Date published: 2026-5-3

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PKI (5-24), PKA Inhibitor Inhibitor (CAS 99534-03-9)

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Alternate Names:
L-threonyl-L-threonyl-L-tyrosyl-L-alanyl-L-a-aspartyl-L-phenylalanyl-L-isoleucyl-L-alanyl-L-serylgl ycyl-L-arginyl-L-threonylglycyl-larginyl-L-aspartic acid
Application:
PKI (5-24), PKA Inhibitor is a potent, competitive, synthetic peptide PKA inhibitor
CAS Number:
99534-03-9
Purity:
≥95%
Molecular Weight:
2222.37
Molecular Formula:
C94H148N32O31
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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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), PKA Inhibitor this is a prominent enzyme-substrate interaction site. PKI (5-24), PKA Inhibitor exhibits a Ki of 2.3 nM with respect to PKA and is an extremely weak inhibitor of cGMP-dependent protein kinase (PKG).


PKI (5-24), PKA Inhibitor Inhibitor (CAS 99534-03-9) References

  1. cGMP signals mainly through cAMP kinase in permeabilized murine aorta.  |  Wörner, R., et al. 2007. Am J Physiol Heart Circ Physiol. 292: H237-44. PMID: 16920816
  2. Structure of a peptide inhibitor bound to the catalytic subunit of cyclic adenosine monophosphate-dependent protein kinase.  |  Knighton, DR., et al. 1991. Science. 253: 414-20. PMID: 1862343
  3. A potent synthetic peptide inhibitor of the cAMP-dependent protein kinase.  |  Cheng, HC., et al. 1986. J Biol Chem. 261: 989-92. PMID: 3511044
  4. Role of cAMP in the reactivation of demembranated ram spermatozoa.  |  San Agustin, JT. and Witman, GB. 1994. Cell Motil Cytoskeleton. 27: 206-18. PMID: 8020107
  5. Phosphotransferase and substrate binding mechanism of the cAMP-dependent protein kinase catalytic subunit from porcine heart as deduced from the 2.0 A structure of the complex with Mn2+ adenylyl imidodiphosphate and inhibitor peptide PKI(5-24).  |  Bossemeyer, D., et al. 1993. EMBO J. 12: 849-59. PMID: 8384554
  6. A cGMP kinase mutant with increased sensitivity to the protein kinase inhibitor peptide PKI(5-24).  |  Ruth, P., et al. 1996. Biol Chem. 377: 513-20. PMID: 8922286
  7. Identification and characterization of cAMP-dependent protein kinase and its possible direct interactions with protein phosphatase-1 in marine dinoflagellates.  |  Dawson, JF., et al. 1996. Biochem Cell Biol. 74: 559-67. PMID: 8960362
  8. Modulation of the cloned skeletal muscle L-type Ca2+ channel by anchored cAMP-dependent protein kinase.  |  Johnson, BD., et al. 1997. J Neurosci. 17: 1243-55. PMID: 9006969
  9. Crystal structure of a polyhistidine-tagged recombinant catalytic subunit of cAMP-dependent protein kinase complexed with the peptide inhibitor PKI(5-24) and adenosine.  |  Narayana, N., et al. 1997. Biochemistry. 36: 4438-48. PMID: 9109651
  10. Regulation of native Kv1.3 channels by cAMP-dependent protein phosphorylation.  |  Chung, I. and Schlichter, LC. 1997. Am J Physiol. 273: C622-33. PMID: 9277360
  11. Identification of protein-protein interfaces by decreased amide proton solvent accessibility.  |  Mandell, JG., et al. 1998. Proc Natl Acad Sci U S A. 95: 14705-10. PMID: 9843953

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

PKI (5-24), PKA Inhibitor, 500 µg

sc-201159
500 µg
$255.00

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.
Answered by: Technical Support
Date published: 2024-07-18
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Rated 5 out of 5 by from Westphal et alWestphal et al. (PubMed ID 10390370) used the PKA inhibitor, PKI (5-24) (PKI), to prevent cAMP from enhancing NMDA currents. -SCBT Publication Review
Date published: 2015-06-07
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PKI (5-24), PKA Inhibitor Inhibitor is rated 5.0 out of 5 by 1.
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