JNK-IN-7

Short Summary : Selective JNK inhibitor

Category : MAPK Signaling|JNK

Purity : 0.9823

CAS Number : 1408064-71-0

Formula : C28H27N7O2

Molecular Weight : 493.56

SMILE : CN(C)CC=CC(=O)NC1=CC=CC(=C1)C(=O)NC2=CC=C(C=C2)NC3=NC=CC(=N3)C4=CN=CC=C4

Solubility : >24.7mg/mL in DMSO

Storage : Store at -20°C

Description : JNK-IN-7 is a selective JNK inhibitor with IC50 values of 1.54 nM, 1.99 nM, 0.75 nM to JNK1, JNK2, JNK3, respectively. It also inhibits phosphorylation of c-Jun, which is a direct substrate of JNK kinase. JNK-IN-8, an analog of JNK-IN-7 with an extra flag methyl, dramatically improved in selectivity and eliminated binding to IRAK1, PIK3C3, PIP4K2C and PIP5K3, comparing to JNK-IN-7. JNK-IN-7 and JNK-IN-8 require Cys116 for JNK2 inhibition. JNK-IN-7 can indeed inhibit IRAK-1 dependent E3 ligase activity of pellino, which plays an role in the Toll receptor signaling pathway in cells at relative high compound concentrations (1C10 mM). The IRAK1 inhibitor JNK-IN-7 inhibited the IL-1-stimulated activation of Pellino 1 in IL-1R cells, but not the Pam3CSK4-stimulated activation of Pellino 1 in RAW264.7 macrophages. JNK-IN-7 also suppressed the phosphorylation of c-Jun in Pam3CSK4-stimulated RAW macrophages, but in contrast with IL-1R cells it did not affect the activation of Pellino 1.References:[1]. Zhang T, Inesta-Vaquera F, Niepel M et al. Discovery of potent and selective covalent inhibitors of JNK. Chem Biol. 2012 Jan 27;19(1):140-54. [2]. Goh ET, Arthur JS, Cheung PC et al. Identification of the protein kinases that activate the E3 ubiquitin ligase Pellino 1 in the innate immune system. Biochem J. 2012 Jan 1;441(1):339-46.

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