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Submit ReviewCEP 1347
说明： Inhibitor of JNK signaling
化学名： (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
纯度： ≥97% (HPLC)
生物活性 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.
技术数据 for CEP 1347
| 分子量 | 615.76 |
| 公式 | C33H33N3O5S2 |
| 储存 | Store at -20°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for CEP 1347
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 6.16 | 10 |
制备储备液 for CEP 1347
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for CEP 1347
参考文献 for CEP 1347
参考文献是支持产品生物活性的出版物。
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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关键词: 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 篇 CEP 1347 的引用文献
引用文献是使用了 Tocris 产品的出版物。 CEP 1347 的部分引用包括：
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
Lucia et al (2014) ARHGEF3 controls HDACi-induced differentiation via RhoA-dependent pathways in acute myeloid leukemias. Epigenetics 10 6-18 PMID: 25494542
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
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
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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
