MG CBP-CREB Interaction Inhibit 1PC X 25

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 M, respectively) by directly binding to CBP′s KIX domain (K_d ~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 (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.

Legal Information

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

Other Notes

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

Packaging

250 mg in Glass bottle

Packaged under inert gas

Reconstitution

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

Warning

Toxicity: Standard Handling (A)