化合物JNK-IN-8 T2668

Product Introduction
Bioactivity


英文名: JNK-IN-8

描述: 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、18.7 和 1 nM。

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].

体内活性: JNK-IN-8（10 mM）对IL-1R细胞中IL-1β刺激的c-Jun磷酸化有抑制作用。与伊马替尼相比,JNK-IN-8有明显的1,4-双苯胺和1,3-氨基苯甲酸结构区域选择性,且以N,N-二甲基丁烯乙酰胺共价结合Cys154靶点。JNK-IN-8抑制HeLa（EC50：486 nM）和A375（EC50：338 nM）细胞中c-Jun的磷酸化。JNK-IN-8与PIK3C3,IRAK1,PIP5K3和PIP4K2C结合可使选择性和消除率显著提高。JNK-IN-8经Cys116抑制JNK2。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 55 mg/mL (108.36 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
5% DMSO+95% Saline : 4.65 mg/mL (9.16 mM, suspension)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)


关键字: JNKIN8 | Inhibitor | JNK | JNK IN 8 | inhibit | JNK-IN-8

相关产品: 15-Methoxypinusolidic acid | Vincristine | Dehydroglyasperin C | Polyphyllin I | Astragaloside | 6,4'-Dihydroxy-7-methoxyflavanone | Tomatidine | (-)-Bornyl acetate | D-JNKI-1 acetate | Loureirin B

相关库: Anti-Neurodegenerative Disease Compound Library | HIF-1 Signaling Pathway Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Inhibitor Library | Tyrosine Kinase Inhibitor Library | Highly Selective Inhibitor Library | Anti-Pancreatic Cancer Compound Library | MAPK Inhibitor Library

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