 
        
        
        
                货号:A837347
                
                同义名:
                    
                        
                            
                                PIK-III; Vacuolar Protein Sorting 34 Inhibitor 2
                            
                        
                    
                
                
                
                    
                     
                    
                     
                
            
Vps34-PIK-III是一种选择性的 VPS34 酶活性抑制剂,抑制自噬作用和 LC3 的新生脂化,导致自噬底物的稳定化。
 
                                 
                                
                            

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| 产品名称 | C2β ↓ ↑ | p110α ↓ ↑ | p110β ↓ ↑ | p110γ ↓ ↑ | p110δ ↓ ↑ | PI3K ↓ ↑ | Vps34 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| A66 | + C2β, IC50: 462 nM | ++ p110α, IC50: 32 nM | 99%+ | ||||||||||||||||
| Taselisib | + C2β, IC50: 292 nM | ++++ PI3Kα, Ki: 0.29 nM | +++ PI3Kβ, Ki: 9.1 nM | ++++ PI3Kγ, Ki: 0.97 nM | ++++ PI3Kδ, Ki: 0.12 nM | + hVps34, IC50: 374 nM | 99%+ | ||||||||||||
| Gedatolisib | ++++ PI3Kα, IC50: 0.4 nM | +++ PI3Kγ, IC50: 5.4 nM | mTOR | 99% | |||||||||||||||
| HS-173 | ++++ PI3Kα , IC50: 0.8 nM | 99%+ | |||||||||||||||||
| Serabelisib | +++ PI3Kα, IC50: 21 nM | 99%+ | |||||||||||||||||
| GNE-477 | ++++ PI3Kα, IC50: 4 nM | mTOR | 99% | ||||||||||||||||
| YM-201636 | + p110α, IC50: 3.3 μM | PIKfyve | 98% | ||||||||||||||||
| AS-252424 | + PI3Kα, IC50: 935 nM | ++ PI3Kγ, IC50: 33 nM | 99% | ||||||||||||||||
| Alpelisib | +++ PI3Kα, IC50: 5 nM | 99%+ | |||||||||||||||||
| AS-604850 | + PI3Kα, IC50: 4.5 μM | + PI3Kγ, IC50: 0.25 μM | 99% | ||||||||||||||||
| SF2523 | ++ PI3Kα, IC50: 34 nM | ++ PI3Kγ, IC50: 158 nM | mTOR,DNA-PK | 99%+ | |||||||||||||||
| Inavolisib | ++++ PI3K alpha, IC50: 0.038 nM | 99%+ | |||||||||||||||||
| Bimiralisib | ++++ PI3Kα, Kd: 1.5 nM | +++ PI3Kβ, Kd: 11 nM | ++ PI3Kγ, Kd: 25 nM | ++ PI3Kδ, Kd: 25 nM | mTOR | 99%+ | |||||||||||||
| GSK1059615 | ++++ PI3Kα, IC50: 0.4 nM | ++++ PI3Kβ, IC50: 0.6 nM | +++ PI3Kγ, IC50: 5 nM | ++++ PI3Kδ, IC50: 2 nM | mTOR | 98% | |||||||||||||
| GSK2636771 | ✔ | 99% | |||||||||||||||||
| Fimepinostat | +++ PI3Kα, IC50: 19 nM | ++ PI3Kβ, IC50: 54 nM | ++ PI3Kδ, IC50: 39 nM | 99%+ | |||||||||||||||
| VS-5584 | ++++ PI3Kα, IC50: 2.6 nM | +++ PI3Kβ, IC50: 21 nM | ++++ PI3Kγ, IC50: 3.0 nM | ++++ PI3Kδ, IC50: 2.7 nM | mTOR | 98% | |||||||||||||
| Dactolisib | ++++ p110α1, IC50: 4 nM | ++ p110β, IC50: 75 nM | +++ p110γ, IC50: 5 nM | +++ p110δ, IC50: 7 nM | 98+% | ||||||||||||||
| PI-103 | ++++ p110α, IC50: 2 nM | ++++ p110β, IC50: 3 nM | +++ p110γ, IC50: 15 nM | ++++ p110δ, IC50: 3 nM | mTOR,DNA-PK | 99%+ | |||||||||||||
| PI-3065 | + p110β, IC50: 1078 nM | +++ p110δ, IC50: 15 nM | 99%+ | ||||||||||||||||
| Voxtalisib | ++ PI3Kα, IC50: 39 nM | ++ PI3Kβ, IC50: 113 nM | +++ PI3Kγ, IC50: 9 nM | ++ PI3Kδ, IC50: 43 nM | mTOR,DNA-PK | 99%+ | |||||||||||||
| AZD-8835 | +++ PI3Kα, IC50: 6.2 nM | + PI3Kβ, IC50: 431 nM | ++ PI3Kγ, IC50: 90 nM | +++ PI3Kδ, IC50: 5.7 nM | 99% | ||||||||||||||
| Pilaralisib analogue | ++ PI3Kα, IC50: 39 nM | ++ PI3Kβ, IC50: 36 nM | +++ PI3Kγ, IC50: 23 nM | ++ PI3Kδ, IC50: 36 nM | 99%+ | ||||||||||||||
| ZSTK474 | +++ PI3Kα, IC50: 16 nM | ++ PI3Kβ, IC50: 44 nM | ++ PI3Kγ, IC50: 49 nM | +++ PI3Kδ, IC50: 4.6 nM | ++ PI3K, IC50: 37 nM | 98% | |||||||||||||
| AS-605240 | ++ PI3Kα, IC50: 60 nM | + PI3Kβ, IC50: 270 nM | +++ PI3Kγ, IC50: 8 nM | + PI3Kδ, IC50: 300 nM | 98% | ||||||||||||||
| TGX-221 | +++ p110β, IC50: 5 nM | ++ p110δ, IC50: 0.1 μM | 99%+ | ||||||||||||||||
| PF-04691502 | ++++ PI3Kα, Ki: 1.8 nM | ++++ PI3Kβ, Ki: 2.1 nM | ++++ PI3Kγ, Ki: 1.9 nM | ++++ PI3Kδ, Ki: 1.6 nM | mTOR | 98+% | |||||||||||||
| GDC-0084 | ++++ PI3Kα, Ki app: 2 nM | ++ PI3Kβ, Ki app: 46 nM | +++ PI3Kγ, Ki app: 10 nM | ++++ PI3Kδ, Ki app: 3 nM | mTOR | 99%+ | |||||||||||||
| Buparlisib | ++ p110α, IC50: 52 nM | + p110β, IC50: 166 nM | + p110γ, IC50: 262 nM | ++ p110δ, IC50: 116 nM | + Vps34, IC50: 2.4 μM | mTOR | 98% | ||||||||||||
| LY294002 | + p110α, IC50: 0.5 μM | + p110β, IC50: 0.97 μM | + p110δ, IC50: 0.57 μM | DNA-PK | 99%+ | ||||||||||||||
| AZD 6482 | + PI3Kα, IC50: 870 nM | +++ PI3Kβ, IC50: 10 nM | ++ PI3Kδ, IC50: 80 nM | DNA-PK | 99%+ | ||||||||||||||
| Pictilisib | ++++ p110α, IC50: 3 nM | ++ p110β, IC50: 33 nM | ++ p110γ, IC50: 75 nM | ++++ p110δ, IC50: 3 nM | mTOR | 99%+ | |||||||||||||
| PKI-402 | ++++ PI3Kα, IC50: 2 nM | +++ PI3Kβ, IC50: 7 nM | +++ PI3Kγ, IC50: 16 nM | +++ PI3Kδ, IC50: 14 nM | mTOR | 98% | |||||||||||||
| Copanlisib | ++++ PI3Kα, IC50: 0.5 nM | ++++ PI3Kβ, IC50: 3.7 nM | +++ PI3Kγ, IC50: 6.4 nM | ++++ PI3Kδ, IC50: 0.7 nM | 99%+ | ||||||||||||||
| Omipalisib | ++++ p110α, Ki: 0.019 nM | ++++ p110β, Ki: 0.13 nM | ++++ p110γ, Ki: 0.06 nM | ++++ p110δ, Ki: 0.024 nM | 99%+ | ||||||||||||||
| Izorlisib | +++ PI3Kα, IC50: 14 nM | ++ PI3Kβ, IC50: 0.12 μM | ++ PI3Kγ, IC50: 36 nM | + PI3Kδ, IC50: 0.50 μM | 99%+ | ||||||||||||||
| AZD8186 | ++ PI3Kα, IC50: 35 nM | ++++ PI3Kβ, IC50: 4 nM | +++ PI3Kδ, IC50: 12 nM | 99% | |||||||||||||||
| KU-0060648 | ++++ PI3Kα, IC50: 4 nM | ++++ PI3Kβ, IC50: 0.5 nM | + PI3Kγ, IC50: 0.59 μM | ++++ PI3Kδ, IC50: 0.1 nM | DNA-PK | 98% | |||||||||||||
| Apitolisib | +++ p110α, IC50: 5 nM | ++ p110β, IC50: 27 nM | +++ p110γ, IC50: 14 nM | +++ p110δ, IC50: 7 nM | mTOR | 98%+ | |||||||||||||
| CZC24832 | + PI3Kβ, IC50: 1.1 μM | ++ PI3Kγ, IC50: 27 nM | 98+% | ||||||||||||||||
| BGT226 maleate | ++++ PI3Kα, IC50: 4 nM | ++ PI3Kβ, IC50: 63 nM | ++ PI3Kγ, IC50: 38 nM | mTOR | 99%+ | ||||||||||||||
| TG 100713 | ++ PI3Kα, IC50: 165 nM | + PI3Kβ, IC50: 215 nM | ++ PI3Kγ, IC50: 50 nM | +++ PI3Kδ, IC50: 24 nM | 98%+ | ||||||||||||||
| PI3K-IN-1 | ++ PI3Kα, IC50: 39 nM | ++ PI3Kβ, IC50: 113 nM | +++ PI3Kγ, IC50: 9 nM | ++ PI3Kδ, IC50: 43 nM | mTOR,DNA-PK | 98+% | |||||||||||||
| TG100-115 | + PI3Kα, IC50: 1.3 μM | + PI3Kβ, IC50: 1.2 μM | ++ PI3Kγ, IC50: 83 nM | + PI3Kδ, IC50: 235 nM | 98% | ||||||||||||||
| PIK-90 | +++ PI3Kα, IC50: 11 nM | + PI3Kβ, IC50: 350 nM | +++ PI3Kγ, IC50: 18 nM | ++ PI3Kδ, IC50: 58 nM | 99%+ | ||||||||||||||
| PIK-294 | + p110β, IC50: 490 nM | ++ p110γ, IC50: 160 nM | +++ p110δ, IC50: 10 nM | 99%+ | |||||||||||||||
| Duvelisib | ++++ PI3Kβ, Ki: 1564 pM | ++ PI3Kγ, Ki: 243 pM | ++++ PI3Kδ, Ki: 23 pM | 99%+ | |||||||||||||||
| GDC-0326 | ++++ PI3Kα, Ki: 0.2 nM | ++ PI3Kβ, Ki: 26.6 nM | +++ PI3Kγ, Ki: 10.2 nM | ++++ PI3Kδ, Ki: 4 nM | 98% | ||||||||||||||
| Quercetin Dihydrate | + PI3Kβ, IC50: 5.4 μM | + PI3Kγ, IC50: 2.4 μM | + PI3Kδ, IC50: 3.0 μM | 95% | |||||||||||||||
| Quercetin | + PI3Kβ, IC50: 5.4 μM | + PI3Kγ, IC50: 2.4 μM | + PI3Kδ, IC50: 3.0 μM | Src,Sirtuin,PKC | 95% | ||||||||||||||
| Leniolisib | + PI3Kα, IC50: 0.244 μM | + PI3Kβ, IC50: 0.424 μM | + PI3Kγ, IC50: 2.23 μM | +++ PI3Kδ, IC50: 0.011 μM | DNA-PK | 99%+ | |||||||||||||
| PIK-108 | ✔ | 99% | |||||||||||||||||
| Eganelisib | +++ PI3Kγ, IC50: 16 nM | 99%+ | |||||||||||||||||
| CAY10505 | ✔ | 99% | |||||||||||||||||
| IPI-3063 | ++++ p110δ, IC50: 2.5 nM | 99% | |||||||||||||||||
| Nemiralisib | ++++ PI3Kδ, pKi: 9.9 | 99%+ | |||||||||||||||||
| PF-4989216 | ++++ p110α, IC50: 2 nM | ++ p110γ, IC50: 65 nM | ++++ p110δ, IC50: 1 nM | 99%+ | |||||||||||||||
| PIK-75 HCl | +++ p110α, IC50: 5.8 nM | ++ p110γ, IC50: 76 nM | + p110δ, IC50: 0.51 μM | DNA-PK | 99%+ | ||||||||||||||
| Tenalisib | ++ PI3Kγ, IC50: 33.2 nM | ++ PI3Kδ, IC50: 24.5 nM | 98% | ||||||||||||||||
| Acalisib | +++ p110δ, IC50: 14 nM | 99%+ | |||||||||||||||||
| Umbralisib | +++ PI3Kδ, IC50: 22.2 nM | 99%+ | |||||||||||||||||
| AMG319 | + PI3Kγ, IC50: 850 nM | +++ PI3Kδ, IC50: 18 nM | 99% | ||||||||||||||||
| IC-87114 | + PI3Kγ, IC50: 29 μM | + PI3Kδ, IC50: 0.5 μM | 99%+ | ||||||||||||||||
| Idelalisib | ++ p110γ, IC50: 89 nM | ++++ p110δ, IC50: 2.5 nM | 98% | ||||||||||||||||
| PIK-293 | + p110γ, IC50: 10 μM | + p110δ, IC50: 0.24 μM | 99%+ | ||||||||||||||||
| Vps34-PIK-III | + PI3Kδ, IC50: 1.2μM | +++ Vps34, IC50: 0.018μM | 99%+ | ||||||||||||||||
| GSK2292767 | ✔ | 98% | |||||||||||||||||
| Seletalisib | + PI3Kγ, IC50: 282 nM | +++ PI3Kδ, IC50: 12 nM | 99%+ | ||||||||||||||||
| P110δ-IN-1 | ++++ P110δ, IC50: 0.6 nM | 99% | |||||||||||||||||
| PI3Kδ-IN-5 | ++++ PI3Kδ, IC50: 0.9 nM | 99% | |||||||||||||||||
| SRX3207 | + PI3K alpha, IC50: 244 nM | + PI3K gamma, IC50: 9790 nM | + PI3K delta, IC50: 388 nM | Syk | 98% | ||||||||||||||
| Parsaclisib HCl | ++++ PI3Kδ, IC50: 1 nM | 98% | |||||||||||||||||
| IHMT-PI3Kδ-372 | +++ PI3Kδ, IC50: 14 nM | 98% | |||||||||||||||||
| Trigonelline | ✔ | Akt | 99%+ | ||||||||||||||||
| Wortmannin | ++++ PI3K, IC50: 3 nM | MLCK,DNA-PK | 99%+ | ||||||||||||||||
| Samotolisib | ✔ | DNA-PK | 99%+ | ||||||||||||||||
| GNE-317 | ✔ | 99%+ | |||||||||||||||||
| Oroxin B | ✔ | Akt,PTEN | 99%+ | ||||||||||||||||
| NU 7026 | + PI3K, IC50: 13 μM | DNA-PK | 98+% | ||||||||||||||||
| Deguelin | ✔ | Akt | 99%+ | ||||||||||||||||
| Ailanthone | ✔ | Akt,ATM/ATR,CDK | 98% | ||||||||||||||||
| Resibufogenin | ✔ | ROS | 98% | ||||||||||||||||
| KU-57788 | + PI3K, IC50: 5 μM | mTOR,DNA-PK | 99%+ | ||||||||||||||||
| Cinobufagine | ✔ | Akt | 99% | ||||||||||||||||
| α-Linolenic acid | ✔ | 97% (GC) | |||||||||||||||||
| MTX-211 | ✔ | EGFR | 98% | ||||||||||||||||
| PI3K/mTOR Inhibitor-2 | ++++ PI3K, IC50: 3.4 nM | mTOR | 99%+ | ||||||||||||||||
| SPP-86 | ✔ | 99%+ | |||||||||||||||||
| (E)-Akt inhibitor-IV | ✔ | 98% | |||||||||||||||||
| Vps34-IN-1 | ++ Vps34, IC50: 25 nM | 98% | |||||||||||||||||
| SAR405 | ++++ Vps34, IC50: 1.2 nM | 98+% | |||||||||||||||||
| 3-Methyladenine | + PI3Kγ, IC50: 60 μM | + Vps34, IC50: 25 μM | Autophagy | 98% | |||||||||||||||
| Vps34-IN-4 | +++ VPS34, IC50: 15 nM | 98%+ | |||||||||||||||||
| Autophinib | +++ Vps34, IC50: 19 nM | Autophagy | 99% | ||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 产品名称 | Autophagy ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| SBI-0206965 | +++ ULK2, IC50: 711 nM ULK1, IC50: 108 nM | 95% | |||||||||||||||||
| Hydroxychloroquine sulfate | ✔ | 99% | |||||||||||||||||
| Valproic acid sodium | ✔ | HDAC | 97% | ||||||||||||||||
| PFK-015 | ++ PFKFB3, IC50: 207 nM | 99%+ | |||||||||||||||||
| MRT68921 HCl | ++++ ULK2, IC50: 1.1 nM ULK1, IC50: 2.9 nM | 99%+ | |||||||||||||||||
| ROC-325 | ✔ | 99%+ | |||||||||||||||||
| Autophinib | +++ Autophagy, IC50: 40 nM | 99% | |||||||||||||||||
| Lys05 | ✔ | 99%+ | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 | 
 | 
| 描述 | Cells rely on autophagy to clear misfolded proteins and damaged organelles to maintain cellular homeostasis. PIK-III is an autophagy inhibitor which can acutely inhibit autophagy and de novo lipidation of LC3, and lead to the stabilization of autophagy substrates. PIK-III could modulate PtdIns(3)P-mediated effectors in mammalian cells. The IC50s of PIK-III are 0.018 μM, 1.2 μM, 3.04 μM, 3.96 μM and 4.43 μM for Vps34, PI3Kδ, PI3Kγ, PI3Kα and PI4Kβ, respectively. In a vitro study, CD34 + cells were treated ex vivo for 48h with PIK-III (5 µM). The reduction in engrafted cells following single PIK-III treatment, including primitive CD34+CD38- and CD34+CD133+ populations, confirmed the essential role of autophagy in the maintenance of the LSC pool[2]. | 
| Concentration | Treated Time | Description | References | |
| Huh7 cells | 5 µM | 24 hours | Vps34-PIK-III significantly decreased the expression of stemness genes and induced AMPK activation. | Cell Death Dis. 2020 Jun 8;11(6):427. | 
| MHCC97H cells | 5 µM | 24 hours | Vps34-PIK-III significantly decreased the expression of stemness genes and induced AMPK activation. | Cell Death Dis. 2020 Jun 8;11(6):427. | 
| Administration | Dosage | Frequency | Description | References | ||
| Nude mice | RKO colon cancer tumor model | Oral | 50 mg/kg | Twice a day for 7 days | To evaluate the ability of compound 19 to inhibit autophagy in vivo, results showed accumulation of LC3-II indicating reduced autophagic capacity. | ACS Med Chem Lett. 2015 Nov 13;7(1):72-6 | 
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 3.13mL 0.63mL 0.31mL | 15.66mL 3.13mL 1.57mL | 31.31mL 6.26mL 3.13mL | |
| CAS号 | 1383716-40-2 | 
| 分子式 | C17H17N7 | 
| 分子量 | 319.36 | 
| SMILES Code | NC1=NC=C(C2=NC(NC3=CC=NC=C3)=NC=C2)C(CC4CC4)=N1 | 
| MDL No. | MFCD28963904 | 
| 别名 | PIK-III; Vacuolar Protein Sorting 34 Inhibitor 2; Vps34 Inhibitor 2; VPS34-IN2 | 
| 运输 | 蓝冰 | 
| InChI Key | XXSDLQLNIVFIJI-UHFFFAOYSA-N | 
| Pubchem ID | 67983123 | 
| 存储条件 | In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry,2-8°C | 
| 溶解方案 | DMSO: 30 mg/mL(93.94 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 
 
 
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			沪公网安备 31011702889066号
			
			沪ICP备2024050318号-1