PI3K Inhibitor

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.

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.

Nivitol (UP302) is a natural phenolic compound discovered from Dianella ensifolia and also acts as a Tyrosinase inhibitor. Nivitol competitively and reversibly inhibits tyrosinase, suppressing melanin production. Nivitol inhibits homogentisate 1,2-dioxygenase (HGD). In human leukemia cells, Nivitol inhibits PI3K/AKT pathway phosphorylation, increases ROS, decreases mitochondrial membrane potential, and induces G2/M cell cycle arrest, apoptosis, and PINK1/Parkin-mediated mitophagy. Nivitol exhibits inhibition of tumor growth in the MV411 xenograft mouse model. Nivitol is used for research on exogenous ochronosis, hyperpigmentation, and leukemia.

Endoxifen Z-isomer methanesulfonate is an orally active selective PKCβ1 inhibitor with an IC₅₀ of 360 nM against human PKCβ1. It also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer methanesulfonate binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer methanesulfonate inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. It can be used in research related to ER⁺ breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors.

Flavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer.

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

BAY1082439 (Standard) is the analytical standard of BAY1082439 (HY-100886). This product is intended for research and analytical applications. BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth.

Umbralisib (hydrochloride) (Standard) is the analytical standard of Umbralisib (hydrochloride). This product is intended for research and analytical applications. Umbralisib (TGR-1202) hydrochloride is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib hydrochloride exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib hydrochloride can be used for haematological malignancies reseach.

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.

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.

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.

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.

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.