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PIK-III

Catalog No.
B6160
VPS34 inhibitor and inhibits autophagy
Grouped product items
SizePriceStock Qty
5mg
$138.00
In stock
25mg
$488.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

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.

Reference:
[1] Dowdle WE et al.  Selective VPS34 inhibitor blocks autophagy and uncovers a role for NCOA4 in ferritin degradation and iron homeostasis in vivo. Nat Cell Biol. 2014 Nov;16(11):1069-79.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt319.36
Cas No.1383716-40-2
FormulaC17H17N7
Solubility≥31.9mg/mL in DMSO
Chemical Name4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)-[4,5'-bipyrimidine]-2,2'-diamine
SDFDownload SDF
Canonical SMILESNC1=NC=C(C2=NC(NC3=CC=NC=C3)=NC=C2)C(CC4CC4)=N1
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Chemical structure

PIK-III

Related Biological Data

PIK-III