rhode-jelly-bean-lip-peptide PKA inhibitor peptides are crucial tools for researchers studying the intricate functions of Protein Kinase A (PKA), a key enzyme in cellular signaling pathways. These synthetic or endogenous peptides act as potent and specific inhibitors, effectively blocking PKA activity.PKI (5-24), PKA Inhibitor Inhibitor (CAS 99534-03-9) By modulating PKA, these peptides allow scientists to dissect its role in various biological processes, from gene regulation to metabolic control. Understanding the properties and applications of PKA inhibitor peptides is essential for advancing research in neuroscience, cell biology, and beyondThe kinase specificity of protein kinase inhibitor peptide.
Protein Kinase A (PKA), also known as cAMP-dependent protein kinase, plays a pivotal role in signal transduction cascades. It is activated by cyclic adenosine monophosphate (cAMP) and phosphorylates a wide array of target proteins, influencing numerous cellular functions. Due to its central role, precise control over PKA activity is vital for cellular homeostasis.ThePKA Inhibitor5-24, also referenced under CAS 99534-03-9, controls the biological activity ofPKA. This small molecule/inhibitoris ... PKA inhibitor peptides, such as the well-characterized PKI (5-24) and PKI (6-22) amide, achieve this control by competitively binding to the catalytic subunit of PKA. This binding interaction effectively prevents PKA from phosphorylating its substrates, thereby inhibiting its downstream effects.
The endogenous inhibitor peptide, PKI, naturally regulates PKA activity. Synthetic analogs, like PKI (5-24), are designed to mimic this natural inhibition, often with enhanced potency and stability.Protein Kinase A Peptides These synthetic peptides are invaluable in laboratory settings, offering a reliable method to study the consequences of PKA inhibition in vitro and in vivoProtein Kinase A-anchoring Inhibitor Peptides Arrest .... Their specificity ensures that observed cellular changes are directly attributable to PKA modulation, minimizing off-target effects.
Several specific PKA inhibitor peptides have emerged as critical research reagents. Among the most prominent are:
* PKI (5-24): This synthetic peptide is a potent, competitive inhibitor of PKA with a low dissociation constant ($K_i$) typically around 2PKI (5-24),PKA Inhibitoris a potent, competitive, syntheticpeptide PKA inhibitor. CAS Number: 99534-03-9. Purity: ≥95%. Molecular Weight: 2222.37..3 nM. It is derived from the pseudosubstrate region of the endogenous PKIProduct Description: 17 residue syntheticpeptide. (TYADFIASGRTGRRNAI-NH2), corresponding to residues 7-23 of both human and mousePKA Inhibitorand 6-22 of .... Its high affinity and specificity make it a standard tool for blocking PKA activity in various experimental models.
* PKI (6-22) amide: This shorter synthetic peptide retains high potency for PKA inhibition, with reported affinities around 1.7-2.5 nMPKA inhibitorfragment (6-22) amide is a syntheticpeptide inhibitor... It is the shortest synthetic PKIpeptidethat retains high potency forPKA inhibition.. It represents the shortest synthetic peptide fragment that effectively inhibits PKA, making it an efficient and cost-effective option for certain research applicationsCyclic Peptides as Protein Kinase Modulators and Their ....
These peptides are often supplied as lyophilized powders, requiring reconstitution for use.What are Protein kinase A (PKA) family inhibitors and how do they ... Their stability and high purity are critical for reproducible experimental results. Researchers select specific PKA inhibitor peptides based on factors such as desired potency, experimental context (e.gPKA Inhibitor., cell permeability requirements), and cost-effectiveness.
The ability of PKA inhibitor peptides to precisely block PKA activity opens up a wide range of research applications.PKA Inhibitor Peptidelyophilized powder, for Neuroscience applications at Sigma-Aldrich. They are instrumental in:
* Elucidating PKA's role in signaling pathways: By inhibiting PKA, researchers can observe downstream effects and identify the specific pathways regulated by this kinase. This is crucial for understanding complex cellular processes like learning and memory, where PKA plays a significant role.PKA Inhibitor
* Studying neuroscience: PKA is involved in synaptic plasticity, long-term potentiation (LTP), and neuronal development.作者：C Liu·2020·被引用次数：72—Protein kinaseinhibitor peptide(PKI) is a potent, heat-stable, and specificPKA inhibitor. It has been demonstrated that PKI can blockPKA-mediated ... PKA inhibitor peptides are used to investigate these processes, for example, by examining how inhibition affects synaptic function or reverses drug tolerance2025年8月10日—TheinhibitionofPKAactivation is essential for the study ofPKAfunctions. Protein kinaseinhibitor peptide(PKI) is a potent, heat-stable, ....
* Investigating cellular functions: From gene expression to metabolic regulation, PKA influences a multitude of cellular activities. Inhibitor peptides allow for the targeted study of PKA's contribution to these functions, aiding in the understanding of diseases associated with PKA dysregulation.
* Developing therapeutic strategies: While primarily research tools, the understanding gained from using PKA inhibitor peptides can inform the development of therapeutic agents targeting diseases where PKA activity is implicated, such as certain cancers or neurological disorders.
When employing PKA inhibitor peptides, several factors are important to consider for successful experimental design and interpretation:
* Specificity: While generally highly specific for PKA, it's important to be aware of potential cross-reactivity with other kinases, especially at very high concentrations or in specific cellular contexts作者：Y Chen·2020—The endogenous protein kinaseinhibitor peptide(PKI) confines the spatial and temporal spread of the activity of protein kinase A (PKA), which ....
* Cell Permeability: Some PKA inhibitor peptides, like the native PKI, are not readily cell-permeant.PKA inhibitorfragment (6-22) amide is apeptide inhibitorof cAMP-dependent protein kinase (PKA). It has a reported affinity of 1.7 nM. For intracellular applications, modified versions (e.g., myristoylated peptides like PKA Inhibitor 14-22 Amide) or cell-penetrating peptides may be necessary to ensure effective delivery into the cell.
* Experimental Conditions: The choice of inhibitor peptide, its concentration, and the duration of exposure should be optimized for the specific experimental system and research question.作者：JT Happ·2021·被引用次数：69—SMO PKIpeptidesalso blockedPKA-C enzymatic activity in vitro, as assessed via aPKA-C substrate phosphorylation assay, with an extended ... Factors such as the concentration of cAMP, the expression levels of PKA, and the presence of other signaling molecules can influence the effectiveness of the inhibitorWhat are Protein kinase A (PKA) family inhibitors and how do they ....
* Purity and Storage: High-purity peptides are essential for reliable results. Proper storage, typically as lyophilized powder at low temperatures, is crucial to maintain peptide integrity and activity.
In conclusion, PKA inhibitor peptides, particularly synthetic analogs like PKI (5-24) and PKI (6-22) amide, are indispensable tools in biological research. Their ability to specifically and potently block PKA activity enables detailed investigation into the enzyme's diverse roles in cellular signaling, providing critical insights into fundamental biological processes and potential therapeutic targets.
Join the newsletter to receive news, updates, new products and freebies in your inbox.