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Description: Potent and selective CREB inhibitor
Chemical Name: 3-(3-Aminopropoxy)-N-[2-[[3-[[(4-chloro-2-hydroxyphenyl)amino]carbonyl]-2-naphthalenyl]oxy]ethyl]-2-naphthalenecarboxamide hydrochloride
Purity: ≥98% (HPLC)
Biological Activity
Potent and selective CREB inhibitor (IC50 = 81 nM). Inhibits cancer cell growth, without harming normal cells (up to 1 μM). Completely suppresses tumor growth in a breast cancer xenograft model.
Compound Libraries
666-15 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 620.52 |
| Formula | C33H30ClN3O5.HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1433286-70-4 |
| PubChem ID | 71566396 |
| InChI Key | LELLCPHHYHLWBH-UHFFFAOYSA-N |
| Smiles | NCCCOC1=CC2=CC=CC=C2C=C1C(NCCOC3=C(C(NC4=CC=C(Cl)C=C4O)=O)C=C(C=CC=C5)C5=C3)=O.Cl |
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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 62.05 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 620.52. 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.61 mL | 8.06 mL | 16.12 mL |
| 5 mM | 0.32 mL | 1.61 mL | 3.22 mL |
| 10 mM | 0.16 mL | 0.81 mL | 1.61 mL |
| 50 mM | 0.03 mL | 0.16 mL | 0.32 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Xie et al (2015) Identification of a potent inhibitor of CREB-mediated gene transcription with efficacious in vivo anticancer activity J.Med.Chem. 58 5075 PMID: 26023867
Li et al (2016) Systemic inhibition of CREB is well-tolerated in vivo. Sci.Rep. 6 34513 PMID: 27694829
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Keywords: 666-15, 666-15 supplier, cyclic, adenosine, monophosphate, cAMP, response, element, binding, protein, CREB, inhibitors, inhibits, breast, cancer, potent, selective, Other, Transcription, Factors, 5661, Tocris Bioscience
5 Citations for 666-15
Citations are publications that use Tocris products. Selected citations for 666-15 include:
O'Reilly et al (2019) Nutritionally Derived Metabolic Cues Typical of the Obese Microenvironment Increase Cholesterol Efflux Capacity of Adipose Tissue Macrophages. Mol Nutr Food Res 63 e1800713 PMID: 30411491
Phua (2017) Angiopoietin-like 4 mediates colonic inflammation by regulating chemokine transcript stability via tristetraprolin. Sci Rep 7 44351 PMID: 28287161
Zhou et al (2019) Microglia Are Indispensable for Synaptic Plasticity in the Spinal Dorsal Horn and Chronic Pain. Cell Rep 27 3844 PMID: 31242418
Hamnett et al (2019) Vasoactive intestinal peptide controls the suprachiasmatic circadian clock network via ERK1/2 and DUSP4 signalling. Nat Commun 10 542 PMID: 30710088
Kleiner et al (2018) Activator protein-1 contributes to the NaCl-induced expression of VEGF and PlGF in RPE cells. Mol Vis 24 647 PMID: 30310263
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Reviews for 666-15
Average Rating: 5 (Based on 1 Review.)
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creb inhibitor.
By
Anonymous on 05/02/2018
Species: Mouse
Cell Line/Tissue: pancreatic cancer cell
drug treatment with different conc from 1nm-5um