Description

PIK-III is a selective inhibitor of VPS34 that binds a unique hydrophobic pocket not present in related kinases such as PI(3)Kα. PIK-III acutely inhibits autophagy and de novo lipidation of LC3, and leads to the stabilization of autophagy substrates.  VPS34 IC50 = 0.018μM.

SMILE:  NC1=NC(CC2CC2)=C(C3=CC=NC(NC4=CC=NC=C4)=N3)C=N1

Systematic Name: 4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)-[4,5'-bipyrimidine]-2,2'-diamine

Molecular Weight: 319.37

Formula: C17H17N7

PMID: 25327288

References

Selective VPS34 inhibitor blocks autophagy and uncovers a role for NCOA4 in ferritin degradation and iron homeostasis in vivo. Dowdle W.E, Nyfeler B., et al. Nature Cell Biology. 16(11):1069-1079 (2014).

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