intended for research and analytical applications. PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with IC₅₀s of 3.4/34/16/1 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ and 4.7 nM for mTOR. Antitumor activity.