1. MAPK/ERK Pathway
  2. JNK

JNK-IN-8 

Cat. No.: HY-13319 Purity: 99.38%
Handling Instructions

JNK-IN-8 is a potent JNK inhibitor with IC50 of 4.7 nM, 18.7 nM, and 1 nM for JNK1, JNK2, and JNK3, respectively.

For research use only. We do not sell to patients.

JNK-IN-8 Chemical Structure

JNK-IN-8 Chemical Structure

CAS No. : 1410880-22-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 147 In-stock
Estimated Time of Arrival: December 31
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
50 mg USD 648 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
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    JNK-IN-8 purchased from MCE. Usage Cited in: J Biol Chem. 2014 Oct 17;289(42):28753-64.

    Effect of the JNK inhibitor (JNK IN 8) on the induction of MKP-1 and MKP-2. RAW264.7 cells are first pretreated with vehicle (DMSO), 3 μM JNK IN 8, 10 μM of U0126, or a combination of both JNK IN 8 and U0126, for 30 min, and then stimulated with LPS for 60 min. Representative images are shown in the panels.

    JNK-IN-8 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 May 4;37(1):99.

    A co-inhibitor of JNK and integrin β obviously decreases phosphorylation levels of JNK and c-JUN and expression of LOXL2 as compared with JNK inhibitor alone or integrin β1 alone.

    View All JNK Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    JNK-IN-8 is a potent JNK inhibitor with IC50 of 4.7 nM, 18.7 nM, and 1 nM for JNK1, JNK2, and JNK3, respectively.

    IC50 & Target[1]

    JNK3

    1 nM (IC50)

    JNK1

    4.7 nM (IC50)

    JNK2

    18.7 nM (IC50)

    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].

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 35 mg/mL (68.95 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9701 mL 9.8505 mL 19.7009 mL
    5 mM 0.3940 mL 1.9701 mL 3.9402 mL
    10 mM 0.1970 mL 0.9850 mL 1.9701 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    507.59

    Formula

    C₂₉H₂₉N₇O₂

    CAS No.

    1410880-22-6

    SMILES

    CC1=CC(NC(C2=CC=CC(NC(/C=C/CN(C)C)=O)=C2)=O)=CC=C1NC3=NC=CC(C4=CN=CC=C4)=N3

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.38%

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    Product Name:
    JNK-IN-8
    Cat. No.:
    HY-13319
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    JNK-IN-8

    Cat. No.: HY-13319