KG-501 (2-naphthol-AS-E-phosphate) is a cAMP response element-binding protein (CREB) inhibitor that disrupts CREB-dependent transcription (Ki = 10 μM) and CREB:CBP interaction (Ki = 50 μM). It also disrupts phospho (Ser-133) CREB binding to KIX with a Ki
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Product Description
Information
KG-501 (2-naphthol-AS-E-phosphate) KG-501 (2-naphthol-AS-E-phosphate) is a cAMP response element-binding protein (CREB) inhibitor that disrupts CREB-dependent transcription (Ki = 10 μM) and CREB:CBP interaction (Ki = 50 μM). It also disrupts phospho (Ser-133) CREB binding to KIX with a Ki of ≈90 μM, using concentrations of CREB that were within the linear range of the binding assay.
Targets
CREB
In vitro
KG-501 inhibits induction of cAMP-responsive genes, at least in part, by blocking the CREB:CBP interaction. The inhibition of the CREB pathway using KG-501, induces an inhibition of neurite outgrowth and synaptogenesis, as well as a decrease of MAP2+ neuronal cells.
In vivo
KG-501 inhibits CREB, CCL2 expression and ERK phosphorylation, also significantly lowers the cAMP level. CREB might contribute to the neuroprotection opposed neuroinflammation through cAMP/ERK adjustment pathway. KG-501 significantly promots the neurological outcomes of AOM-treated mice, reduces phosphorylation of ERK and the concentration of cAMP in cortex.
This compound belongs to the class of organic compounds known as naphthalene-2-carboxanilides. These are naphthalene-2-carboxamides, where the carboxamide group is substituted with an aniline.
External Descriptors
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1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
