上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
JNK-IN-8 (Synonyms: JNK Inhibitor XVI) 纯度: 99.59%
JNK-IN-8 (JNK Inhibitor XVI) 是一种有效的 JNK 抑制剂,抑制 JNK1,JNK2 和 JNK3,IC50 分别为 4.7 nM,18.7 nM 和 1 nM。
JNK-IN-8 Chemical Structure
CAS No. : 1410880-22-6
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Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥1106 | In-stock | |
2 mg | ¥620 | In-stock | |
5 mg | ¥990 | In-stock | |
10 mg | ¥1780 | In-stock | |
50 mg | ¥5600 | In-stock | |
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生物活性 |
JNK-IN-8 (JNK Inhibitor XVI) is a potent JNK inhibitor with IC50s of 4.7 nM, 18.7 nM, and 1 nM for JNK1, JNK2, and JNK3, respectively[1]. |
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IC50 & Target[1] |
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体外研究 (In Vitro) |
JNK-IN-8 inhibits phosphorylation of c-Jun, a direct substrate of JNK kinase. JNK-IN-8 inhibits c-Jun phosphorylation in HeLa and A375 cells with EC50 of 486 nM and 338 nM, respectively. JNK-IN-8 also exhibits exceptional selectivity based upon KinomeScan and enzymatic profiling. Cumulatively these combined profiling technologies demonstrate that both JNK-IN-8 and JNK-IN-12 are remarkably selective covalent JNK inhibitors and are appropriate for interrogating JNK-dependent biological phenomena[1]. JNK-IN-8, a selective pan-JNK inhibitor, is discovered to inhibit JNK kinase by broad-base kinase selectivity profiling of a library of acrylamide kinase inhibitors based on the structure of imatinib using the KinomeSca approach. JNK-IN-8 possess distinct regio-chemistry of the 1,4-dianiline and 1,3-aminobenzoic acid substructures relative to imatinib and uses an N,N-dimethyl butenoic actemide warhead to covalently target Cys154. JNK-IN-8 adopts an L-shaped type I binding conformation to access Cys 154 located towards the lip of the ATP-binding site[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
507.59 |
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Formula |
C29H29N7O2 |
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CAS 号 |
1410880-22-6 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 35 mg/mL (68.95 mM) * “≥” means soluble, but saturation unknown. 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Kinase Assay [1] |
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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Cell Assay [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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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