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CEP 1347
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CEP 1347图片
CAS NO:156177-65-0
包装:1mg
市场价:4469元

产品介绍
CEP 1347 是一种具有神经保护作用的 JNK/SAPK 通路抑制剂。
Cas No.156177-65-0
别名KT7515
化学名(5S,6S,8S)-methyl 2,11-bis((ethylthio)methyl)-5-methyl-13-oxo-6,7,8,13,14,15-hexahydro-5H-16-oxa-4b,8a,14-triaza-5,8-methanodibenzo[b,h]cycloocta[jkl]cyclopenta[e]-as-indacene-6-carboperoxoate
Canonical SMILESO=C([C@@H](C1)[C@]2(C)O[C@@H]1N3C4=C5N2C(C=CC(CSCC)=C6)=C6C5=C(CNC7=O)C7=C4C8=C3C=CC(CSCC)=C8)OOC
分子式C33H33N3O5S2
分子量615.76
溶解度<6.16mg/ml in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

CEP-1347, also called KT 7515, is an inhibitor of the c-Jun N-terminal kinase (JNK) signaling pathway, with an IC50 value for JNK1 activation of 20 ± 2 nM in rat embryonic motoneurons [1].

The JNK pathway, also known as the stress-activated protein kinase (SAPK) pathway, is one of the signaling cascades that mediate the apoptotic death in response to a variety of stressful stimuli. JNK activation by phosphorylation is important for neuronal cell death after injury in vivo and after trophic factor withdrawal in vitro [2].

CEP-1347 induced neuronal survival. JNK1 activity in untreated cell cultures increased approximately fourfold within 24 hr after plating. As early as 15 min after the application of CEP-1347 at 500 nM, the activity of JNK1 sharply decreased to ~50% of control levels. For the next 24 hr, the activity of JNK1 continued to decrease. Cultures rich in motoneurons were grown in the presence of CEP-1347 at increasing concentrations, and the IC50 for JNK1 activity at 22 hr was 21 ± 2 nM, whereas the EC50 for cell survival at 5 d was 20 ± 2 nM [1].

CEP-1347 can affect noise-induced hearing loss. Data showed that hearing thresholds 2 d before noise exposure showed no significant difference between the noise-exposed control and treated group. Hearing threshold shifts in all guinea pigs 2 d after the noise exposure. By day 6 after exposure, threshold shifts were significantly less in the CEP-1347 group than in the noise-exposed control group. By 2 weeks after exposure, the difference between the two groups became more pronounced [2].

References:
[1].  Maroney AC, Glicksman MA, Basma AN, et al. Motoneuron apoptosis is blocked by CEP-1347 (KT 7515), a novel inhibitor of the JNK signaling pathway[J]. The Journal of neuroscience, 1998, 18(1): 104-111.
[2].  Pirvola U, Liang XQ, Virkkala J, et al. Rescue of hearing, auditory hair cells, and neurons by CEP-1347/KT7515, an inhibitor of c-Jun N-terminal kinase activation[J]. The Journal of Neuroscience, 2000, 20(1): 43-50.