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                        p110α
                    
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                        p110β
                    
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                        p110δ
                    
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                        p110γ
                    
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                        C2β
                    
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                        Vps34
                    
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      Vps34 選擇性抑制劑
      
        
      
            
            
      
                目錄號(hào)
                產(chǎn)品名
                產(chǎn)品描述
                Selective / Pan
                IC50 / Ki
            
      
                  
            
            
                
      
                    S7682
                    SAR405
                    SAR405 is a low-molecular-mass kinase inhibitor of PIK3C3/Vps34 (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR. SAR405 prevents autophagy and synergizes with MTOR (mechanistic target of rapamycin) inhibition in tumor cells.
                    Selective
                    Vps34, IC50: 1.2 nM
                
      
            
                
      
                    S8456
                    VPS34 inhibitor 1 (Compound 19)
                    VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM.
                    Selective
                    VPS34, IC50: 15 nM
                
      
            
                
      
                    S7683
                    PIK-III
                    PIK-III (VPS34-IN2), which is a selective inhibitor of ?VPS34 enzymatic activity, inhibits autophagy and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates. The IC50 values for VPS34 and PI(3)Kδ are 0.018 μM and 1.2 μM respectively. 
                    Selective
                    Vps34, IC50: 0.018μM
                
      
            
                
      
                    S8596
                    Autophinib
                    Autophinib is a potent autophagy inhibitor with a novel chemotype with IC50 values of 90 and 40 nM for autophagy in starvation induced autophagy assay and rapamycin induced autophagy assay. The IC50 value for Vps34 is 19 nM in vitro.

                    Selective
                    Vps34, IC50: 19 nM
                
      
            
                
      
                    S7980
                    VPS34-IN1
                    Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks. Vps34-IN1 modulates autophagy.
                    Selective
                    Vps34, IC50: 25 nM
                
      
            
                
      
                    S7103
                    Taselisib (GDC 0032)
                    Taselisib (GDC 0032, RG7604) is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with Ki of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.
                    Pan
                    hVps34, IC50: 374 nM
                
      
            
                
      
                    S2247
                    Buparlisib (BKM120)
                    Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Buparlisib induces apoptosis. Phase 2.
                    Pan
                    Vps34, IC50: 2.4 μM
                
      
            
                
      
                    S2767
                    3-MA (3-Methyladenine)
                    3-MA (3-Methyladenine) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells;  blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation. Solutions are unstable and should be fresh-prepared.
                    Pan
                    Vps34, IC50: 25 μM
                
      
            
                  
        
      
        
    
      

      
    







      


      
    
    
    
    
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