2. Signaling Pathways
  3. PI3K/Akt/mTOR
  4. PI3K
  5. PI3KC2α Isoform

PI3KC2α

PI3KC2α (phosphoinositide 3-kinase class II alpha) is a class II phosphoinositide 3-kinase that generates phosphatidylinositol 3-phosphate (PI(3)P) and phosphatidylinositol 3,4-bisphosphate (PI(3,4)P₂), thereby regulating intracellular membrane trafficking and phosphoinositide-dependent signaling processes[1][2]. PI3KC2α functions prominently at clathrin-coated membrane compartments, where it supports clathrin-mediated endocytosis, endosomal membrane dynamics, and vesicular trafficking through localized phosphoinositide production[2][3][4]. Mechanistically, PI3KC2α-derived phosphoinositides contribute to endocytic membrane remodeling, endosomal organization, and Rab11-dependent pathways required for primary cilium function[2][3]. Through these activities, PI3KC2α participates in cellular processes linked to angiogenesis, cell division, endothelial signaling, and platelet membrane morphology[2]. In disease-relevant models, loss of PI3KC2α activity disrupts endocytic trafficking and ciliary function, while pathogenic PIK3C2A mutations have been associated with syndromic developmental abnormalities characterized by skeletal, ocular, and growth defects linked to ciliary dysfunction[3][5]. Compared with related class II isoforms, PI3KC2α has a prominent role in clathrin-dependent endocytosis and membrane remodeling, whereas other class II PI3Ks display distinct cellular functions and tissue distributions[4]. For experimental applications, the PITCOIN series represents potent and highly selective PI3KC2α inhibitors that acutely suppress PI3KC2α-dependent phosphoinositide synthesis and provide pharmacological tools for investigating endocytic dynamics, platelet biology, and PI3KC2α-regulated signaling pathways[2].

PI3KC2α Related Products (8):

Cat. No. Product Name Effect Purity
  • HY-10115
    PI-103
    		Inhibitor 99.82%
    PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy.
  • HY-12030
    PIK-90
    		Inhibitor 99.70%
    PIK-90 is a DNA-PK and PI3K inhibitor, which inhibits p110α, p110γ and DNA-PK with IC50s of 11, 18 and 13 nM, respectively.
  • HY-12046
    PIK-93
    		Inhibitor 99.81%
    PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM, and also inhibits PI3Kγ and PI3Kα with IC50 of 16 nM and 39 nM, respectively.
  • HY-13281
    PIK-75 hydrochloride
    		Inhibitor 99.66%
    PIK-75 hydrochloride 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 hydrochloride inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 hydrochloride induces apoptosis.
  • HY-107834
    PIK-75
    		Inhibitor 99.94%
    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.
  • HY-118903
    PIK-124
    		Inhibitor
    PIK-124 is a thiazolidinone-based PI3Kγ-biased PI3K inhibitor, with an IC50 of 3 nM against PI3Kγ. PIK-124 exhibits cross-reactivity with PI3Kα (IC50 = 23 nM), PI3Kδ (IC50 = 340 nM), PI3KC2α (IC50 = 140 nM) and PI3KC2β (IC50 = 370 nM). PIK-124 is applicable to breast cancer-related research.
  • HY-156371
    MIPS-21335
    		Inhibitor 99.61%
    MIPS-21335 is a PI3KC2α inhibitor with an IC50 of 7 nM. MIPS-21335 also inhibits PI3KC2β, p110α, p110β and p110δ, with IC50 values of 43, 140, 386 and 742 nM, respectively. MIPS-21335 has antithrombotic effect. MIPS-21335 can be used for the researches of cardiovascular disease and metabolic disease, such as thrombosis and hyperlipidemia.
  • HY-112443
    AZD3458
    		Inhibitor 99.71%
    AZD3458 is a potent and remarkably selective PI3Kγ inhibitor with pIC50s of 9.1, 5.1, <4.5, and 6.5 for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively.