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                同义名:
                    
                        
                            
                                TCS JNK 6o; c-Jun N-terminal Kinase Inhibitor VIII
                            
                        
                    
                
                
                
                    
                     
                    
                     
                
            
JNK Inhibitor VIII是一种c-Jun氨基末端激酶(JNK-1、-2、-3)抑制剂,Ki值分别为2 nM、4 nM和52 nM,IC50值分别为45 nM和160 nM(针对JNK-1和JNK-2)。
 
                                 
                                
                            

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| 产品名称 | JNK ↓ ↑ | JNK1 ↓ ↑ | JNK2 ↓ ↑ | JNK3 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Mulberroside A | ✔ | 99%+ | |||||||||||||||||
| Loureirin B | ✔ | Calcium Channel,Potassium Channel | 99%+ | ||||||||||||||||
| Ginsenoside Re | ✔ | NF-κB | 98% | ||||||||||||||||
| (+)-(3R,8S)-Falcarindiol | ✔ | STAT,ERK | 99%+ | ||||||||||||||||
| trans-Zeatin | ✔ | ERK,p38 MAPK | 95+% | ||||||||||||||||
| Urolithin B | ✔ | ERK,NF-κB | 95% | ||||||||||||||||
| Cucurbitacin IIb | ✔ | NF-κB | 99% | ||||||||||||||||
| Astragaloside IV | ✔ | Akt,mTOR,NF-κB | 98% | ||||||||||||||||
| m-PEG25-NHS ester | ✔ | 95% | |||||||||||||||||
| NDMC101 | ✔ | 99%+ | |||||||||||||||||
| DB07268 | ++++ JNK1, IC50: 9 nM | 99%+ | |||||||||||||||||
| SP600125 | + MKK4, IC50: 0.4 μM | +++ JNK1, IC50: 40 nM | +++ JNK2, IC50: 40 nM | +++ JNK3, IC50: 90 nM | 98% | ||||||||||||||
| JNK-IN-7 | ++++ JNK1, IC50: 1.5 nM | ++++ JNK2, IC50: 2 nM | ++++ JNK3, IC50: 0.7 nM | 99% | |||||||||||||||
| JNK-IN-8 | ++++ JNK1, IC50: 4.7 nM | +++ JNK2, IC50: 18.7 nM | ++++ JNK3, IC50: 1 nM | 99%+ | |||||||||||||||
| 3,3',5-Triiodo-L-thyronine | ++ JNK1, Kd: 240 nM | ++ JNK2, Kd: 290 nM | +++ JNK3, Kd: 66 nM | 98% | |||||||||||||||
| IQ-1S free acid | + JNK1, IC50: 390 nM | ++ JNK2, IC50: 360 nM | +++ JNK3, IC50: 87 nM | 99% | |||||||||||||||
| BI-78D3 | ++ JNK, IC50: 280 nM | ++ JNK, IC50: 280 nM | ++ JNK, IC50: 280 nM | ++ JNK, IC50: 280 nM | 99%+ | ||||||||||||||
| Bentamapimod | +++ JNK1, IC50: 80 nM | +++ JNK2, IC50: 90 nM | ++ JNK3, IC50: 230 nM | 98% | |||||||||||||||
| Resveratrol | + JNK1, IC50: 50 μM | 98% | |||||||||||||||||
| Indirubin-3′-oxime | ✔ | 99%+ | |||||||||||||||||
| SU3327 | + JNK, IC50: 0.7 μM | + JNK, IC50: 0.7 μM | + JNK, IC50: 0.7 μM | + JNK, IC50: 0.7 μM | 99%+ | ||||||||||||||
| JNK Inhibitor VIII | ++++ JNK1, Ki: 2 nM JNK1, IC50: 45 nM | ++++ JNK2, IC50: 160 nM JNK2, Ki: 4 nM | +++ JNK3, Ki: 52 nM | 98% | |||||||||||||||
| Doramapimod | ✔ | 99%+ | |||||||||||||||||
| RPI-1 | ✔ | 99% | |||||||||||||||||
| TCS JNK 5a | ++ JNK2, pIC50: 6.5 | ++ JNK3, pIC50: 6.7 | 98% | ||||||||||||||||
| SP 600125, negative control | + JNK2, IC50: 18 μM | + JNK3, IC50: 24 μM | 97% | ||||||||||||||||
| 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 | c-Jun N-terminal kinase-1 (JNK-1) is a member of the mitogen activated protein kinase (MAP kinase) family of enzymes responsible for the serine/threonine phosphorylation of intracellular targets. JNK-1 and the other JNK enzymes JNK-2 and JNK-3 are activated in response to cellular stresses and various cytokines, and they participate in the onset of apoptosis. TCS JNK 6o is a pan-JNK inhibitor with Ki values of 2, 4 and 52 nM for JNK-1, JNK-2 and JNK-3, respectively, and has IC50 values of 45 and 160 nM for JNK-1 and JNK-2, respectively. In Sprague-Dawley rats, TCS JNK 6o showed a short half-life of roughly 1 h, with rapid clearance and barely measurable bioavailability. Microsomal incubation studies revealed that oxidative metabolism was very rapid with this compound[2]. Moreover, inhibition of primordial follicle activation occurred in the presence of TCS JNK 6o when compared with controls (P < 0.05) after 2 days of culture[3]. | 
| Concentration | Treated Time | Description | References | |
| Primary mouse HSCs | 16 µM | 60 minutes | Inhibited TGFβ-induced c-Jun phosphorylation | Gastroenterology. 2010 Jan;138(1):347-59. | 
| Primary human HSCs | 16 µM | 60 minutes | Inhibited TGFβ-induced c-Jun phosphorylation | Gastroenterology. 2010 Jan;138(1):347-59. | 
| Primary mouse HSCs | 16 µM | 48 hours | Inhibited AngII-induced αSMA expression | Gastroenterology. 2010 Jan;138(1):347-59. | 
| Primary mouse HSCs | 16 µM | 48 hours | Inhibited TGFβ-induced αSMA expression | Gastroenterology. 2010 Jan;138(1):347-59. | 
| Primary human HSCs | 16 µM | 26 hours | Inhibited PDGF-induced [3H]-thymidine incorporation | Gastroenterology. 2010 Jan;138(1):347-59. | 
| HepG2 cells | 5 μM | 1 hour | Pretreatment with JNK inhibitor VIII prevented X1-induced mitochondrial depolarization | Biochem Pharmacol. 2020 Jan;171:113728. | 
| Huh7 cells | 5 μM | 1 hour | Pretreatment with JNK inhibitor VIII prevented X1-induced mitochondrial depolarization | Biochem Pharmacol. 2020 Jan;171:113728. | 
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 2.81mL 0.56mL 0.28mL | 14.03mL 2.81mL 1.40mL | 28.06mL 5.61mL 2.81mL | |
| CAS号 | 894804-07-0 | 
| 分子式 | C18H20N4O4 | 
| 分子量 | 356.38 | 
| SMILES Code | O=C(NC1=NC(OCC)=C(C#N)C(N)=C1)CC2=CC(OC)=CC=C2OC | 
| MDL No. | MFCD19690908 | 
| 别名 | TCS JNK 6o; c-Jun N-terminal Kinase Inhibitor VIII | 
| 运输 | 蓝冰 | 
| InChI Key | KQMPRSZTUSSXND-UHFFFAOYSA-N | 
| Pubchem ID | 11624601 | 
| 存储条件 | In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry,Store in freezer, under -20°C | 
| 溶解方案 | DMSO: 250 mg/mL(701.51 mM),配合低频超声助溶,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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