Butyzamide是一种口服有效的 Mpl 激活剂,Mpl 是血小板生成素受体。Butyzamide 增加 JAK2、STAT3、STAT5 和 MAPK 的磷酸化水平,并在小鼠异种移植实验中提升人血小板水平。
                                
                                
                            

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| 产品名称 | JAK1 ↓ ↑ | JAK2 ↓ ↑ | JAK3 ↓ ↑ | Tyk2 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Decernotinib | 
                                                
                                                    +++
                                                    
                                                    
                                                     JAK1, Ki: 11 nM JAK1, IC50: 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。 | |||||||||||||||||||
| 产品名称 | STAT1 ↓ ↑ | STAT3 ↓ ↑ | STAT5 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Nifuroxazide | ✔ | 98% | |||||||||||||||||
| Fludarabine | ✔ | 98% | |||||||||||||||||
| Artesunate | ✔ | 98% | |||||||||||||||||
| BP-1-102 | 
                                                
                                                    +++
                                                    
                                                    
                                                     STAT3, Kd: 504 nM  | 
                                            
                                        
                                            
                                            99%+ | |||||||||||||||||
| Niclosamide | 
                                                
                                                    ++
                                                    
                                                    
                                                     STAT3, IC50: 0.7 μM  | 
                                            
                                        
                                            
                                            98% | |||||||||||||||||
| Napabucasin | ✔ | 98% | |||||||||||||||||
| Cryptotanshinone | 
                                                
                                                    ++
                                                    
                                                    
                                                     STAT3, IC50: 4.6 μM  | 
                                            
                                        
                                            
                                            98% | |||||||||||||||||
| Stattic | 
                                                
                                                    +
                                                    
                                                    
                                                     STAT3, IC50: 5.1 μM  | 
                                            
                                        
                                            
                                            98% | |||||||||||||||||
| NSC 74859 | 
                                                
                                                    +
                                                    
                                                    
                                                     STAT3, IC50: 86 μM  | 
                                            
                                        
                                            
                                            99%+ | |||||||||||||||||
| Ochromycinone | ✔ | 98% | |||||||||||||||||
| HO-3867 | ✔ | 97% | |||||||||||||||||
| C188-9 | 
                                                
                                                    ++++
                                                    
                                                    
                                                     STAT3, Kd: 4.7 nM  | 
                                            
                                        
                                            
                                            99%+ | |||||||||||||||||
| HJC0152 | ✔ | 99% | |||||||||||||||||
| SH5-07 | ✔ | 95% | |||||||||||||||||
| SH-4-54 | 
                                                
                                                    ++++
                                                    
                                                    
                                                     STAT3, Kd: 300 nM  | 
                                            
                                        
                                            
                                            
                                                
                                                    +++
                                                    
                                                    
                                                     STAT5, Kd: 464 nM  | 
                                            
                                        
                                        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 | p38 MAPK ↓ ↑ | p38α ↓ ↑ | p38β ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| BMS-582949 | 
                                                
                                                    +++
                                                    
                                                    
                                                     p38 MAPK, IC50: 13 nM  | 
                                            
                                        
                                            
                                            98% | |||||||||||||||||
| Adezmapimod | 99%+ | ||||||||||||||||||
| Pexmetinib | ✔ | Tie-2 | 99%+ | ||||||||||||||||
| Skepinone-L | 
                                                
                                                    ++++
                                                    
                                                    
                                                     p38α, IC50: 5 nM  | 
                                            
                                        
                                            
                                            98% | |||||||||||||||||
| Doramapimod | 
                                                
                                                    ++++
                                                    
                                                    
                                                     p38α, IC50: 38 nM p38α, Kd: 0.1 nM  | 
                                            
                                        
                                            
                                            99%+ | |||||||||||||||||
| VX-702 | 99%+ | ||||||||||||||||||
| Ralimetinib dimesylate | 
                                                
                                                    ++++
                                                    
                                                    
                                                     p38α, IC50: 7 nM  | 
                                            
                                        
                                            
                                            98% | |||||||||||||||||
| SB 202190 | 
                                                
                                                    ++
                                                    
                                                    
                                                     p38α, IC50: 50 nM  | 
                                            
                                        
                                            
                                            
                                                
                                                    ++
                                                    
                                                    
                                                     p38β, IC50: 100 nM  | 
                                            
                                        
                                        99%+ | ||||||||||||||||
| Losmapimod | 
                                                
                                                    ++++
                                                    
                                                    
                                                     p38α, pKi: 8.1  | 
                                            
                                        
                                            
                                            
                                                
                                                    +++
                                                    
                                                    
                                                     p38β, pKi: 7.6  | 
                                            
                                        
                                        99%+ | ||||||||||||||||
| Neflamapimod | 
                                                
                                                    +++
                                                    
                                                    
                                                     p38α, IC50: 10 nM  | 
                                            
                                        
                                            
                                            
                                                
                                                    +
                                                    
                                                    
                                                     p38β, IC50: 220 nM  | 
                                            
                                        
                                        99%+ | ||||||||||||||||
| PH-797804 | 
                                                
                                                    ++
                                                    
                                                    
                                                     p38α, IC50: 26 nM  | 
                                            
                                        
                                            
                                            
                                                
                                                    +
                                                    
                                                    
                                                     p38β, IC50: 102 nM  | 
                                            
                                        
                                        99% | ||||||||||||||||
| TAK-715 | 
                                                
                                                    ++++
                                                    
                                                    
                                                     p38α, IC50: 7.1 nM  | 
                                            
                                        
                                            
                                            
                                                
                                                    +
                                                    
                                                    
                                                     p38β, IC50: 0.20 μM  | 
                                            
                                        
                                        99%+ | ||||||||||||||||
| SB 239063 | 
                                                
                                                    ++
                                                    
                                                    
                                                     p38α, IC50: 44 nM  | 
                                            
                                        
                                            
                                            
                                                
                                                    ++
                                                    
                                                    
                                                     p38β, IC50: 44 nM  | 
                                            
                                        
                                        99%+ | ||||||||||||||||
| Pamapimod | 
                                                
                                                    +++
                                                    
                                                    
                                                     p38α, IC50: 0.014 μM  | 
                                            
                                        
                                            
                                            
                                                
                                                    +
                                                    
                                                    
                                                     p38β, IC50: 0.48 μM  | 
                                            
                                        
                                        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 | Butyzamide is an orally bioavailable stimulator of Mpl, a thrombopoietin (TPO) receptor. It enhances the phosphorylation of JAK2, STAT3, STAT5, and MAPK. Additionally, Butyzamide elevates human platelet levels in a mouse xenotransplantation assay[1]. | 
| 体内研究 | Butyzamide (10 mg/kg, 50 mg/kg; oral administration; once daily for 20 days) elevates human platelet levels in NOG mice transplanted with human fetal liver-derived CD34+ cells[1].  | 
                    
| 体外研究 | In Ba/F3-hMpl cells, treatment with Butyzamide (3 μM; 15 min) triggers the phosphorylation of JAK2, STAT3, STAT5, and MAPK[1]. Butyzamide (3 μM; 48 h) stimulates the formation of colony-forming unit-megakaryocyte and polyploid megakaryocytes from human CD34+ hematopoietic progenitor cells[1].  | 
                    
| 计算器 | ||||
| 存储液制备 | ![]()  | 
                        1mg | 5mg | 10mg | 
| 
                             1 mM 5 mM 10 mM  | 
                        
                             1.69mL 0.34mL 0.17mL  | 
                        
                             8.45mL 1.69mL 0.85mL  | 
                        
                             16.90mL 3.38mL 1.69mL  | 
                    |
| CAS号 | 1110767-45-7 | 
| 分子式 | C29H32Cl2N2O5S | 
| 分子量 | 591.55 | 
| SMILES Code | O(C)C1=C(C=CC=C1C(OCCC)C(C)(C)C)C=2N=C(NC(=O)C3=CC(Cl)=C(/C=C(/C(O)=O)\C)C(Cl)=C3)SC2 | 
| MDL No. | N/A | 
| 别名 | |
| 运输 | 蓝冰 | 
| 存储条件 | 
                                
                                    
                                             In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place,Sealed in dry,2-8°C  | 
                        
| 溶解方案 | 
                                
                                    
                                     DMSO: 105 mg/mL(177.5 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  | 
                        
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