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217505

Sigma-Aldrich

CBP-CREB Interaction Inhibitor

The CBP-CREB Interaction Inhibitor, also referenced under CAS 92-78-4, controls the biological activity of CBP-CREB.

Synonym(e):

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

Empirische Formel (Hill-System):
C17H12ClNO2
CAS-Nummer:
Molekulargewicht:
297.74
UNSPSC-Code:
12352200
NACRES:
NA.77

Qualitätsniveau

Assay

≥97% (HPLC)

Form

solid

Hersteller/Markenname

Calbiochem®

Lagerbedingungen

OK to freeze
protect from light

Farbe

beige

Löslichkeit

DMSO: 100 mg/mL

Versandbedingung

ambient

Lagertemp.

2-8°C

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)

InChIKey

OHAXNCGNVGGWSO-UHFFFAOYSA-N

Allgemeine Beschreibung

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 M, respectively) by directly binding to CBP′s KIX domain (Kd ~8.6 M using a recombinant KIX). Shown to inhibit CRE- (cAMP response element) dependent transcription activity induced by forskolin in a HEK293T-based RLuc reporter assay (IC50<2.5 M), while exhibiting little effect against the KID-independent CREB-VP16 transcription activity. Also reported to inhibit the enzymatic activity of Firefly luciferase (IC50 ~1 M), but not that of RLuc.
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.

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Sonstige Hinweise

Li, B.X. and Xiao, X., 2009. ChemBioChem10, 2721.
Best, J.L., et al. 2004. Proc. Natl. Acad. Sci. USA101, 17622.

Rechtliche Hinweise

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Piktogramme

Exclamation mark

Signalwort

Warning

H-Sätze

Gefahreneinstufungen

Eye Irrit. 2 - Skin Sens. 1B

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 1


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