PKA Inhibitor Fragment (6-22) amide

Names

[ CAS No. ]:
121932-06-7

[ Name ]:
PKA Inhibitor Fragment (6-22) amide

[Synonym ]:
Protein Kinase A Inhibitor Fragment 6-22 amide
PKA inhibitor fragment (6-22) amide
MFCD00133792

Biological Activity

[Description]:

PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice[1][2].

[Related Catalog]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PKA

Signaling Pathways >> Stem Cell/Wnt >> PKA

Research Areas >> Neurological Disease

[Target]

PKA:2.8 nM (Ki)

[References]

[1]. Katz BM, et, al. Synthesis, characterization and inhibitory activities of (4-N3[3,5-3H]Phe10)PKI(6-22)amide and its precursors: photoaffinity labeling peptides for the active site of cyclic AMP-dependent protein kinase. Int J Pept Protein Res. 1989 Jun;33(6):439

[2]. Dalton GD, et, al. Alterations in brain Protein Kinase A activity and reversal of morphine tolerance by two fragments of native Protein Kinase A inhibitor peptide (PKI). Neuropharmacology. 2005 Apr; 48(5): 648-57.

Chemical & Physical Properties

[ Molecular Formula ]:
C₈₀H₁₃₀N₂₈O₂₄

[ Molecular Weight ]:
1868.06000

[ Exact Mass ]:
1866.98000

[ PSA ]:
881.72000

[ Storage condition ]:
−20°C

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

Articles

Protein kinase inhibitor-(6-22)-amide peptide analogs with standard and nonstandard amino acid substitutions for phenylalanine 10. Inhibition of cAMP-dependent protein kinase.

J. Biol. Chem. 264 , 14579, (1989)

The minimal structure in the heat-stable inhibitor protein of cAMP-dependent protein kinase required for a low nanomolar potency of inhibition is the peptide Thr6-Tyr-Ala-Asp-Phe-Ile-Ala-Ser-Gly-Arg-T...