217505
CBP-CREB Interaction Inhibitor
The CBP-CREB Interaction Inhibitor, also referenced under CAS 92-78-4, controls the biological activity of CBP-CREB.
Synonym(s):
CBP-CREB Interaction Inhibitor, Luciferase Inhibitor III, N-(4-Chlorophenyl)-3-hydroxy-2-naphthamide, KIX-KID Interaction Inhibitor
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About This Item
Empirical Formula (Hill Notation):
C17H12ClNO2
CAS Number:
Molecular Weight:
297.74
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥97% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
Quality Level
assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
beige
solubility
DMSO: 100 mg/mL
shipped in
ambient
storage temp.
2-8°C
SMILES string
Clc1ccc(cc1)NC(=O)c2cc3c(cc2O)cccc3
InChI
1S/C17H12ClNO2/c18-13-5-7-14(8-6-13)19-17(21)15-9-11-3-1-2-4-12(11)10-16(15)20/h1-10,20H,(H,19,21)
InChI key
OHAXNCGNVGGWSO-UHFFFAOYSA-N
General description
A cell-permeable naphthamide compound that effectively blocks the interaction between the KIX domain of CBP and the KID domain of CREB in HEK293T-based and cell-free Renilla luciferase (RLuc) complementation assays (IC50 = 2.26 and 2.9 µM, respectively) by directly binding to CBP′s KIX domain (Kd ~8.6 µM using a recombinant KIX). Shown to inhibit CRE- (cAMP response element) dependent transcription activity induced by forskolin (Cat. No. 344270) in a HEK293T-based RLuc reporter assay (IC50<2.5 µM), while exhibiting little effect against the KID-independent CREB-VP16 transcription activity. Also reported to inhibit the enzymatic activity of Firefly luciferase (IC50 ~1 µM), but not that of RLuc.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Li, B.X. and Xiao, X., 2009. ChemBioChem10, 2721.
Best, J.L., et al. 2004. Proc. Natl. Acad. Sci. USA101, 17622.
Best, J.L., et al. 2004. Proc. Natl. Acad. Sci. USA101, 17622.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
signalword
Warning
hcodes
Hazard Classifications
Eye Irrit. 2 - Skin Sens. 1B
Storage Class
11 - Combustible Solids
wgk
WGK 1
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