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JNK-IN-7 Chemical Structure
|Product name: JNK-IN-7|
|Cat. No.: HY-15617|
JNK-IN-7 is a relatively selective JNKs inhibitor(IC50= 1.54/1.99/0.75 for JNK1/2/3); also bound to IRAK1, PIK3C3, PIP5K3 and PIP4K2C.
IC50 Value: 1.54 nM(JNK1); 1.99 nM (JNK2); 0.75 nM (JNK3)
Covalent modification of IRAK1 by JNK-IN-7 is a possibility and subsequent biochemical kinase assay revealed anIC50 of ~10 nM against IRAK1. JNK-IN-7 exhibited binding inhibition of 95% or more to approximately 14 kinases at the concentration of 1.0 μM. JNK-IN-7 was next tested for its ability to inhibit the enzymatic activity of a panel of 121 kinases at a concentration of 1.0 μM .
|M.Wt||493.56||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||2.0261 mL||10.1305 mL||20.2610 mL|
|5 mM||0.4052 mL||2.0261 mL||4.0522 mL|
|10 mM||0.2026 mL||1.0130 mL||2.0261 mL|
. Zhang, Tinghu, et al. Discovery of Potent and Selective Covalent Inhibitors of JNK. Chemistry & Biology (Oxford, United Kingdom) (2012), 19(1), 140-154.
The mitogen-activated kinases JNK1/2/3 are key enzymes in signaling modules that transduce and integrate extracellular stimuli into coordinated cellular response. Here, we report the discovery of irreversible inhibitors of JNK1/2/3. We describe two JNK3 cocrystal structures at 2.60 and 2.97 ? resoln. that show the compds. form covalent bonds with a conserved cysteine residue. JNK-IN-8 is a selective JNK inhibitor that inhibits phosphorylation of c-Jun, a direct substrate of JNK, in cells exposed to submicromolar drug in a manner that depends on covalent modification of the conserved cysteine residue. Extensive biochem., cellular, and pathway-based profiling establish the selectivity of JNK-IN-8 for JNK and suggests that the compd. will be broadly useful as a pharmacol. probe of JNK-dependent signal transduction. Potential lead compds. have also been identified for kinases, including IRAK1, PIK3C3, PIP4K2C, and PIP5K3.
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