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
Biological ActivityCEP 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Preservation of cholinergic activity and prevention of neuron death by CEP-1347/KT-7515 following excitotoxic injury of the nucleus basalis magnocellularis.
Saporito et al.
Motoneuron apoptosis is blocked by CEP-1347 (KT 7515), a novel inhibitor of the JNK signaling pathway.
Maroney et al.
CEP-1347/KT-7515, an inhibitor of SAPK/JNK pathway activation, promotes survival and blocks multiple events associated with Abeta-induced cortical neuron apoptosis.
Bozyczko-Coyne et al.
Citations for CEP 1347
The citations listed below are publications that use Tocris products. Selected citations for CEP 1347 include:
6 Citations: Showing 1 - 6
The novel MDM4 inhibitor CEP-1347 activates the p53 pathway and blocks malignant meningioma growth in vitro and in vivo.
Authors: Mitobe Et al.
Phosphorylation of mixed lineage kinase MLK3 by cyclin-dependent kinases CDK1 and CDK2 controls ovarian cancer cell division.
Authors: William R Et al.
J Biol Chem 2022;298:102263
MAP4K4 promotes pancreatic tumorigenesis via phosphorylation and activation of mixed lineage kinase 3.
Authors: Daniel R Et al.
Identification of genes required for Enzalutamide resistance in castration-resistant prostate cancer cells in vitro.
Authors: Yajun Et al.
Mol Cancer Ther 2021;20:398-409
WDR62 mediates TNFα-dependent JNK activation via TRAF2-MLK3 axis.
Authors: Prinz Et al.
Mol Biol Cell 2018;29:2470
ARHGEF3 controls HDACi-induced differentiation via RhoA-dependent pathways in acute myeloid leukemias.
Authors: Lucia Et al.
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