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 (96):

Cat. No. Product Name Effect Purity
  • HY-10108
    LY294002 Inhibitor 99.97%
    LY294002 is a broad-spectrum inhibitor of PI3K, with IC50 of 0.5/0.57/0.97 μM for PI3Kα/δ/β, respectively, also potently inhibits CK2 with IC50 of 98 nM.
  • HY-19312
    3-Methyladenine Inhibitor 99.84%
    3-Methyladenine is a selective PI3K inhibitor with IC50 of 25 μM and 60 μM for Vps34 and PI3Kγ, respectively, and it can inhibit all PtdIns3Ks at 10 mM.
  • HY-10197
    Wortmannin Inhibitor 99.65%
    Wortmannin is a multi-target inhibitor of PI3K and MLCK with IC50s of 3 nM and 200 nM, respectively.
  • HY-15244
    BYL-719 Inhibitor 99.04%
    BYL-719 is a potent and selective PI3Kα inhibitor with IC50 of 5 nM.
  • HY-50673
    BEZ235 Inhibitor 98.83%
    BEZ235 is a dual pan-class I PI3K and mTOR kinase inhibitor with IC50 of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively.
  • HY-P0175
    740 Y-P Activator
    740 Y-P (PDGFR 740Y-P) is a potent and cell permeable PI3K activator.
  • HY-101272
    GDC-0326 Inhibitor 99.31%
    GDC-0326 is a potent and selective PI3Kα inhibitor with a Ki of 0.2 nM.
  • HY-70063
    NVP-BKM120 Inhibitor 99.68%
    NVP-BKM120 is a pan-class I PI3K inhibitor, with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ, respectively.
  • HY-100716
    IPI549 Inhibitor 99.14%
    IPI549 is a potent and selective PI3Kγ Inhibitor with IC50 of 16 nM.
  • HY-13026
    CAL-101 Inhibitor 98.38%
    CAL-101 is a highly selective and potent p110δ inhibitor with IC50 of 2.5 nM, is 40- to 300-fold more selective for p110δ relative to other PI3K class I enzymes (p110α, p110β, and p110γ; IC50 are 820, 565, and 89nM, respectively).
  • HY-12481
    SAR405 Inhibitor 98.48%
    SAR405 is a PIK3C3/Vps34 inhibitor with an IC50 of 1.2 nM.
  • HY-50094
    GDC-0941 Inhibitor 99.52%
    GDC-0941 is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
  • HY-12279
    TGR-1202 Inhibitor 98.55%
    TGR-1202 is a novel PI3Kδ inhibitor, with IC50 and EC50 of 22.2 nM and 24.3 nM, respectively; Also active against CK1ε, with an EC50 value of 6.0 μM.
  • HY-18085
    Quercetin Inhibitor 98.21%
    Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4±0.6 μM, 3.0±0.0 μM and 5.4±0.3 μM for PI3K γ, PI3K δ and PI3K β, respectively.
  • HY-12513
    LY3023414 Inhibitor 99.70%
    LY3023414 potently and selectively inhibits class I PI3K isoforms, mTORC1/2, and DNA-PK with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 165 nM and 4.24 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, mTOR and DNA-PK, respectively.
  • HY-12795
    Vps34-IN-1 Inhibitor 99.64%
    Vps34-IN-1 is an inhibitor of Vps34 extracted from patent WO/2012085815 A1, compound example 16a; has an IC50 of 4 nM.
  • HY-15346
    BAY 80-6946 Inhibitor 98.09%
    BAY 80-6946 is an ATP-competitive selective class-I PI3 kinases inhibitor, with IC50s of 0.5, 0.7, 3.7 and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, and much less active against mTOR (IC50=45 nM) and other PIKs (no inhibition at 1 μM).
  • HY-13898
    GDC-0032 Inhibitor 99.75%
    GDC-0032 is a potent β-sparing small molecule inhibitor of PI3K, with Ki values of 0.29 nM, 0.91 nM, 0.97 nM for PI3Kα, PI3Kβ and PI3Kγ, respectively.
  • HY-15177
    PF-04691502 Inhibitor 99.49%
    PF-04691502 is a potent and selective inhibitor of PI3K and mTOR kinases with antitumor activity.
  • HY-10297
    GSK2126458 Inhibitor 99.31%
    GSK2126458 is a highly selective and potent inhibitor of PI3K with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2, respectively.