CEP 1347 - CAS 156177-65-0
Catalog number:
156177-65-0
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C33H33N3O5S2
Molecular Weight:
615.76
COA:
Inquire
Targets:
Amyloid-β
Description:
CEP 1347, also named KT 7515 or CHEMBL290352, is an ethylthiomethyl derivative, is a potent, selective inhibitor of the cJun-amino terminal kinase pathway currently under clinical evaluation for the treatment of neurodegenerative diseases. Blocks Aβ-induced cortical neuron apoptosis (EC50 ~51 nM).
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Brife Description:
Blocks Aβ-induced cortical neuron apoptosis (EC50 ~51 nM)
Appearance:
Pale yellow solid
Synonyms:
CHEMBL290352; CEP-1347; 3,9-Bis(etsm)-K-252a; CEP1347; 156177-65-0; CEP 1347; KT7515; 3,9-Bis((ethylthio)methyl)-K-252a; KT 7515; KT-7515; GTPL8173; SCHEMBL12047710; BDBM24942; CEP1374; CEP 1374; CEP-1374; ZINC3928304; AKOS024458422; KT-1575; 170587-65-2; 9,12-Epoxy-1H-diindolo(1,2,3-fg:3',2',1'-kl)pyrrolo(3,4-i)(1,6)benzodiazocine-10-carboxylic acid, 5,16-bis((ethylthio)methyl)-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, methyl ester, (9S-(9alpha,10beta,12alpha))-; CEP 1347|(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; methyl (15S,16R,18R)-10,23-bis[(ethylsulfanyl)methyl]-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1^{15,18}.0^{2,6}.0^{7,27}.0^{8,13}.0^{19,26}.0^{20,25}]octacosa-1,6,8,10,12,20,22,24,26-nonaene-16-carboxylate;
Solubility:
Soluble to 10 mM in DMSO
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -25℃ for long term (months to years).
MSDS:
Inquire
Application:
Anti-Alzheimer agents; Amyloid-β inhibitor
Density:
1.51 g/cm3
InChIKey:
SCMLRESZJCKCTC-KMYQRJGFSA-N
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
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
1.Pharmacokinetic interactions of CEP-1347 and atazanavir in HIV-infected patients.
Ma Q1, Gelbard HA, Maggirwar SB, Dewhurst S, Gendelman HE, Peterson DR, DiFrancesco R, Hochreiter JS, Morse GD, Schifitto G. J Neurovirol. 2013 Jun;19(3):254-60. doi: 10.1007/s13365-013-0172-z. Epub 2013 Jun 5.
CEP-1347 is a potent inhibitor of mixed lineage kinase (MLK), which was investigated for ameliorating HIV-associated neurocognitive disorders. CEP-1347 and atazanavir pharmacokinetics were determined when CEP-1347 50 mg twice daily was administered to HIV-infected patients (n = 20) receiving combination antiretroviral therapy including atazanavir and ritonavir (ATV/RTV, 300/100 mg) once daily continuously. Co-administration of CEP-1347 and ATV/RTV resulted with significant changes in pharmacokinetics of ATV but not RTV. Specifically, an increase in ATV accumulation ratio of 15 % (p = 0.007) and a prolongation of T(½) from 12.7 to 15.9 h (p = 0.002) were observed. The results suggested that co-administration of CEP-1347 with ATV/RTV in HIV-infected patients might result in limited impact on ATV but not on RTV pharmacokinetics.
2.Targeting mixed lineage kinases in ER-positive breast cancer cells leads to G2/M cell cycle arrest and apoptosis.
Wang L1, Gallo KA, Conrad SE. Oncotarget. 2013 Aug;4(8):1158-71.
Estrogen receptor (ER)-positive tumors represent the most common type of breast cancer, and ER-targeted therapies such as antiestrogens and aromatase inhibitors have therefore been widely used in breast cancer treatment. While many patients have benefited from these therapies, both innate and acquired resistance continue to be causes of treatment failure. Novel targeted therapeutics that could be used alone or in combination with endocrine agents to treat resistant tumors or to prevent their development are therefore needed. In this report, we examined the effects of inhibiting mixed-lineage kinase (MLK) activity on ER-positive breast cancer cells and non-tumorigenic mammary epithelial cells. Inhibition of MLK activity with the pan-MLK inhibitor CEP-1347 blocked cell cycle progression in G2 and early M phase, and induced apoptosis in three ER-positive breast cancer cell lines, including one with acquired antiestrogen resistance. In contrast, it had no effect on the cell cycle or apoptosis in two non-tumorigenic mammary epithelial cell lines.
3.[Therapy of Parkinson's disease--up to date].
Murata M1. Rinsho Shinkeigaku. 2008 Nov;48(11):986-8.
The prognosis of Parkinson's disease (PD) has been improved with developing anti-parkinsonian agents. Recently the re-evaluation of L-dopa and dopamine agonists is the topic in the world based on focusing non motor side effects of dopamine agonists such as sudden uncontrollable somnolence and valvulopathy in place of motor complication. The development of anti-parkinsonian drugs based on the new mechanism has been progressed such as CEP-1347, AAV-neuturin, AAV-GAD, and AAV-DDC. The most reliable new drug is zonisamide which is originally synthesized in Japan for epilepsy. A nation-wide randomized double blind study showed that Zonisamide improves motor function of advanced PD patients. Long-term efficacy was also shown. The mechanism of zonisamide for PD is the increase of dopamine synthesis and moderate inhibition of monoamine oxydase B activity. Inhibitatory effects of sodium channel and T-type calcium channel may also affects. Zonisamide has neuroprotective effects though inhibition of quinoprotein and increasing the levels of GSH and Mn SOD.
4.Mkp1 is a c-Jun target gene that antagonizes JNK-dependent apoptosis in sympathetic neurons.
Kristiansen M1, Hughes R, Patel P, Jacques TS, Clark AR, Ham J. J Neurosci. 2010 Aug 11;30(32):10820-32. doi: 10.1523/JNEUROSCI.2824-10.2010.
Developing sympathetic neurons depend on NGF for survival. When sympathetic neurons are deprived of NGF in vitro, a well documented series of events, including c-Jun N-terminal kinase (JNK) pathway activation, release of cytochrome c from the mitochondria, and caspase activation, culminates in the death of the neuron by apoptosis within 24-48 h. This process requires de novo gene expression, suggesting that increased expression of specific genes activates the cell death program. Using rat gene microarrays, we found that NGF withdrawal induces the expression of many genes, including mkp1, which encodes a MAPK phosphatase that can dephosphorylate JNKs. The increase in mkp1 mRNA level requires the MLK-JNK-c-Jun pathway, and we show that Mkp1 is an important regulator of JNK-dependent apoptosis in sympathetic neurons. In microinjection experiments, Mkp1 overexpression can inhibit JNK-mediated phosphorylation of c-Jun and protect sympathetic neurons from apoptosis, while Mkp1 knockdown accelerates NGF withdrawal-induced death.
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CAS 156177-65-0 CEP 1347

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