1. PI3K/Akt/mTOR
  2. PI3K

PI3K

PI3K (Phosphoinositide 3-kinase), via phosphorylation of the inositol lipid phosphatidylinositol 4,5-bisphosphate (PI(4,5)P2), forms the second messenger molecule phosphatidylinositol (3,4,5)-trisphosphate (PI(3,4,5)P3) which recruits and activates pleckstrin homology domain containing proteins, leading to downstream signalling events crucial for proliferation, survival and migration. Class I PI3K enzymes consist of four distinct catalytic isoforms, PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ.

There are three major classes of PI3K enzymes, being class IA widely associated to cancer. Class IA PI3K are heterodimeric lipid kinases composed of a catalytic subunit (p110α, p110β, or p110δ; encoded by PIK3CA, PIK3CB, and PIK3CD genes, respectively) and a regulatory subunit (p85).

The PI3K pathway plays an important role in many biological processes, including cell cycle progression, cell growth, survival, actin rearrangement and migration, and intracellular vesicular transport.

PI3K Related Products (389):

Cat. No. Product Name Effect Purity
  • HY-18085
    Quercetin Inhibitor
    Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively[1].
  • HY-15244
    Alpelisib Inhibitor 99.95%
    Alpelisib (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. Alpelisib (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. Alpelisib (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC50s of 5/250/290/1200 nM, respectively. Antineoplastic activity[1][2][3].
  • HY-10108
    LY294002 Inhibitor
    LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively[1]. LY294002 also inhibits CK2 with an IC50 of 98 nM[2]. LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an apoptosis activator[3].
  • HY-P0175
    740 Y-P Activator 99.67%
    740 Y-P (740YPDGFR; PDGFR 740Y-P) is a potent and cell-permeable PI3K activator. 740 Y-P readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone[1].
  • HY-19312
    3-Methyladenine Inhibitor
    3-Methyladenine (3-MA) is a PI3K inhibitor. 3-Methyladenine is a widely used inhibitor of autophagy via its inhibitory effect on class III PI3K[1].
  • HY-161366
    OMS14 Inhibitor
    OMS14 is exhibits inhibitory activity for phosphoinositide 3-kinase γ (PI3Kγ) and PIK3CD/PIK3R1, which inhibits 19% PI3Kγ and 65% PIK3CD/PIK3R1 activity at 100 μM. OMS14 exhibits anticancer efficacy in various cancer cells[1].
  • HY-162382
    KTC1101 Inhibitor
    KTC1101 is an orally active pan-PI3K inhibitor. KTC1101 can inhibit the PI3K signaling pathway, reduce downstream AKT and mTOR phosphorylation, and reduces the expression of Ki67. The anti-tumor effect of KTC1101 has a dual mechanism of action: directly inhibiting tumor cell growth and dynamically enhancing immune response[1].
  • HY-101776A
    Desmethyl-VS-5584 hydrochloride Inhibitor 98.63%
    Desmethyl-VS-5584 hydrochloride
  • HY-147767
    PI3Kα-IN-6 Inhibitor
    PI3Kα-IN-6 (Compound 5b) is a PI3Kα inhibitor. PI3Kα-IN-6 exhibits anticancer potential and no toxicity in normal cells. PI3Kα-IN-6 increases generation of ROS, reduces mitochondrial membrane potential (MMP) and induces apoptosis[1].
  • HY-70063
    Buparlisib Inhibitor 99.90%
    Buparlisib (BKM120; NVP-BKM120) is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.
  • HY-125542
    DCZ3301 Inhibitor
    DCZ3301 is a potent aryl-guanidino inhibitor. DCZ3301 inhibits cell proliferation, induces G2/M cell cycle arrest and apoptosis. DCZ3301 inhibits the activation of the PI3K/AKT pathway by downregulating the protein expression of PI3K and phosphorylation of AKT. DCZ3301 can be used in research of cancer[1].
  • HY-D0254
    Gallein
    Gallein is a G protein βγ (Gβγ) subunit signalling inhibitor. Gallein disrupts the interaction of Gβγ subunits with the PI3Kγ. Anticancer agent[1]. Gallein used as a red dye, an acid-base indicator and as a detection reagent for phosphates[2].
  • HY-147284
    PI3K-IN-37 Inhibitor
    PI3K-IN-37 (Example 84.1) is a PI3K α/β/δ inhibitor with IC50s of 6, 8, 4 nM, respectively. PI3K-IN-37 can also inhibit mTOR (IC50=4 nM)[1].
  • HY-10683
    PKI-402 Inhibitor 98.43%
    PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC50=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).
  • HY-15174
    Dactolisib Tosylate Inhibitor 99.87%
    Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.
  • HY-100398
    PF-04979064 Inhibitor 99.83%
    PF-04979064 is a potent and selective PI3K/mTOR dual kinase inhibitor with Kis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively.
  • HY-155211
    mTOR inhibitor-13 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[1].
  • HY-147285
    PI3K/mTOR Inhibitor-9 Inhibitor
    PI3K/mTOR Inhibitor-9 (Compound 1) is a potent mTOR and PI3K inhibitor with IC50 values of 38 nM, 6.6 μM, 6.6 μM and 0.8 μM against mTOR (phospho-S6 cellular assay), PI3Kα, PI3Kγ and PI3Kδ, respectively[1].
  • HY-N0728S
    α-Linolenic acid-d5 Inhibitor
    α-Linolenic acid-d5 is the deuterium labeled α-Linolenic acid. α-Linolenic acid, isolated from seed oils, is an essential fatty acid that cannot be synthesized by humans. α-Linolenic acid can affect the process of thrombotic through the modulation of PI3K/Akt signaling. α-Linolenic acid possess the anti-arrhythmic properties and is related to cardiovascular disease and cancer[1].
  • HY-11042
    GNE-477 Inhibitor 98.70%
    GNE-477 is a potent and efficacious dual PI3K (IC50=4 nM)/mTOR(Ki=21 nM) inhibitor.