PKI (5-24), PKA Inhibitor is a potent, competitive, synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase) derived from the active domain of the naturally-occurring heat-stable inhibitor protein PKI. This pseudosubstrate inhibitor peptide mimics the protein substrate by binding to the catalytic site via the arginine-cluster basic subsite, which provides high specificity. PKA catalytic subunit residues Tyr235 and Phe239 form a sandwich-like structure with residue Phe10 of PKI (5-24); this is a prominent enzyme-substrate interaction site. PKI (5-24) exhibits a Ki of 2.3 nM with respect to PKA and is an extremely weak inhibitor of cGMP-dependent protein kinase (PKG).
1. Cheng, H.C., et al. 1986. J. Biol. Chem. 261: 989-992. PMID: 3511044 2. Knighton, D.R., et al. 1991. Science. 253: 414-420. PMID: 1862343 3. Bossemeyer, D., et al. 1993. EMBO J. 12: 849-859. PMID: 8384554 4. Ruth, P., et al. 1996. Biol. Chem. 377: 513-520. PMID: 8922286 5. Narayana, N., et al. 1997. Biochemistry. 36: 4438-4448. PMID: 9109651
Dissolve peptide in distilled water first. The concentration should be high enough to allow for the addition of buffer after the product is dissolved completely.
If necessary, a few drops of dilute acetic acid or ammonium hydroxide can be added to help solubilize the peptide.
The solution can be sonicated briefly to help solubility. For storage, solutions should be in the pH range of 5-7.0, aliquoted and stored at -20°C or lower. Solutions can be stored for approximately 3 to 4 months.
What is the difference between these 2 reagents:
1-PKI (5-24), PKA Inhibitor (CAS 99534-03-9)
2-PKA Inhibitor IV (CAS 99534-03-9)
Asked by: Moustafahamouly
Thank you for your question. There is no difference between these two chemicals. We will look into discontinuing one from our catalog.
Answered by: Technical Support
Date published: 2019-03-10
Is PKA Inhibitor (5-24) membrane permeable?
Asked by: Ivan Goussakov
Thank you for your question. This biochemical is not cell permeable. Please contact Technical Service if you have any further questions or need additional information.
Answered by: Tech Service
Date published: 2018-11-30
Is it cell permeable?
Asked by: ascientist
Thank you for your question. We do not have any data to support this biochemical, PKI (5-24), PKA Inhibitor (CAS 99534-03-9): sc-201159, being cell permeable. We do have a reference in the primary literature which describes how this biochemical can be altered (through conjugation with a peptide) to become cell permeable. If you have more questions about this, please refer to this publication on NCBI's PubMed: PMID: 16761111.
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