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                同义名:
                    
                        
                            
                                JNK Inhibitor IX; c-Jun N-terminal Kinase Inhibitor IX
                            
                        
                    
                
                
                
                    
                     
                    
                     
                
            
TCS JNK 5a是JNK3的有效抑制剂,其pIC50为6.7。它还抑制JNK2,其pIC50为6.5。
 
                                 
                                
                            

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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 | ✔ | p38 MAPK,ERK | 95+% | ||||||||||||||||
| Urolithin B | ✔ | NF-κB,ERK | 95% | ||||||||||||||||
| Cucurbitacin IIb | ✔ | NF-κB | 99% | ||||||||||||||||
| Astragaloside IV | ✔ | mTOR,Akt,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, IC50: 45 nM JNK1, Ki: 2 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 (JNK) is implicated in various human diseases, including cancer, inflammatory disorders, and neurodegeneration. JNK inhibitor IX is a potent JNK inhibitor with pIC50 values of 6.5 and 6.7 for JNK2 and JNK3, respectively[3]. Pre-treatment of human dermal fibroblasts with JNK inhibitor IX (10μM) 30min before chromium exposure significantly reduces caspase-3 activity compared to the group only treated with chromium[4]. Treatment of myeloid cells with JNK inhibitor IX (10μM) for 24 h significantly reduced JNK phosphorylation and increased apoptotic cell death in response to imatinib mesylate[5]. | 
| 作用机制 | JNK inhibitor IX is a potent, ATP-competitive inhibitor of both JNK2 and JNK3[3]. | 
| Concentration | Treated Time | Description | References | |
| Human CD34+ cells | 0.1 μM | 10 days | Used to test the effect on hematopoietic stem cell expansion. The results showed that the inhibitor significantly increased the frequency and number of CD34+CD45RA− cells compared with DMSO-treated control cells | Cell Discov. 2019 Jan 8;5:2. | 
| IMR90 human diploid fibroblasts | 0.5 μM | 4 days | induced spotty nuclear morphology and cellular senescence | Mol Biol Cell. 2015 Sep 1;26(17):2971-85. | 
| Mouse spermatogonial stem cells | 3 μM | 6 days | To inhibit JNK signaling pathway and study its effect on spermatogonial stem cell proliferation. Results showed that JNK Inhibitor IX significantly suppressed spermatogonial stem cell proliferation. | Stem Cell Reports. 2015 Mar 10;4(3):489-502. | 
| HepG2 cells | 10 μM | 7 days | To test the effect of JNK-IN-5A on TAG accumulation in DNL and OA steatosis models. Results showed that JNK-IN-5A significantly reduced TAG accumulation in the DNL model but had no significant effect on the OA model. | iScience. 2023 Aug 25;26(10):107727. | 
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 3.01mL 0.60mL 0.30mL | 15.04mL 3.01mL 1.50mL | 30.08mL 6.02mL 3.01mL | |
| CAS号 | 312917-14-9 | 
| 分子式 | C20H16N2OS | 
| 分子量 | 332.42 | 
| SMILES Code | O=C(NC1=C(C#N)C(CCCC2)=C2S1)C3=C4C=CC=CC4=CC=C3 | 
| MDL No. | MFCD01005305 | 
| 别名 | JNK Inhibitor IX; c-Jun N-terminal Kinase Inhibitor IX; TCS JNK 5a, TCS-JNK-5a, JNK Inhibitor IX, SC-202671, SC 202671, SC202671 | 
| 运输 | 蓝冰 | 
| InChI Key | WQGDQGAFSDMBLA-UHFFFAOYSA-N | 
| Pubchem ID | 766949 | 
| 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: 18 mg/mL(54.15 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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