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.

3 Items

  • PI3K/mTOR ligand-1
    Cat. No.
    A79740

    PI3K/mTOR ligand-1

    PI3K/mTOR ligand-1 is a ligand targeting the PI3K/mTOR pathway, crucial for cell growth and metabolism regulation. It functions as a building block for the synthesis of PROTACs aimed at modulating PI3K/mTOR signaling. This compound is valuable in cancer research and drug discovery efforts focusing on targeted protein degradation and pathway inhibition.

    25 mg
    $60.00
    50 mg
    $90.00
    All 3 sizes
  • HL-2
    Cat. No.
    A81364

    HL-2

    HL-2 is a selective ligand for the phosphoinositide 3-kinase (PI3K) kinase, utilized in the synthesis of proteolysis-targeting chimeras (PROTACs). Its role in modulating PI3K activity makes it a valuable tool for studying signal transduction pathways and cancer biology. HL-2's application extends to drug development and the investigation of therapeutic strategies targeting PI3K-related diseases.

    Out of stock

    All 3 sizes
  • Copanlisib-NH
    Cat. No.
    B21863

    Copanlisib-NH

    Copanlisib-NH is a selective ligand for the PI3Kα/δ isoforms, making it a valuable tool in targeted protein degradation studies. This compound serves as a ligand in the development of PROTACs aimed at degrading PI3Kα/δ proteins, facilitating research on mechanisms of resistance and cellular pathways in oncology. Notably, Copanlisib-NH is applicable in breast cancer research, offering insights into therapeutic strategies that exploit the PI3K signaling pathway.

    Out of stock

    All 3 sizes

3 Items

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