Biological ActivityAKAP disruptor. Selectively binds PKA-RI with high affinity (KD values are 6.2 and 12.1 nM for the RIα and β subunits, respectively) and blocks its interaction with AKAP. Inhibits type I PKA-mediated phosphorylation in live cells. Cell permeable.
(Modifications: Leu-1 = NH2-PEG3-CH2-CO-Leu, X = (S)-2-(4-pentenyl)alanine, X-2 and X-6 stapled together with a double bond)
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
PKA-type I selective constrained peptide disruptors of AKAP complexes.
Wang et al.
ACS Chem.Biol., 2015;10:1502
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