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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Cited by 30 Publications

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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 MUXGeY5kfGmxbjDhd5NigQ>? NFnxfpUyKGh? MUHJcohq[mm2aX;uJI9nKEqQS{OtcYVlcWG2ZXSgZ{1rfW5icHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEF|N{WgZ4VtdHNiYX\0[ZIhOSCqcjDpcoN2[mG2aX;uMEBKSzVyPUCuN|M5KM7:TR?= NXnuVWRTOjV2MUW1N|U>
human HeLa cells NF3HZW9HfW6ldHnvckBie3OjeR?= NV;u[HBXOSCq M3nTUmlvcGmkaYTpc44hd2ZiSl7LN{1u\WSrYYTl[EBkNWq3bjDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iSHXMZUBk\WyuczDh[pRmeiBzIHjyJIlv[3WkYYTpc44tKEmFNUC9NE41QDZizszN M1\pOVI2PDF3NUO1

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
c-Jun / p-c-Jun / ATF2 / p-ATF2 / Elk-1 / pElk-1; 

PubMed: 27941886     


JNK-IN-8 treatment inhibited c-Jun phosphorylation at Ser63 and Ser73 by JNK in TNBC cells as analyzed by Western blotting.

Notch1 / c-Myc / Cyclin D1 / p21; 

PubMed: 27941886     


JNK-IN-8 treatment reduced expression of Notch1 and c-Jun phosphorylation at Ser63 and Ser73 as analyzed by Western blotting. JNK-IN-8 treatment also reduced expression of c-MYC, cyclin D1, and p21. Cells were treated with JNK-IN-8 for 48 h and then subjected to Western blotting. α-Tubulin was used as a loading control.

27941886
Growth inhibition assay
Cell viability; 

PubMed: 25847947     


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

25847947

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (197.0 mM)
Water Insoluble
Ethanol Insoluble
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

* 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
in solvent
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID