JNK-IN-8

Catalog No.S4901

JNK-IN-8 Chemical Structure

Molecular Weight(MW): 507.59

JNK-IN-8 is the first irreversible JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 4.7 nM, 18.7 nM and 1 nM, >10-fold selectivity against MNK2, Fms and no inhibition to c-Kit, Met, PDGFRβin A375 cell line.

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USD 170 In stock
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3 Customer Reviews

  • The viability of DLBCL cell lines was assessed after 72 h of treatment with the indicated concentrations of the JNK inhibitor JNK-IN-8. Mean + SEM of at least three independent experiments is shown.

    J Exp Med, 2015, 212(5): 775-92. JNK-IN-8 purchased from Selleck.

    ICT induces JNK activation, mediating mPTP opening and CRC cell necrosis. JNK expression (p- and regular) in HT-29 or the primary CRC cells stimulated with applied ICT was tested by Western blots (a). HT-29 cells were pre-treated with JNK inhibitors SP600125 (SP), JNK inhibitor IX (JNK-IX), and JNK-IN-8 (JNKi-8) (5 μM each) for 1 h, followed by ICT (25 μM) stimulation, MMP decrease was tested by JC-10 dye assay (b, after 12 h), and cell necrosis was tested by LDH release assay (c, after 72 h).

    Tumour Biol, 2016, 37(3):3135-44. JNK-IN-8 purchased from Selleck.

  • SCC-9 cells were pre-treated with JNK inhibitor SP 600125 (1 umol/L) or JNK-IN-8 (1 umol/L) for 1 h, cells were also stimulated with indicated AZD8055 and cultured for 72 h, cell survival was analyzed. Scramble RNAi or JNK1/2 RNAi (JNK RNAi-1 or JNK RNAi-2, see methods) transfected HEK-293 cells were stimulated with AZD8055, cells were further cultured for 72 h before cell survival was tested.

    Biochem Biophys Res Commun 2013 440(4), 701-6. JNK-IN-8 purchased from Selleck.

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Biological Activity

Description JNK-IN-8 is the first irreversible JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 4.7 nM, 18.7 nM and 1 nM, >10-fold selectivity against MNK2, Fms and no inhibition to c-Kit, Met, PDGFRβin A375 cell line.
Features JNK-IN-8 and JNK-IN-7 are structurally very similar, but whereas the former is a specific covalent inhibitor of JNKs.
Targets
JNK3 [1]
(A375 cells)
JNK1 [1]
(A375 cells)
JNK2 [1]
(A375 cells)
Kit (V559D,T670I) [1]
(A375 cells)
Kit (V559D) [1]
(A375 cells)
1 nM 4.7 nM 18.7 nM 56 nM 92 nM
In vitro

JNK-IN-8 inhibits c-Jun phosphorylation in HeLa and A375 cells with EC50 of 486 nM and 338 nM, respectively. JNK-IN-8 shows a dramatic improvement in selectivity and eliminated binding to IRAK1, PIK3C3, PIP4K2C, and PIP5K3. JNK-IN-8 requires Cys116 for JNK2 inhibition. [1] JNK-IN-8 (10 mM) suppresses the IL-1β-stimulated phosphorylation of c-Jun in IL-1R cells, an established substrate of the JNKs. JNK-IN-8 covalently attaches to the JNK isoforms caused a small retardation in the electrophoretic mobility of the JNK isoforms. [2] JNK-IN-8 is discovered to inhibit JNK kinase by broad-based kinase selectivity profiling of a library of acrylamide kinase inhibitors based on the structure of imatinib using the KinomeScan approach. JNK-IN-8 possesses distinct regiochemistry of the 1,4-dianiline and 1,3-aminobenzoic acid substructures relative to imatinib and uses an N,N-dimethyl butenoic acetamide warhead to covalently target Cys154. JNK-IN-8 adopts an L-shaped type I binding conformation to access Cys 154 located toward the lip of the ATP-binding site. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human A375 cells MXHGeY5kfGmxbjDhd5NigQ>? MmfjNUBp MmPSTY5pcWKrdHnvckBw\iCMTluzMY1m\GmjdHXkJIMucnWwIIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCDM{e1JINmdGy|IHHmeIVzKDFiaIKgbY5kfWKjdHnvckwhUUN3ME2wMlM{QCEQvF2= MV[yOVQyPTV|NR?=
human HeLa cells MUTGeY5kfGmxbjDhd5NigQ>? NWm0bm53OSCq MlzVTY5pcWKrdHnvckBw\iCMTluzMY1m\GmjdHXkJIMucnWwIIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCKZVzhJINmdGy|IHHmeIVzKDFiaIKgbY5kfWKjdHnvckwhUUN3ME2wMlQ5PiEQvF2= NETnV2MzPTRzNUWzOS=>

... Click to View More Cell Line Experimental Data

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (197.0 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
10mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 507.59
Formula

C29H29N7O2

CAS No. 1410880-22-6
Storage powder
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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JNK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID