RI-STAD 2

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Cat.No. 6567 - RI-STAD 2 | NH2-PEG3-CH2-CO-Leu-[(S)-2-(4-pentenyl)alanine]-Gln-Tyr-Ala-[(S)-2-(4-pentenyl)alanine]-Gln-Leu-Ala-Asp-Gln-Ile-Ile-Lys-Glu-Ala-Thr-Glu-Lys (double bond covalent bridge: X-2-X-6)
Description: AKAP disruptor; selectively binds PKA-RI with high affinity and blocks its interaction with AKAP; cell permeable
Datasheet
Citations
Reviews
Literature

Biological Activity

AKAP 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.

Technical Data

M. Wt 2401.75
Formula C109H181N25O35
Sequence LXQYAXQLADQIIKEATEK

(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)

Storage Store at -20°C
Smiles O=C(N[C@@H](CCC(N)=O)C(N[C@@H](CC(C)C)C(N[C@@H](C)C(N[C@@H](CC(O)=O)C(N[C@@H](CCC(N)=O)C(N[C@@H]([C@@H](C)CC)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CCCCN)C(N[C@@H](CCC(O)=O)C(N[C@@H](C)C(N[C@@H]([C@H](O)C)C(N[C@@H](CCC(O)=O)C(N[C@@H](CCCCN)C(O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@](CCC/C=C/CCC[C@](NC([C@H](CC(C)C)NC(COCCOCCOCCN)=O)=O)(C(N[C@@H](CCC(N)=O)C(N[C@@H](CC1=CC=C(C=C1)O)C(N[C@H]2C)=O)=O)=O)C)(NC2=O)C

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.

Solubility Data

Solubility Soluble to 1 mg/ml in 50% acetonitrile / water

References

References are publications that support the biological activity of the product.

Wang et al (2015) PKA-type I selective constrained peptide disruptors of AKAP complexes. ACS Chem.Biol. 10 1502 PMID: 25765284


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Keywords: RI-STAD 2, RI-STAD 2 supplier, RI-STAD2, stapled, peptide, selective, AKAP, disruptors, disrupts, a-kinase, anchoring, proteins, RI, PKA, protein, kinase, A, A-kinase-anchoring, protiens, Stapled, Peptides, 6567, Tocris Bioscience

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Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.