CEP 1347

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CEP 1347 | CAS No. 156177-65-0 | JNK/c-jun Inhibitors
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Description: Inhibitor of JNK signaling

Chemical Name: (9S,10R,12R)-5-16-Bis[(ethylthio)methyl]-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester

Purity: ≥97%

Product Details
Citations (6)

Biological Activity

CEP 1347 is a potent inhibitor of mixed lineage kinases MLK3, MLK1 and MLK2 (IC50 values in vitro are 23-39 nM, 38-61 nM and 51-82 nM, respectively), and blocks downstream c-jun N-terminal kinase (JNK) activation (IC50 = 20 nM). CEP 1347 rescues motor neurons undergoing apoptosis (EC50 = 20 nM), blocks Aβ-induced cortical neuron apoptosis (EC50 ~51 nM) and, in an animal model of Huntington's disease, restores BDNF mRNA to wild type levels. CEP 1347 is also a MDM4 inhibitor. It displays inhibition of malignant meningioma cells growth in vitro, and shows anti-tumor activity in a mouse xenograft model of meningioma in vivo. CEP 1347 is orally bioavailable and brain penetrant.

Technical Data

Soluble to 10 mM in DMSO
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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Citations for CEP 1347

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