| 名称 | JNK-IN-8 |
| 描述 | JNK-IN-8 (JNK Inhibitor XVI) is an effective JNK inhibitor that inhibits JNK1, JNK2, and JNK3 with IC₅₀ values of 4.7, 18.7, and 1 nM, respectively. JNK-IN-8 offers the advantages of minimal off-target activity, sustained inhibition, and high specificity. JNK-IN-8 primarily acts by blocking the JNK/c-Jun signaling pathway, inhibiting the phosphorylation of the downstream transcription factor c-Jun, thereby regulating the expression of genes associated with inflammatory responses, apoptosis, and stress responses. JNK-IN-8 can be used in research on tumors, inflammation, and neurological diseases. |
| 细胞实验 | JNK-IN-8 is dissolved in DMSO and stored, and then diluted with appropriate media before use[1]. HEK-293 cells stably expressing Interleukin Receptor 1 (HEK293-IL1R) are cultured in Dulbecco's Modified Eagle's medium (DMEM) supplemented with 10% FBS, 2 mM glutamine and 1×antimycotic/antibiotic solution. Cells are serum starved for 18 h before incubation with DMSO or JNK-IN-8, stimulated with 2 μM Anisomycin for 1h and lysates are clarified by centrifugation for 10 min at 16000 g and 4°C[1]. |
| 激酶实验 | A375 cells are pre-treated with 1 μM JNK-IN-8 for the indicated amounts of time. Remove the medium and wash 3 times with PBS. Resuspend the cell pellet with 1 mL Lysis Buffer (1% NP-40, 1% CHAPS, 25 mM Tris, 150 mM NaCl, Phosphatase Inhibitor Cocktail, and Protease Inhibitor Cocktail). Rotate end-to-end for 30 min at 4°C. Lysates are cleared by centrifugation at 14000 rpm for 15 min in the Eppendorf. The cleared lysates gel filtered into Kinase Buffer (0.1% NP-40, 20 mM HEPES, 150 mM NaCl, Phosphatase Inhibitor Cocktail, Protease Inhibitor Cocktail) using Bio-Rad 10DG colums. The total protein concentration of the gel-filtered lysate should be around 5-15 mg/mL. Cell lysate is labeled with the probe from ActivX at 5 μM for 1 hour. Samples are reduced with DTT, and cysteines are blocked with iodoacetamide and gel filtered to remove excess reagents and exchange the buffer. Add 1 volume of 2X Binding Buffer (2% Triton-100, 1% NP-40, 2 mM EDTA, 2X PBS) and 50 μL streptavidin bead slurry and rotate end-to-end for 2 hours, centrifuge at 7000 rpm for 2 min. Wash 3 times with 1X Binding Buffer and 3 times with PBS. Add 30 μL 1X sample buffer to beads, heat samples at 95°C for 10 min. Run samples on an SDS-PAGE gel at 110V. After transferred, the membrane is immunoblotted with JNK antibody[1]. |
| 体外活性 | 方法：PDAC 细胞接种于 6 孔板，长期培养。每 3 天更换含 JNK-IN-8 培养基（1 μM），持续 14 天，结晶紫染色计数集落。
结果：JNK-IN-8 单药抑制集落形成。[1] |
| 体内活性 | 方法：将 P411-T1 或 P422-T1 PDX 组织移植于裸鼠皮下。待肿瘤可触及后，随机分组开始口服灌胃 JNK-IN-8 (30 mg/kg，每日一次)，共 14 天。
结果： 与体外结果一致，证实 JNK-IN-8 能增强 FOLFOX 的体内抗肿瘤活性。[1]
方法：成年雄性 Sprague-Dawley 大鼠通过气管内滴注 LPS(5 mg/kg) 建立 ARDS 模型，24 小时后开始腹腔注射 JNK-IN-8 (20 mg/kg) ，每日一次。给药后通过行为学测试和分子生物学分析评估效果。
结果：JNK-IN-8 处理显著缩短了 ARDS 大鼠的逃避潜伏期，改善了空间学习和记忆能力，海马组织中 TNF-α、IL-6 和 IL-1β等促炎细胞因子水平显著降低。[2] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 56 mg/mL (110.33 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.94 mM), Sonication is recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
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| 关键字 | Kit (V559D,T670I) | Kit (V559D) | JNK-IN-8 | JNKIN8 | JNK3 | JNK2 | JNK1 | JNK IN 8 | JNK | Inhibitor | inhibit | cKit |
| 相关产品 | Astragaloside IV | Berberine hydrogen sulphate | Chloranil | Gilteritinib | Lenvatinib | Chloramphenicol | Regorafenib | Pazopanib | Dasatinib | Sorafenib | Pexidartinib | Metacetamol |
| 相关库 | 抑制剂库 | 经典已知活性库 | 抗癌化合物库 | 已知活性化合物库 | 激酶抑制剂库 | 抗衰老化合物库 | 高选择性抑制剂库 | 神经退行性疾病化合物库 | 免疫/炎症分子化合物库 | 膜蛋白靶向化合物库 | 疼痛相关化合物库 | 酪氨酸激酶分子库 |
