Description
666-15 is a potent and selective inhibitor of cyclic adenosine monophosphate response element binding protein (CREB)-mediated gene transcription with an IC₅₀ of 81 nM. The IC₅₀ values for inhibiting the growth of A549, MCF-7, MDA-MB-231, MDA-MB-468 cell lines are 0.47 μM, 0.31 μM, 0.073 μM, 0.046 μM respectively. It is a weak inhibitor of CREB-CBP (CREB-binding protein) interaction with an IC₅₀ of 18.27 μM. Intraperitoneal injection of 666-15 at 10 mg/kg/day, 5 days per week for 5 weeks suppresses tumor growth in an in vivo MDA-MB-468 xenograft model.
666-15 is a potent and selective inhibitor of cyclic adenosine monophosphate response element binding protein (CREB)-mediated gene transcription with an IC₅₀ of 81 nM. The IC₅₀ values for inhibiting the growth of A549, MCF-7, MDA-MB-231, MDA-MB-468 cell lines are 0.47 μM, 0.31 μM, 0.073 μM, 0.046 μM respectively. It is a weak inhibitor of CREB-CBP (CREB-binding protein) interaction with an IC₅₀ of 18.27 μM. Intraperitoneal injection of 666-15 at 10 mg/kg/day, 5 days per week for 5 weeks suppresses tumor growth in an in vivo MDA-MB-468 xenograft model.
Alternate Name/Synonyms: 3-(3-aminopropoxy)-N-[2-[3-[(4-chloro-2-hydroxyphenyl)carbamoyl]naphthalen-2-yl]oxyethyl]naphthalene-2-carboxamide, hydrochloride; 3-(3-Aminopropoxy)-N-(2-((3-((4-chloro-2-hydroxyphenyl)carbamoyl)naphthalen-2-yl)oxy)ethyl)-2-naphthamide hydrochloride; CREB 666-15; CREB Inhibitor; CBP-CREB Interaction Inhibitor II; Compound 3i
Appearance: Solid
Formulation:
CAS Number: 1433286-70-4
Structure Available?: True
Peptide sequence:
Salt Form: True
Molecular Formula: C₃₃H₃₁Cl₂N₃O₅
Molecular Weight: 620.52
Cell-Permeable?: True
Purity: 98.65%
Solubilities: ~30 mg/ml in in DMSO
Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
Country of Origin: USA
Tag Line: A potent CREB inhibitor
MDL Number:
PubChem CID: 71566396
SMILES: C1=CC=C2C=C(C(=CC2=C1)C(=O)NCCOC3=CC4=CC=CC=C4C=C3C(=O)NC5=C(C=C(C=C5)Cl)O)OCCCN.Cl
InChi: InChI=1S/C33H30ClN3O5.ClH/c34-25-10-11-28(29(38)20-25)37-33(40)27-17-22-7-2-4-9-24(22)19-31(27)42-15-13-36-32(39)26-16-21-6-1-3-8-23(21)18-30(26)41-14-5-12-35;/h1-4,6-11,16-20,38H,5,12-15,35H2,(H,36,39)(H,37,40);1H
InChi Key: LELLCPHHYHLWBH-UHFFFAOYSA-N
Additional Information
Storage Condition: |
-20ºC |
Shipping Condition: |
RT |
Shelf Life: |
36months |