121932-06-7
Chemical Structure
PKA Inhibitor Fragment (6-22) amide
Synonym(s): PKI-(6-22)-amide
- CAS No.: 121932-06-7
- Formula:C80H130N28O24
- Molecular Weight:1868.06
IUPAC Name: (3S,6S,9S,12S,15S,21S,24S,30S,33S,36S,39S,42S,43S)-36-(2-amino-2-oxoethyl)-3-((S)-2-((S)-2-((2S,3R)-2-amino-3-hydroxybutanamido)-3-(4-hydroxyphenyl)propanamido)propanamido)-6-benzyl-9-((S)-sec-butyl)-42-carbamoyl-21,30,33-tris(3-guanidinopropyl)-24-((R)-1-hydroxyethyl)-15-(hydroxymethyl)-12,39,43-trimethyl-4,7,10,13,16,19,22,25,28,31,34,37,40-tridecaoxo-5,8,11,14,17,20,23,26,29,32,35,38,41-tridecaazapentatetracontanoic acid
InChIKey: VAKHFAFLRUNHLQ-PEBJKXEYSA-N
SMILES: CC[C@H](C)[C@@H](C(N)=O)NC([C@H](C)NC([C@H](CC(N)=O)NC([C@H](CCCNC(N)=N)NC([C@H](CCCNC(N)=N)NC(CNC([C@H]([C@H](O)C)NC([C@H](CCCNC(N)=N)NC(CNC([C@H](CO)NC([C@H](C)NC([C@H]([C@@H](C)CC)NC([C@@H](NC([C@H](CC(O)=O)NC([C@H](C)NC([C@@H](NC([C@@H](N)[C@H](O)C)=O)CC1=CC=C(C=C1)O)=O)=O)=O)CC2=CC=CC=C2)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O
Biological Activity: PKA Inhibitor Fragment (6-22) amide is a highly potent and specific competitive inhibitor of PKA, with Ki values of 1.7 nM and 1.6 nM against human and bovine PKA catalytic subunits, respectively. The IC50 of PKA Inhibitor Fragment (6-22) amide targeting bovine PKA is 8.6 nM. PKA Inhibitor Fragment (6-22) amide effectively abolishes PKA activity in mouse brain and spinal cord, and exerts in vivo efficacy via intracerebroventricular administration. PKA Inhibitor Fragment (6-22) amide significantly reverses low-dose morphine analgesic tolerance in mice and blocks photoaffinity labeling of cAMP-dependent protein kinase. PKA Inhibitor Fragment (6-22) amide can be applied to research in fields related to the mechanism of morphine analgesic tolerance and skin wound healing[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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PKA Inhibitor Fragment (6-22) amide | 98.00% | PKA Inhibitor Fragment (6-22) amide is a highly potent and specific competitive inhibitor of PKA, with Ki values of 1.7 nM and 1.6 nM against human and bovine PKA catalytic subunits, respectively. The IC50 of PKA Inhibitor Fragment (6-22) amide targeting bovine PKA is 8.6 nM. PKA Inhibitor Fragment (6-22) amide effectively abolishes PKA activity in mouse brain and spinal cord, and exerts in vivo efficacy via intracerebroventricular administration. PKA Inhibitor Fragment (6-22) amide significantly reverses low-dose morphine analgesic tolerance in mice and blocks photoaffinity labeling of cAMP-dependent protein kinase. PKA Inhibitor Fragment (6-22) amide can be applied to research in fields related to the mechanism of morphine analgesic tolerance and skin wound healing. | ||||||||||||||||||||
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- [1]. Dalton G D, 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)[J]. Neuropharmacology, 2005, 48(5): 648-657.
- [2]. 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;33(6):439-445. [Content Brief]
- [3]. Carmo J, et al. Uvaol Improves the Functioning of Fibroblasts and Endothelial Cells and Accelerates the Healing of Cutaneous Wounds in Mice. Molecules. 2020;25(21):4982. Published 2020 Oct 28. [Content Brief]
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