Name: PIK-III
Price: 289.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    IC50: 18 nM for VPS34
    PIK-III is a VPS34 inhibitor and is able to inhibit autophagy.
    VPS34 kinase has been found to be responsible for synthesis and deposition of phosphatidylinositol-3-phosphate at autophagosome formation sites, resulting in the recruitment of PtdIns(3)P-binding proteins.
    In vitro: In previous study, PIK-III was identified as a selective inhibitor of VPS34 binding in a hydrophobic pocket. In addition, PIK-III could acutely inhibit the autophagy and lipidation of LC3, which led to the stabilization of autophagy substrates. Moreover, substrates such as NCOA4 were identified by conducting ubiquitin-affinity proteomic assay on PIK-III-treated cells, which accumulated in cells with ATG7 deficience and co-localized with autolysosomes. NCOA4 could bind ferritin heavy chain-1 directly to target the iron-binding ferritin complex following starvation or iron depletion [1].
    In vivo: Animal study showed that PIK-III-treated Ncoa4-/- mice had a profound accumulation of iron in splenic macrophages that were important for iron reutilization from engulfed red blood cells. In summary, such in vivo results provided a novel mechanism for selective autophagy of ferritin and revealed a previously untouched role for autophagy and NCOA4 in the control of in-vivo iron homeostasis [1].
    Clinical trial: Up to now, PIK-III is still in the preclinical development stage.
- Properties
  - Alternative Name
    
    4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)-[4,5'-bipyrimidine]-2,2'-diamine
    
    CAS Number
    
    1383716-40-2
    
    Molecular Formula
    
    C17H17N7
    
    Molecular Weight
    
    319.36
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥31.9 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Manuela Antonioli , Benedetta Pagni, et al. "HPV sensitizes OPSCC cells to cisplatin-induced apoptosis by inhibiting autophagy through E7-mediated degradation of AMBRA1." Autophagy. 2020 Nov 23;1-13. PMID:33172332
    2. Ge L, Zhang M, et al. "Remodeling of ER-exit sites initiates a membrane supply pathway for autophagosome biogenesis." EMBO Rep. 2017 Sep;18(9):1586-1603. PMID:28754694

PIK-III

PIK-III

Background

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