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JNK protein kinase inhibitor JNK-IN-8, 5 mg  

JNK protein kinase inhibitor JNK-IN-8, 5 mg

(E)-3-(4-(dimethylamino)but-2-enamido)-N-(3-methyl-4-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl)benzamide

JNK-IN-8 is a remarkably potent and selective irreversible inhibitor of JNK.

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PKI-JNKIN8-005

Availability: within 3 days

175,50 €

Background: JNK-IN-8 is a remarkably potent and selective covalent inhibitor of JNK (IC50 values 4.67 nM, 18.7 nM, and 0.98nM for JNK1/JNK2/JNK3, respectively). JNK-IN-8 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 (EC50 values 486 nM and 338 nM for inhibition of c-Jun phosphorylation in HeLa and A375 cells, respectively), >10-fold selectivity against MNK2, Fms and no inhibition to c-Kit, Met, PDGFRβin A375 cell line. Useful as a pharmacological probe of JNK-dependent signal transduction.

Chemical formula: C29H29N7O2
Molecular weight: 507.59 g/mol
Purity: 98 %
Appearance: Pale-yellow solid
Solubility: Soluble in DMSO
CAS Number: 1410880-22-6

Manufacturer:  Axon Medchem BV

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.  

References

T. Zhang et al. Discovery of potent and selective covalent inhibitors of JNK. Chem. Biol. 2012, 19, 140-154.

Goh ET, et al. Biochem J, 2012, 441(1), 339-346.

Liu Q, et al. Chem Biol, 2013, 20(2), 146-159.

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