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Submit ReviewCEP 1347
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% (HPLC)
Biological Activity for CEP 1347
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 for CEP 1347
| M. Wt | 615.76 |
| Formula | C33H33N3O5S2 |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 156177-65-0 |
| PubChem ID | 9917013 |
| InChI Key | SCMLRESZJCKCTC-KMYQRJGFSA-N |
| Smiles | O=C(NC8)C1=C8C(C(C=C(CSCC)C=C7)=C7N45)=C4C2=C1C6=C(C=CC(CSCC)=C6)N2[C@H]3C[C@](O)([C@](OC)=O)[C@]5(C)O3 |
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.
Solubility Data for CEP 1347
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 6.16 | 10 |
Preparing Stock Solutions for CEP 1347
The following data is based on the product molecular weight 615.76. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 16.24 mL | 81.2 mL | 162.4 mL |
| 0.5 mM | 3.25 mL | 16.24 mL | 32.48 mL |
| 1 mM | 1.62 mL | 8.12 mL | 16.24 mL |
| 5 mM | 0.32 mL | 1.62 mL | 3.25 mL |
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Product Datasheets for CEP 1347
References for CEP 1347
References are publications that support the biological activity of the product.
Maroney et al (1998) Motoneuron apoptosis is blocked by CEP-1347 (KT 7515), a novel inhibitor of the JNK signaling pathway. J.Neurosci. 18 104 PMID: 9412490
Bozyczko-Coyne et al (2001) CEP-1347/KT-7515, an inhibitor of SAPK/JNK pathway activation, promotes survival and blocks multiple events associated with Abeta-induced cortical neuron apoptosis. J.Neurochem. 77 849 PMID: 11331414
Saporito et al (1998) Preservation of cholinergic activity and prevention of neuron death by CEP-1347/KT-7515 following excitotoxic injury of the nucleus basalis magnocellularis. Neuroscience 86 461 PMID: 9881861
Conforti et al (2008) Blood level of brain-derived neurotrophic factor mRNA is progressively reduced in rodent models of Huntington's disease: Restoration by the neuroprotective compound CEP-1347. Mol.Cell.Neurosci. 39 1 PMID: 18571429
Maroney et al (2001) Cep-1347 (KT7515), a semisynthetic inhibitor of the mixed lineage kinase family. J.Biol.Chem. 276 25302 PMID: 11325962
Mitobe et al (2023) The novel MDM4 inhibitor CEP-1347 activates the p53 pathway and blocks malignant meningioma growth in vitro and in vivo. Biomedicines 11 1967 PMID: 11071967
If you know of a relevant reference for CEP 1347, please let us know.
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Keywords: CEP 1347, CEP 1347 supplier, CEP1347, inhibitors, inhibits, JNK, signaling, Mitogen-Activated, Protein, Kinases, c-Jun, N-Terminal, SAPKs, Stress-Activated, amyloidbeta, amyloidb, amyloidβ, MDM4, p53, meningioma, in, vivo, JNK/c-jun, Amyloid, Beta, Peptides, 4924, Tocris Bioscience
6 Citations for CEP 1347
Citations are publications that use Tocris products. Selected citations for CEP 1347 include:
William R et al (2022) Phosphorylation of mixed lineage kinase MLK3 by cyclin-dependent kinases CDK1 and CDK2 controls ovarian cancer cell division. J Biol Chem 298 102263 PMID: 35843311
Prinz et al (2018) WDR62 mediates TNFα-dependent JNK activation via TRAF2-MLK3 axis. Mol Biol Cell 29 2470 PMID: 30091641
Mitobe et al (2023) The novel MDM4 inhibitor CEP-1347 activates the p53 pathway and blocks malignant meningioma growth in vitro and in vivo. Biomedicines 11 1967 PMID: 11071967
Lucia et al (2014) ARHGEF3 controls HDACi-induced differentiation via RhoA-dependent pathways in acute myeloid leukemias. Epigenetics 10 6-18 PMID: 25494542
Yajun et al (2021) Identification of genes required for Enzalutamide resistance in castration-resistant prostate cancer cells in vitro. Mol Cancer Ther 20 398-409 PMID: 33298586
Daniel R et al (2021) MAP4K4 promotes pancreatic tumorigenesis via phosphorylation and activation of mixed lineage kinase 3. Oncogene 40 6153-6165 PMID: 34511598
Do you know of a great paper that uses CEP 1347 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
MAPK Signaling Scientific Review
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.
Pathways for CEP 1347
