JNK-IN-8

Catalog No.S4901 Synonyms: JNK Inhibitor XVI

For research use only.

JNK-IN-8 (JNK Inhibitor XVI) 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.

JNK-IN-8 Chemical Structure

CAS No. 1410880-22-6

Selleck's JNK-IN-8 has been cited by 71 publications

Purity & Quality Control

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Biological Activity

Description JNK-IN-8 (JNK Inhibitor XVI) 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 HeLa cells MYjGeY5kfGmxbjDhd5NigQ>? M1rNfVEhcA>? M3[yTmlvcGmkaYTpc44hd2ZiSl7LN{1u\WSrYYTl[EBkNWq3bjDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iSHXMZUBk\WyuczDh[pRmeiBzIHjyJIlv[3WkYYTpc44tKEmFNUC9NE41QDZizszN NVz0N5g2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0NVU2OzVpPkK1OFE2PTN3PD;hQi=>
human A375 cells M3vL[WZ2dmO2aX;uJIF{e2G7 M4XyfVEhcA>? M3PrU2lvcGmkaYTpc44hd2ZiSl7LN{1u\WSrYYTl[EBkNWq3bjDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iQUO3OUBk\WyuczDh[pRmeiBzIHjyJIlv[3WkYYTpc44tKEmFNUC9NE4{OzhizszN MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTRzNUWzOUc,OjV2MUW1N|U9N2F-
Assay
Methods Test Index PMID
Western blot Notch1 / c-Myc / Cyclin D1 / p21 ; c-Jun / p-c-Jun / ATF2 / p-ATF2 / Elk-1 / pElk-1 27941886
Growth inhibition assay Cell viability 25847947

Protocol (from reference)

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

10mg/mL

Chemical Information

Molecular Weight 507.59
Formula

C29H29N7O2

CAS No. 1410880-22-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C=CC(=C1)NC(=O)C2=CC(=CC=C2)NC(=O)C=CCN(C)C)NC3=NC=CC(=N3)C4=CN=CC=C4

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Tech Support

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.

Handling Instructions

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