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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。
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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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 278 | 现货 | |
2 mg | ¥ 393 | 现货 | |
5 mg | ¥ 659 | 现货 | |
10 mg | ¥ 987 | 现货 | |
25 mg | ¥ 1,970 | 现货 | |
50 mg | ¥ 2,930 | 现货 | |
100 mg | ¥ 4,260 | 现货 | |
200 mg | ¥ 5,920 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 795 | 现货 |
产品描述 | JNK-IN-8 (JNK Inhibitor XVI) is an irreversible JNK1/2/4 inhibitor (IC50: 4.7/18.7/1 nM). The selectivity is higher 10-fold than MNK2, Fms and no inhibition of Met, c-Kit, PDGFRβ in A375 cell line. |
靶点活性 | JNK2:18.7 nM, JNK1:4.7 nM, JNK:1 nM |
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。 |
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]. |
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]. |
别名 | JNK Inhibitor XVI |
分子量 | 507.59 |
分子式 | C29H29N7O2 |
CAS No. | 1410880-22-6 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 55 mg/mL (108.36 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
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