PKI (5-24), PKA InhibitorA potent, competitive, synthetic peptide PKA inhibitor

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

PKI (5-24), PKA Inhibitor | CAS 99534-03-9 is rated 5.0 out of 5 by 1.
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Synonym: 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: A potent, competitive, synthetic peptide PKA inhibitor
CAS Number: 99534-03-9
Purity: ≥95%
Molecular Weight: 2222.37
Molecular Formula: C94H148N32O31
* Refer to Certificate of Analysis for lot specific data (including water content).
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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); 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).


References

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

Usage :
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.
Physical State :
Solid
Sequence :
Thr-Thr-Tyr-Ala-Asp-Phe-Ile-Ala-Ser-Gly-Arg-Thr-Gly-Arg-Arg-Asn-Ala-Ile-His-Asp
Solubility :
Soluble in water.
Storage :
Store at -20° C
Ki Data :
PKA: Ki= 2.3 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
16131004
MDL Number :
MFCD00133989
SMILES :
CC[C@H](C)[C@@H](C(=O)N[C@@H](CC1=CN=CN1)C(=O)N[C@@H](CC(=O)O)C(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](C(C)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CC3=CC=C(C=C3)O)NC(=O)[C@H](C(C)O)NC(=O)[C@H](C(C)O)N

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Certificate of Analysis

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PKI (5-24), PKA Inhibitor  Product Citations

See how others have used PKI (5-24), PKA Inhibitor. Click on the entry to view the PubMed entry .

Citations 1 to 9 of 9 total

PMID: # 27678415  Zuo, W. et al. 2016. Neuropharmacology.

PMID: # 26593676  Seo, J. et al. 2016. Free Radic. Biol. Med. 90: 133-44.

PMID: # 26537248  Alazami, AM. et al. 2015. Genome Biol. 16: 240.

PMID: # 26283508  Zuo, W. et al. 2015. Addict Biol.

PMID: # 24569881  Arakel, EC. et al. 2014. J. Cell. Sci. 127: 2106-19.

PMID: # 24825897  Kang, Q. et al. 2014. The Journal of biological chemistry. 289: 17480-96.

PMID: # 22796382  Campo, GM. et al. 2012. Matrix Biol. 31: 338-51.

PMID: # 10390370  Westphal, RS. et al. 1999. Science. 285: 93-96.

PMID: # 9632797  Kontos, C.D. et al. 1998. Molecular and cellular biology. 18: 4131-40.

Citations 1 to 9 of 9 total

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: 2018-05-11
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Rated 5 out of 5 by from Westphal et al Westphal 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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