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.
Catalogue number RGNCY-0041
SAR405 is a low molecular mass kinase inhibitor of Vps34 (KD 1.5 nM) and has a highly selective protein and lipid kinase profile. Inhibition of Vps34 kinase activity by SAR405 affects both late endosome-lysosome compartments and prevents autophagy. In addition, the concomitant inhibition of VPS34 and mTOR, with SAR405 and the US Food and Drug Administration–approved mTOR inhibitor everolimus, results in synergistic antiproliferative activity in renal tumor cell lines, indicating a potential clinical application in cancer. VSP34 IC50 = 1.2nM
Catalogue number RGNCY-0042
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