Vps34-PIK-III - PI3K 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEVps34-PIK-IIICat. No.: HY-12794CAS No.: 1383716-40-2分式: CHN分量: 319.36作靶点: PI3K; Autophagy作通路: PI3K/Akt/mTOR; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 31 mg/mL (97.07 mM)* me

2、ans soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.1313 mL 15.6563 mL 31.3126 mL5 mM 0.6263 mL 3.1313 mL 6.2625 mL10 mM 0.3131 mL 1.5656 mL 3.1313 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Vps34-PIK-III是有效选择性的 VPS34 抑制剂，IC50 值为18 nM。IC

3、50 & Target Vps34 PI(3)K PI(3)K PI(3)K18 nM (IC50) 1.2 M (IC50) 3.04 M (IC50) 3.96 M (IC50)Autophagy1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE体外研究 PIK-III is a selective inhibitor of VPS34 that binds a unique hydrophobic pocket not present in related kinasessuch as PI3K. PIK-III is at least 1

4、00-fold-selective for VPS34 over related lipid kinases such as PI3K and theprotein kinase mTOR. PIK-III acutely inhibits autophagy and de novo lipidation of LC3, and leads to thestabilization of autophagy substrates. In H4 cells expressing the mCherry-GFP-LC3 reporter PIK-III inhibitsthe formation o

5、f mCherry-positive autolysosomes and increases the cytosolic signal of LC3 under basalconditions and when autophagy is induced with the mTOR inhibitor AZD8055. PIK-III prevents the turnover ofGFP-tagged p62 under basal conditions and when autophagy is activated. PIK-III treatment leadsto anincrease

6、in the levels of LC3-I in H4 and PSN1 cells 2.体内研究 The DFX-induced NCOA4-dependent turnover of FTH1 and FTL is blocked with PIK-III suggesting anautophagy-dependent process 2.REFERENCES1. Honda A, et al. Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulat

7、e Autophagy in Vivo.ACS Med Chem Lett. 2015 Nov 13;7(1):72-6.2. Dowdle WE, et al. Selective VPS34 inhibitor blocks autophagy and uncovers a role for NCOA4 in ferritin degradation and ironhomeostasis in vivo. Nat Cell Biol. 2014 Nov;16(11):1069-79.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use