PI3K

Phosphoinositide 3-kinases (PI3Ks) are lipid kinases that catalyze the phosphorylation of phosphatidylinositol 4,5-bisphosphate (PI(4,5)P₂) to generate the second messenger phosphatidylinositol (3,4,5)-trisphosphate (PI(3,4,5)P₃). The production of PI(3,4,5)P₃ facilitates the recruitment and activation of pleckstrin homology (PH) domain–containing proteins at the plasma membrane, thereby initiating downstream signaling cascades essential for cellular proliferation, survival, and migration.

PI3Ks are divided into three major classes, among which Class I PI3Ks are most prominently implicated in cancer biology. Class I enzymes comprise four distinct catalytic isoforms: PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ.

Class IA PI3Ks, the subclass most commonly associated with oncogenic signaling, function as heterodimeric lipid kinases composed of a catalytic p110 subunit (p110α, p110β, or p110δ, encoded by PIK3CA, PIK3CB, and PIK3CD, respectively) and a regulatory p85 subunit.

The PI3K signaling pathway plays a central role in diverse biological processes, including cell cycle progression, cellular growth, survival, actin cytoskeletal rearrangement, migration, and intracellular vesicular trafficking.

Frequently Asked Questions
Phosphoinositide 3-kinases (PI3Ks) are a family of lipid kinases that phosphorylate phosphatidylinositol lipids to regulate cell growth, survival, metabolism, and immune signaling. PI3K activation leads to downstream AKT and mTOR pathway signaling. Aberrant PI3K signaling is frequently observed in cancer due to PIK3CA mutations, PTEN loss, or receptor tyrosine kinase activation.
Class I PI3Ks include four catalytic isoforms: PI3Kα (PIK3CA) PI3Kβ (PIK3CB) PI3Kδ (PIK3CD) PI3Kγ (PIK3CG) PI3Kα and β are broadly expressed, while PI3Kδ and γ are enriched in leukocytes and play critical roles in immune regulation. Isoform selectivity is an important consideration in drug development due to toxicity and immune effects.
PI3K inhibitors can be classified as: Pan-PI3K inhibitors Isoform-selective inhibitors (α, β, δ, γ) Dual PI3K/mTOR inhibitors Irreversible inhibitors Selectivity influences therapeutic window and toxicity profile.
While PI3K inhibitors block upstream lipid kinase activity, mTOR inhibitors act downstream at the level of mTORC1 or mTORC2. Dual PI3K/mTOR inhibitors target both nodes of the pathway and may achieve broader pathway suppression.

4 Items

  • 10-Gingerol
    Cat. No.
    A14475

    10-Gingerol

    10-Gingerol is an AMPK agonist derived from ginger oleoresin, exhibiting notable anti-inflammatory, antioxidant, and anti-proliferative properties. It effectively suppresses neointimal hyperplasia and inhibits the proliferation of vascular smooth muscle cells. Demonstrating significant radical scavenging activities, 10-Gingerol has IC50 values of 10.47 μM against DPPH, 1.68 μM against superoxide, and 1.35 μM against hydroxyl radicals. This compound also inhibits MDA-MB-231 tumor cell line proliferation with an IC50 of 12.1 μM, while targeting the PI3K/Akt signaling pathway to suppress proliferation, migration, invasion, and promote apoptosis. It holds potential for research applications in ulcerative colitis.

    5 mg
    $70.00
    10 mg
    $130.00
    All 6 sizes
  • SY-LB-35
    Cat. No.
    A24106

    SY-LB-35

    SY-LB-35 is a potent agonist of bone morphogenetic protein (BMP) receptors, capable of activating both canonical and non-canonical signaling pathways. In the C2C12 myoblast cell line, SY-LB-35 significantly enhances cell proliferation and viability, promoting cell cycle progression by increasing the proportion of cells in the S and G2/M phases. Mechanistically, it activates the canonical Smad pathway as well as non-canonical PI3K/Akt, ERK, p38, and JNK signaling cascades. These properties make SY-LB-35 a valuable tool for studying BMP-related cellular processes and a potential therapeutic candidate for tissue regeneration and muscle repair.

    5 mg
    $59.00
    10 mg
    $101.00
    All 4 sizes
  • 20-5,14-HEDE
    Cat. No.
    A25381

    20-5,14-HEDE

    Synonyms: WIT003

    20-5,14-HEDE is a synthetic analog of 20-HETE that primarily targets the PI3K/Akt signaling pathway. This compound exhibits significant anti-apoptotic properties and promotes cell survival, making it valuable for studies related to cellular resilience. Additionally, 20-5,14-HEDE functions as an agonist for 20-HETE, increasing intracellular calcium levels and enhancing vasoconstriction. Its multifaceted biological activities make it suitable for research in cardiovascular and cellular signaling pathways.

    1 mg
    $785.00
    5 mg
    $2,010.00
    All 3 sizes
  • Propylparaben sodium
    Cat. No.
    A31961

    Propylparaben sodium

    Synonyms: Propyl parahydroxybenzoate sodium; Propyl 4-hydroxybenzoate sodium

    Propylparaben sodium acts as a weak estrogen receptor agonist and serves as a voltage-gated sodium channel blocker, while also modulating the PI3K-AKT and JNK signaling pathways. It is known to induce oxidative stress, affecting the estrous cycle and hormone levels, as well as ovarian reserve function. Propylparaben sodium can inhibit the growth of antral follicles and influence the accumulation of steroid hormones in follicle culture media. This compound is suitable for research related to ovarian aging and myocardial ischemia-reperfusion injury.

    5 mg
    $20.00
    100 mg
    $25.00
    All 4 sizes

4 Items

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