 
        
        
        iJak-381是一种 JAK1/2 抑制剂,具有抗炎活性。iJak-381 可阻断 IL-13 的信号传导,还抑制 IL-4 和 IL-6 信号通路。iJak-381 还降低 p-STAT6 的水平,抑制炎症细胞流入小鼠肺部。iJak-381 可抑制气道高反应性反应 (AHR)。
 
                                 
                                
                            

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| 产品名称 | JAK1 ↓ ↑ | JAK2 ↓ ↑ | JAK3 ↓ ↑ | Tyk2 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Decernotinib | +++ JAK1, IC50: 11 nM JAK1, Ki: 11 nM | +++ JAK2, Ki: 13 nM | ++++ JAK3, Ki: 2.5 nM | +++ TYK2, Ki: 13 nM | 99%+ | ||||||||||||||
| ZM39923 HCl | + JAK1, pIC50: 4.4 | + JAK3, pIC50: 7.1 | EGFR | 97% | |||||||||||||||
| Cerdulatinib | +++ JAK1, IC50: 12 nM | +++ JAK2, IC50: 6 nM | +++ JAK3, IC50: 8 nM | ++++ TYK2, IC50: 0.5 nM | 99%+ | ||||||||||||||
| Momelotinib | +++ JAK1, IC50: 11 nM | ++ JAK2, IC50: 18 nM | + JAK3, IC50: 155 nM | 99%+ | |||||||||||||||
| XL019 | + JAK1, IC50: 134.3 nM | ++++ JAK2, IC50: 2.2 nM | + JAK3, IC50: 214.2 nM | FLT3 | 99%+ | ||||||||||||||
| Ruxolitinib | +++ JAK1, IC50: 3.3 nM | ++++ JAK2, IC50: 2.8 nM | 98% | ||||||||||||||||
| Tofacitinib | + JAK1, IC50: 112 nM | ++ JAK2, IC50: 20 nM | ++++ JAK3, IC50: 1 nM | 98% | |||||||||||||||
| Ruxolitinib (S enantiomer) | +++ JAK1, IC50: 3.3 nM | ++++ JAK2, IC50: 2.8 nM | ++ TYK2, IC50: 19 nM | 98% | |||||||||||||||
| Filgotinib | +++ JAK1, IC50: 10 nM | ++ JAK2, IC50: 28 nM | + JAK3, IC50: 810 nM | + TYK2, IC50: 116 nM | 99% | ||||||||||||||
| Baricitinib | +++ JAK1, IC50: 5.9 nM | +++ JAK2, IC50: 5.7 nM | ++ TYK2, IC50: 53 nM | 99% | |||||||||||||||
| Gandotinib | ++ JAK1, IC50: 19.8 nM | ++++ JAK2, IC50: 0.288 nM JAK2 (V617F), Ki: 0.245 nM | ++ JAK3, IC50: 48.0 nM | ++ TYK2, IC50: 44 nM | FLT3 | 99%+ | |||||||||||||
| Oclacitinib maleate | +++ JAK1, IC50: 10nM | ++ JAK2, IC50: 18nM | + JAK3, IC50: 99nM | + TYK2, IC50: 84nM | 98+% | ||||||||||||||
| NVP-BSK805 2HCl | ++ JAK1, IC50: 31.63 nM | ++++ JAK2, IC50: ~0.5 nM | ++ JAK3, IC50: 18.68 nM | +++ TYK2, IC50: 10.76 nM | 95% | ||||||||||||||
| Peficitinib | ✔ | 98% | |||||||||||||||||
| Go6976 | ✔ | FLT3 | 99%+ | ||||||||||||||||
| AZD-1480 | ++++ JAK2, IC50: 0.26 nM | 99%+ | |||||||||||||||||
| Fedratinib | +++ JAK2, IC50: 3 nM JAK2 (V617F), IC50: 3 nM | RET,FLT3 | 99%+ | ||||||||||||||||
| WP1066 | + JAK2, IC50: 2.3 μM | 98% | |||||||||||||||||
| Curcumol | ✔ | 98% | |||||||||||||||||
| AZ960 | ++++ JAK2, IC50: <3 nM JAK2, Ki: 0.45 nM | 97% | |||||||||||||||||
| GLPG0634 analog | ✔ | 99%+ | |||||||||||||||||
| CEP-33779 | ++++ JAK2, IC50: 1.8 nM | 99%+ | |||||||||||||||||
| FLLL32 | + JAK2, IC50: <5 μM | 99%+ | |||||||||||||||||
| WHI-P154 | + JAK3, IC50: 1.8 μM | VEGFR,EGFR,Src | 98% | ||||||||||||||||
| BMS-911543 | ++++ JAK2, IC50: 1.1 nM | + JAK3, IC50: 75 nM | ++ TYK2, IC50: 66 nM | 95% | |||||||||||||||
| TG101209 | +++ JAK2, IC50: 6 nM | + JAK3, IC50: 169 nM | RET,FLT3 | 99%+ | |||||||||||||||
| AT9283 | ++++ JAK2, IC50: 1.2 nM | ++++ JAK3, IC50: 1.1 nM | 99%+ | ||||||||||||||||
| Pacritinib | ++ JAK2, IC50: 23 nM JAK2 (V617F), IC50: 19 nM | + JAK3, IC50: 520 nM | ++ TYK2, IC50: 50 nM | FLT3 | 97% | ||||||||||||||
| Tofacitinib citrate | ++ JAK2, IC50: 20 nM | ++++ JAK3, IC50: 1 nM | 99% | ||||||||||||||||
| FM-381 | ++++ JAK3, IC50: 127 pM | 98% | |||||||||||||||||
| 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。 | |||||||||||||||||||
| 描述 | iJak-381 acts as an inhibitor of JAK1/2, exhibiting anti-inflammatory properties. It disrupts IL-13 signaling and also impedes the signaling pathways of IL-4 and IL-6. Additionally, iJak-381 lowers p-STAT6 levels and curtails the entry of inflammatory cells into the mouse lungs. It effectively prevents airway hyperresponsiveness (AHR)[1]. | 
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 1.63mL 0.33mL 0.16mL | 8.17mL 1.63mL 0.82mL | 16.34mL 3.27mL 1.63mL | |
| CAS号 | 1831144-46-7 | 
| 分子式 | C28H28ClF2N9O3 | 
| 分子量 | 612.03 | 
| SMILES Code | O=C(C1=C2N=CC=CN2N=C1)NC3=CN(CC(N4CCC(N(CCC#N)C)CC4)=O)N=C3C5=CC(Cl)=CC=C5OC(F)F | 
| MDL No. | N/A | 
| 别名 | |
| 运输 | 蓝冰 | 
| InChI Key | ITNFPSJJBYFVEA-UHFFFAOYSA-N | 
| Pubchem ID | 118522534 | 
| 存储条件 | In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, 2-8°C | 
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