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JNK-IN-8

Name: JNK-IN-8
Brand: Selleck Chemicals
SKU: S4901
Rating: 5 (71 reviews)

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.

CAS No. 1410880-22-6

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

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JNK Signaling Pathway Map

Biological Activity

Description

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-

Click to View More Cell Line Experimental Data

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)

References

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. Click to purchase: PEG300 Tween 80	10mg/mL

Chemical Information

Molecular Weight	507.59
Formula	C₂₉H₂₉N₇O₂
CAS No.	1410880-22-6
Storage	3 years	-20°C	powder
Storage	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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In vivo Formulation Calculator (Clear solution)

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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.

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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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