CEP 1347

Pricing Availability   Qty
Description: Inhibitor of JNK signaling
Chemical Name: (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
Purity: ≥97% (HPLC)
Datasheet
Citations (6)
Reviews
Literature (1)
Pathways (1)

Biological Activity 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.

Technical Data for CEP 1347

M. Wt 615.76
Formula C33H33N3O5S2
Storage Store at -20°C
Purity ≥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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for CEP 1347

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 6.16 10

Preparing Stock Solutions for CEP 1347

The following data is based on the product molecular weight 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 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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Product Datasheets for CEP 1347

Certificate of Analysis / Product Datasheet
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View Related Products by Product Action

View all JNK/c-Jun Inhibitors

Keywords: 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 Citations for CEP 1347

Citations are publications that use Tocris products. Selected citations for CEP 1347 include:

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

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


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


MAPK Signaling Scientific Review

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

MAPK Signaling Pathway

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.