JNK-IN-8
Catalog No.S4901
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.
4 Customer Reviews
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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.
Striatal slices from 6-OHDA-lesion mice were incubated for 5 min with vehicle, SKF38393 (3 μM), or SKF38393 in the presence of SP600125 (20 μM) or JNK-IN-8 (10 μM). P-cJun and P-ERK 1/2 were determined by Western blotting (25 and 10 μg of protein were loaded, respectively). Note the reduction of SKF38393-induced P-cJun produced by the two JNK inhibitors (top panels). In contrast, SP600125 and JNK-IN-8 did not affect the increase in P-ERK 1/2 produced by SKF38393 (bottom panels). Summary of data were calculated as percentage of control and are represented as mean ± S.E.M. 1 W ANOVA indicated significant effect of the treatment for both P-cJun (F3,16 = 15.22, p < 0.0001, n = 5 slices from 5 mice) and P-ERK 1/2 (F3,16 =18.23, p < 0.0001, n= 5 slices from mice).
Neurobiol Dis, 2018, 110:37-46. JNK-IN-8 purchased from Selleck.
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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. | |||||||||||||||||||||||
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| Features | JNK-IN-8 and JNK-IN-7 are structurally very similar, but whereas the former is a specific covalent inhibitor of JNKs. | |||||||||||||||||||||||
| Targets |
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| 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] |
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| Cell Data |
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Protocol
Solubility (25°C)
| In vitro | DMSO | 100 mg/mL warmed (197.0 mM) |
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| 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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