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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Mitogen-activated protein kinase (MAPK)>JNK inhibitors>JNK-IN-8
JNK-IN-8
  • JNK-IN-8

JNK-IN-8 NEW

Price $39 $70 $122
Package 2mg 5mg 10mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-17

Product Details

Product Name: JNK-IN-8 CAS No.: 1410880-22-6
Purity: 99.24% Supply Ability: 10g
Release date: 2024/11/17

Product Introduction

Bioactivity

名稱JNK-IN-8
描述JNK-IN-8 (JNK Inhibitor XVI) is an irreversible JNK1/2/4 inhibitor (IC50: 4.7/18.7/1 nM) with over 10-fold selectivity compared to MNK2 and Fms, and no inhibition of Met, c-Kit, or PDGFRβ in the A375 cell line.
細胞實驗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].
激酶實驗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].
體內(nèi)活性JNK-IN-8 (10 mM) effectively inhibits the phosphorylation of c-Jun stimulated by IL-1β in IL-1R cells. It displays significant selectivity for the 1,4-bis(phenylamino) and 1,3-aminobenzoic acid structural regions compared to imatinib, covalently binding to the Cys154 target via an N,N-dimethylbutenamide linkage. JNK-IN-8 inhibits the phosphorylation of c-Jun in HeLa (EC50: 486 nM) and A375 (EC50: 338 nM) cells. Its binding with PIK3C3, IRAK1, PIP5K3, and PIP4K2C significantly enhances selectivity and elimination rates. JNK-IN-8 inhibits JNK2 through Cys116.
存儲條件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 55 mg/mL (108.36 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
關(guān)鍵字JNKIN8 | Inhibitor | JNK | JNK IN 8 | inhibit | JNK-IN-8
相關(guān)產(chǎn)品Gilteritinib | Regorafenib monohydrate | Sorafenib | Astragaloside IV | Pexidartinib | Regorafenib | Sorafenib tosylate | (-)-Bornyl acetate | Anisomycin | Imatinib | Pazopanib | Axitinib
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Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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