JNK-IN-8

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Cat No.

CEI-1383

Description

JNK-IN-8 is a selective and irreversible type 2 inhibitor of JNK with IC50 value of 4.67 nM, 18.7 nM and 980 pM for JNK1, JNK2 and JNK3, respectively.

Product Overview

JNK-IN-8 is a specific JNK1/2/3 inhibitor with IC50 value of 4.67, 18.7, 0.98 nM respectively. C-Jun N-terminal kinase (JNK) 1, 2 and 3 belong to the mitogen-activated protein kinase (MAPK) family, which are able to phosphorylate c-Jun on the Ser63 and Ser73 residue. They are responsive for stress stimuli, including cytokines and heat shock, and get involved in T cell differentiation and cell apoptosis process. JNK 1 and 2 are ubiquitous in all cell types but JNK 3 is only found in cells of brain, heart and testes tissues. JNK-IN-8 is a JNK1/2/3 inhibitor with high specificity. When JNK-IN-8 was profiled with a panel of 400 kinases, it exhibited specific binding to JNK 1/2/3 but not to other kinases. Crystallization study also found that JNK-IN-8 forms covalent bonds with conserved cysteine residue of JNK 1/2/3, resulting in a conformational change of the activation loop that blocks the substrate binding, thereby inhibiting the activity of JNK 1/2/3.In Hela cells and A375 cells, pretreatment of cells with JNK-IN-8 resulted in the inhibition of c-Jun which is a direct phosphorylation substrate of JNK 1/2/3, confirming the inhibitory action of JNK-IN-8 on JNK 1/2/3.In HEK293-ILR1 cells following stimulation by anisomycin, the JNK-IN-8 was observed to inhibit c-Jun but not MSK1 and p38, and the inhibition was not reversible by removing JNK-IN-8 from culture medium. Additionally, JNK-IN-8 only exhibited on-pathway inhibition of JNK signaling pathway, which can be monitored by the phosphorylation of c-Jun.

CAS_No

1410880-22-6

Molecular Weight

507.59

Purity

0.9991

Storage

Store at -20°C

Targets

JNK

IC50

4.67 nM; 18.7 nM; 980 pM

Molecular Formula

C29H29N7O2

Chemical Name

3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]-N-[3-methyl-4-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide

Solubility

Soluble in DMSO > 10 mM

Shipping Conditions

Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request

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Our Products Cannot Be Used As Medicines Directly For Personal Use.

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