生物活性 | |||
---|---|---|---|
描述 | IQ-3 is a specific inhibitor of the JNK family and is particularly potent against JNK3.The Kd values of IQ-3 against JNK1, JNK2 and JNK3 were 0.24 μM, 0.29 μM and 0.066 μM, respectively. Further studies have confirmed that IQ-3 is a competitive inhibitor of the ATP-binding site of JNK3. The IC50 values of the response of IQ-3 to the different analyses in different cells were 2.5 μM and 2.5 μM, respectively. The response IC50 values of IQ-3 in different cells with different analytical methods were 2.2 μM (TNF-α in human monoMac-6 cells), 1.5 μM (IL-6 in human monoMac-6 cells), 4.7 μM (TNF-α in human PBMCs), 9.1 μM (IL-6 in human PBMCs), and 6.1 μM (NO in murine J774.A1), respectively. IQ-3 inhibited LPS-induced NF-κB/AP-1 transcriptional activity with an IC50 value of 1.4 μM (human THP-1 blue monocytes)[1]. |
临床研究 | |||||
---|---|---|---|---|---|
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00796302 | Attention Deficit Disorder Wit... 展开 >>h Hyperactivity 收起 << | Phase 4 | Completed | - | United States, New York ... 展开 >> State University of New York Stony Brook Stony Brook, New York, United States, 11794 United States, Ohio Case Western Reserve University Cleveland, Ohio, United States, 44106 Ohio State University Nisonger Center Columbus, Ohio, United States, 43210 United States, Pennsylvania University of Pittsburgh Pittsburgh, Pennsylvania, United States, 15213 收起 << |
NCT00447902 | HIV Infections | Phase 3 | Terminated | - | United States, California ... 展开 >> 1182.99.32 Boehringer Ingelheim Investigational Site Beverly Hills, California, United States United States, Florida 1182.99.31 Boehringer Ingelheim Investigational Site Fort Lauderdale, Florida, United States United States, Rhode Island 1182.99.12 Boehringer Ingelheim Investigational Site Providence, Rhode Island, United States United States, Texas 1182.99.1 Boehringer Ingelheim Investigational Site Austin, Texas, United States 1182.99.4 Boehringer Ingelheim Investigational Site Houston, Texas, United States Argentina 1182.99.54001 Capital Federal, Argentina Brazil 1182.99.55002 Hospital DIA Sacomã - São Paulo, Brazil 1182.99.55004 Unidade de Referência em doenças Infecciosas Preveníveis Santo André, Brazil 1182.99.55001 Universidade Federal de Sao Paulo Sao Paulo, Brazil 1182.99.55003 Centro de Referência e Treinamento - DST/AIDS Vila Mariana - Sao Paulo, Brazil France 1182.99.3301A Boehringer Ingelheim Investigational Site Garches, France 1182.99.3306G Boehringer Ingelheim Investigational Site Nantes, France 1182.99.3306K Boehringer Ingelheim Investigational Site Nantes, France 1182.99.3310C Boehringer Ingelheim Investigational Site Nice cedex 3, France 1182.99.3310D Boehringer Ingelheim Investigational Site Nice cedex 3, France 1182.99.3310E Boehringer Ingelheim Investigational Site Nice cedex 3, France 1182.99.3310F Boehringer Ingelheim Investigational Site Nice cedex 3, France 1182.99.3310G Boehringer Ingelheim Investigational Site Nice cedex 3, France 1182.99.3310H Boehringer Ingelheim Investigational Site Nice cedex 3, France 1182.99.3304A Boehringer Ingelheim Investigational Site Paris, France 1182.99.3304C Boehringer Ingelheim Investigational Site Paris, France 1182.99.3302A Boehringer Ingelheim Investigational Site Perpignan, France Germany 1182.99.4909 Boehringer Ingelheim Investigational Site Düsseldorf, Germany Italy 1182.99.3912 Boehringer Ingelheim Investigational Site Ancona, Italy 1182.99.3901 Boehringer Ingelheim Investigational Site Milano, Italy 1182.99.3911 Boehringer Ingelheim Investigational Site Milano, Italy 1182.99.3916 Boehringer Ingelheim Investigational Site Milano, Italy 1182.99.3906 Boehringer Ingelheim Investigational Site Pavia, Italy Spain 1182.99.3402 Barcelona, Spain 1182.99.3407 Madrid, Spain 收起 << |
NCT00796302 | - | Completed | - | - |
实验方案 | |||
---|---|---|---|
1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.93mL 0.59mL 0.29mL |
14.65mL 2.93mL 1.46mL |
29.30mL 5.86mL 2.93mL |
参考文献 |
---|