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CEP 1347,JNK信号传导抑制剂

JNK信号传导抑制剂
规格或纯度: ≥97%(HPLC)
有货

库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
C287932-1mg
 1mg 期货 Stock Image
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mitogen-activated protein kinase kinase kinase 10 Inhibitor mitogen-activated protein kinase kinase kinase 11 Inhibitor mitogen-activated protein kinase kinase kinase 12 Inhibitor mitogen-activated protein kinase kinase kinase 9 Inhibitor
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基本描述

规格或纯度 ≥97%(HPLC)
英文名称 CEP 1347
别名 (9S,10R,12R)-5-16-Bis [[(ethylthiothiomethylmethyl)]-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-环氧-1H-二吲哚并[1,2,3-fg：3',2',1'-kl]吡咯并[3,4-i] [1,6]苯并重氮辛-10-羧酸甲酯
英文别名 CEP-1347|156177-65-0|CEP 1347|KT7515|3,9-Bis((ethylthio)methyl)-K-252a|KT-7515|CEP1347|200HA2LIMK|CHEMBL290352|KT-1575|methyl (5S,6R,8R)-2,11-bis((ethylthio)methyl)-6-hydroxy-5-methyl-13-oxo-5,6,7,8,14,15-hexahydro-13H-16-oxa-4b,8a,14-triaza-5,8-methanodi
生化机理 c-jun N末端激酶（JNK）信号传导抑制剂。拯救经历凋亡的运动神经元（EC50 = 20 nM）。阻断Aβ诱导的皮质神经元凋亡（EC50?51 nM）。不抑制ERK1活性。具有神经保护作用。
储存温度 -20°C储存
运输条件 超低温冰袋运输

名称和标识符

IUPAC Name methyl (15S,16R,18R)-10,23-bis(ethylsulfanylmethyl)-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8(13),9,11,20(25),21,23,26-nonaene-16-carboxylate
INCHI InChI=1S/C33H33N3O5S2/c1-5-42-15-17-7-9-22-19(11-17)26-27-21(14-34-30(27)37)25-20-12-18(16-43-6-2)8-10-23(20)36-29(25)28(26)35(22)24-13-33(39,31(38)40-4)32(36,3)41-24/h7-12,24,39H,5-6,13-16H2,1-4H3,(H,34,37)/t24-,32+,33+/m1/s1
InChi Key SCMLRESZJCKCTC-KMYQRJGFSA-N
Canonical SMILES CCSCC1=CC2=C(C=C1)N3C4CC(C(O4)(N5C6=C(C=C(C=C6)CSCC)C7=C8CNC(=O)C8=C2C3=C75)C)(C(=O)OC)O
关联CAS 156177-65-0
PubChem CID 9917013
MeSH Entry Terms 3,9-bis((ethylthio)methyl)-K-252a;3,9-bis(EtSM)-K-252a;CEP 1347;CEP-1347;CEP1347;KT 7515;KT-7515;KT7515
分子量 615.76

化学和物理性质

溶解性 溶于DMSO, 最高浓度 (mg/mL): 6.16, 最高浓度(mM): 10

关联配体

Ligand ID 8173
名称 CEP-1347
别名 KT7515
类别 Synthetic organic
学名 4-amino-N-(4,6-dimethylpyrimidin-2-yl)benzenesulfonamide
生物活性评价 CEP-1347 is often descrided as a selective inhibitor of mitogen-activated protein kinase kinase kinase 11 (MLK3), but in fact has inhibitory activity (> 99% inhibition) across all MLKs and a range of additional kinases . The off-targets include leucine-rich repeat kinase 2 (LRRK2), fms-related tyrosine kinase 3 (FLT3), calcium/calmodulin-dependent protein kinase ID (CAMK1D), c-kit receptor tyrosine kinase (KIT) and Aurora kinases A and C .
We have tagged MLK1 as the primary molecular target for this compound for data metrics proposes only, and fully acknowledge its effect on other targets.
评价 CEP-1347 is a semi-synthetic analogue of the natural alkaloid . CEP-1347 was originally identified as a pan-mixed lineage kinase (MLK) family inhibitor . In this setting it inhibits downstream c-jun N-terminal kinase (JNK) activation and has neuroprotective activity .
临床描述 The purpose of this study is to establish safety for CEP-1347 and to determine an efficacious dose in the treatment of Parkinson's disease.
来源公司 Teva Pharmaceutical Industries

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参考文献

1. Conforti P, Ramos C, Apostol BL, Simmons DA, Nguyen HP, Riess O, Thompson LM, Zuccato C, Cattaneo E.  (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):  (1-7).  [PMID:18571429]
2. Apostol BL, Simmons DA, Zuccato C, Illes K, Pallos J, Casale M, Conforti P, Ramos C, Roarke M, Kathuria S et al..  (2008)  CEP-1347 reduces mutant huntingtin-associated neurotoxicity and restores BDNF levels in R6/2 mice..  Mol Cell Neurosci,  39  (1):  (8-20).  [PMID:18602275]
3. Pirvola U, Xing-Qun L, Virkkala J, Saarma M, Murakata C, Camoratto AM, Walton KM, Ylikoski J.  (2000)  Rescue of hearing, auditory hair cells, and neurons by CEP-1347/KT7515, an inhibitor of c-Jun N-terminal kinase activation..  J Neurosci,  20  (1):  (43-50).  [PMID:10627579]
4. Maroney AC, Finn JP, Connors TJ, Durkin JT, Angeles T, Gessner G, Xu Z, Meyer SL, Savage MJ, Greene LA et al..  (2001)  Cep-1347 (KT7515), a semisynthetic inhibitor of the mixed lineage kinase family..  J Biol Chem,  276  (27):  (25302-8).  [PMID:11325962]
5. Harris CA, Deshmukh M, Tsui-Pierchala B, Maroney AC, Johnson Jr EM.  (2002)  Inhibition of the c-Jun N-terminal kinase signaling pathway by the mixed lineage kinase inhibitor CEP-1347 (KT7515) preserves metabolism and growth of trophic factor-deprived neurons..  J Neurosci,  22  (1):  (103-13).  [PMID:11756493]
6. Parkinson Study Group PRECEPT Investigators.  (2007)  Mixed lineage kinase inhibitor CEP-1347 fails to delay disability in early Parkinson disease..  Neurology,  69  (15):  (1480-90).  [PMID:17881719]
7. Saporito MS, Brown EM, Miller MS, Carswell S.  (1999)  CEP-1347/KT-7515, an inhibitor of c-jun N-terminal kinase activation, attenuates the 1-methyl-4-phenyl tetrahydropyridine-mediated loss of nigrostriatal dopaminergic neurons In vivo..  J Pharmacol Exp Ther,  288  (2):  (421-7).  [PMID:9918541]
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