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                同义名:
                    
                        
                            
                                IQ-1S (free acid); IQ-1S
                            
                        
                    
                
                
                
                    
                     
                
            
IQ-1S free acid是一种选择性 JNK3 抑制剂,IC50 值为 87 nM,对 JNK 1/2 的活性较弱,其 IC50 值分别为 390 nM 和 360 nM。
 HazMat Fee +
 HazMat Fee + There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
| Type | HazMat fee for 500 gram (Estimated) | 
| Excepted Quantity | USD 0.00 | 
| Limited Quantity | USD 15-60 | 
| Inaccessible (Haz class 6.1), Domestic | USD 80+ | 
| Inaccessible (Haz class 6.1), International | USD 150+ | 
| Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ | 
| Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ | 
 
                                 
                                
                            

| 规格 | 价格 | 会员价 | 库存 | 数量 | |||
|---|---|---|---|---|---|---|---|
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| 产品名称 | JNK ↓ ↑ | JNK1 ↓ ↑ | JNK2 ↓ ↑ | JNK3 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Mulberroside A | ✔ | 99%+ | |||||||||||||||||
| Loureirin B | ✔ | Potassium Channel,Calcium Channel | 99%+ | ||||||||||||||||
| Ginsenoside Re | ✔ | NF-κB | 98% | ||||||||||||||||
| (+)-(3R,8S)-Falcarindiol | ✔ | ERK,STAT | 99%+ | ||||||||||||||||
| trans-Zeatin | ✔ | p38 MAPK,ERK | 95+% | ||||||||||||||||
| Urolithin B | ✔ | NF-κB,ERK | 95% | ||||||||||||||||
| Cucurbitacin IIb | ✔ | NF-κB | 99% | ||||||||||||||||
| Astragaloside IV | ✔ | Akt,NF-κB,mTOR | 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, Ki: 4 nM JNK2, IC50: 160 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 | The activating protein 1 (AP-1) and nuclear factor-κB (NF-κB) families of transcription factors are implicated in many pathological processes. C-Jun N-terminal kinases (JNKs) have been shown to regulate the transcriptional activity of AP-1. IQ-1S free acid is a potent inhibitor of pro-inflammatory cytokines without cytotoxic effect. It inhibits NF-κB/AP-1 activity with an IC50 value of 2.3±0.41μM. Treatment of human peripheral blood mononuclear cells with IQ-1S free acid (20μM) significantly inhibited LPS (200ng/ml)-induced production of pro-inflammatory cytokines, including IL-1α, IL-1β, IL-6, IL-10, and TNF-α, compared to DMSO-treated controls. The IC50 values of IQ-1S free acid for TNF-α and IL-6 in human MonoMac-6 cells are 1.3±0.31 and 3.8±0.78μM, respectively. The IC50 values of IQ-1S free acid for TNF-α and IL-6 in human peripheral blood mononuclear cells are 2.6±0.63 and 5.6±1.1μM, respectively. The IC50 values of IQ-1S free acid for NO in murine J774.A1 cells is 3.1±0.87μM. The binding affinity of IQ-1S free acid for JNK1, JNK2, and JNK3 are 0.24, 0.36, and 0.10μM, respectively. IQ-1S free acid also exhibits binding affinity towards CK1δ, PI3Kγ, and MKNK2 with Kd values of 0.38, 0.47, and 0.92μM, respectively. When mice were i.p. administered with IQ-1S free acid at a dose of 12.5 and 30mg/kg, the serum AUC0-12h values were 2.9 and 7.4μM/h, respectively. The i.p. injection of OVA-challenged mice with 12.5mg/kg IQ-1S free acid (every 12 h, a total of 5 injections) significantly suppressed OVA-induced CD4+ T-cell immune response compared to the vehicle-treated group[3]. | 
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 4.04mL 0.81mL 0.40mL | 20.22mL 4.04mL 2.02mL | 40.44mL 8.09mL 4.04mL | |
| CAS号 | 23146-22-7 | 
| 分子式 | C15H9N3O | 
| 分子量 | 247.25 | 
| SMILES Code | O/N=C1C2=C(C3=NC4=CC=CC=C4N=C3\1)C=CC=C2 | 
| MDL No. | MFCD00612483 | 
| 别名 | IQ-1S (free acid); IQ-1S; IQ-1 | 
| 运输 | 蓝冰 | 
| InChI Key | YSYIWCNPSZNNKW-UHFFFAOYSA-N | 
| Pubchem ID | 619002 | 
| 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: 16 mg/mL(64.71 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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