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(e): CBP-CREB Interaction Inhibitor, Luciferase Inhibitor III, N-(4-Chlorophenyl)-3-hydroxy-2-naphthamide, KIX-KID Interaction Inhibitor
• Empirische Formel (Hill-System): C₁₇H₁₂ClNO₂
• CAS-Nummer: 92-78-4
• Molekulargewicht: 297.74
• MDL number: MFCD00021639
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥97% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Eigenschaften

• Quality Segment: 100
• 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

Beschreibung

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 (K_d ~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.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Sicherheitshinweise

• Piktogramme: GHS07
• Signalwort: Warning
• Gefahrencodes: H317,H319
• Sicherheitshinweise: P261 - P264 - P272 - P280 - P302 + P352 - P305 + P351 + P338
• Hazard Classifications: Eye Irrit. 2 - Skin Sens. 1B
• Lagerklasse: 11 - Combustible Solids
• Was ist los?: WGK 1