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CEP 1347 - ≥97%(HPLC), high purity , CAS No.156177-65-0, Inhibitor of mitogen-activated protein kinase kinase kinase 10;Inhibitor of mitogen-activated protein kinase kinase kinase 11;Inhibitor of mitogen-activated protein kinase kinase kinase 12;Inhibitor of mitogen-activated protein kinase kinase kinase 9

Item Number
C287932
Grouped product items
SKUSizeAvailabilityPrice Qty
C287932-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$632.90
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Inhibitor of JNK signaling

View related series
Epigenetics JAK JAK/STAT Signaling 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 Protein Tyrosine Kinase/RTK Stem Cell/Wnt

Basic Description

Synonyms(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 | HY-10412 | methyl (15S,16R,18R)-10,23-bis(ethylsulf
Specifications & PurityMoligand™, ≥97%(HPLC)
Biochemical and Physiological MechanismsInhibitor of c-jun N-terminal kinase (JNK) signaling. Rescues motor neurons undergoing apoptosis (EC50= 20 nM). Blocks Aβ-induced cortical neuron apoptosis (EC50~51 nM). Does not inhibit ERK1 activity. Neuroprotective.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of mitogen-activated protein kinase kinase kinase 10;Inhibitor of mitogen-activated protein kinase kinase kinase 11;Inhibitor of mitogen-activated protein kinase kinase kinase 12;Inhibitor of mitogen-activated protein kinase kinase kinase 9

Product Properties

ALogP4.4

Associated Targets(Human)

DLK1 Tchem Protein delta homolog 1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAP3K10 Tchem Mitogen-activated protein kinase kinase kinase 10 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAP3K12 Tchem Mitogen-activated protein kinase kinase kinase 12 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAP3K11 Tchem Mitogen-activated protein kinase kinase kinase 11 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAP3K9 Tchem Mitogen-activated protein kinase kinase kinase 9 (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KIT Tclin Stem cell growth factor receptor (10667 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PRKAA2 Tchem AMP-activated protein kinase, alpha-2 subunit (1328 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RPS6KA1 Tchem Ribosomal protein S6 kinase alpha 1 (2796 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RPS6KA6 Tchem Ribosomal protein S6 kinase alpha 6 (2027 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
FLT1 Tclin Vascular endothelial growth factor receptor 1 (6262 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KDR Tclin Vascular endothelial growth factor receptor 2 (20924 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CAMK2D Tchem CaM kinase II delta (2813 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
FLT4 Tclin Vascular endothelial growth factor receptor 3 (3216 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP3K11 Tchem Mitogen-activated protein kinase kinase kinase 11 (808 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP3K10 Tchem Mitogen-activated protein kinase kinase kinase 10 (401 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NTRK1 Tclin Nerve growth factor receptor Trk-A (7922 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP3K9 Tchem Mitogen-activated protein kinase kinase kinase 9 (945 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CAMK2A Tchem CaM kinase II alpha (1938 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
FLT3 Tclin Tyrosine-protein kinase receptor FLT3 (13481 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AURKC Tchem Serine/threonine-protein kinase Aurora-C (1780 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CAMK1D Tchem CaM kinase I delta (2141 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TNIK Tchem TRAF2- and NCK-interacting kinase (1174 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SH-SY5Y (11521 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRSK2 Tchem BR serine/threonine-protein kinase 2 (1562 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP4K4 Tchem Mitogen-activated protein kinase kinase kinase kinase 4 (2886 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DLK1 Tchem Protein delta homolog 1 (64 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
LRRK2 Tchem Leucine-rich repeat serine/threonine-protein kinase 2 (6390 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PRKD3 Tchem Protein kinase C (PKC) (1010 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Brain (1 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Plasma (328 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

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
Isomeric SMILES CCSCC1=CC2=C(C=C1)N3[C@H]4C[C@@]([C@](O4)(N5C6=C(C=C(C=C6)CSCC)C7=C8CNC(=O)C8=C2C3=C75)C)(C(=O)OC)O
Alternate 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
Molecular Weight 615.76

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 6.16, Max Conc. mM: 10

Related Documents

 SDS

 Specification Sheet

References

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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