PKC beta Inhibitors
PKC β inhibitors are a subset of compounds belonging to the broader class of protein kinase C (PKC) inhibitors. These inhibitors specifically target and modulate the activity of PKC β isoforms within cells. PKC β isoforms are members of the PKC family of serine/threonine kinases, which play a crucial role in signal transduction pathways that regulate various cellular processes. The inhibition of PKC β involves the disruption of its enzymatic activity, which is responsible for phosphorylating target proteins and initiating downstream signaling cascades. This class of inhibitors exerts its effects by binding to specific regions of PKC β, leading to conformational changes that hinder its catalytic activity. Structurally, PKC β inhibitors possess diverse chemical backbones, often characterized by heterocyclic rings and functional groups that are designed to interact with key amino acid residues within the active site of the kinase. These inhibitors can be categorized into different subclasses based on their chemical structures and modes of binding. While some PKC β inhibitors compete with ATP for binding to the kinase's active site, others operate through allosteric mechanisms, disrupting the kinase's ability to interact with its substrates or co-factors.
Understanding the structural and mechanistic details of PKC β inhibitors is essential for the development of targeted interventions, as these inhibitors can modulate cellular processes related to cell growth, differentiation, and signaling. However, the focus of this description is solely on the chemical class itself. By elucidating the interactions between PKC β inhibitors and their target enzyme, researchers aim to advance our understanding of cellular signaling pathways and contribute to the development of novel tools for investigating fundamental biological processes.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
PKC-412 | 120685-11-2 | sc-200691 sc-200691A | 1 mg 5 mg | $52.00 $114.00 | 10 | |
PKC-412 is a potent inhibitor of PKC beta, distinguished by its ability to interfere with the enzyme's catalytic function through allosteric modulation. This compound engages in specific hydrogen bonding and hydrophobic interactions, enhancing its affinity for the enzyme's regulatory domain. By altering conformational dynamics, PKC-412 influences the enzyme's activity and downstream signaling cascades, providing a nuanced approach to modulating cellular processes and interactions within signaling networks. | ||||||
PP242 | 1092351-67-1 | sc-301606A sc-301606 | 1 mg 5 mg | $57.00 $172.00 | 8 | |
PP242 is a selective inhibitor of PKC beta, characterized by its unique binding affinity that disrupts the enzyme's active site through competitive inhibition. This compound exhibits distinct molecular interactions, including π-π stacking and van der Waals forces, which stabilize its complex with PKC beta. By modulating the enzyme's phosphorylation state, PP242 effectively alters signal transduction pathways, impacting cellular responses and regulatory mechanisms within the cell. | ||||||
Hispidin | 555-55-5 | sc-203998 | 5 mg | $416.00 | ||
Hispidin acts as a modulator of PKC beta, showcasing a unique ability to influence enzyme conformation through allosteric interactions. Its structural features facilitate specific hydrogen bonding and hydrophobic interactions, enhancing its binding efficacy. This compound alters the kinetics of phosphorylation events, leading to nuanced changes in downstream signaling cascades. Hispidin's distinct molecular dynamics contribute to its role in regulating cellular processes, emphasizing its intricate biochemical behavior. | ||||||
PKCβ Inhibitor | 257879-35-9 | sc-204199 | 500 µg | $312.00 | 1 | |
PKCβ Inhibitor selectively targets the PKC beta isoform, exhibiting a unique binding affinity that disrupts its catalytic activity. This compound engages in specific electrostatic interactions, stabilizing a conformation that inhibits substrate access. Its kinetic profile reveals a competitive inhibition mechanism, altering the phosphorylation landscape within cells. The inhibitor's distinct molecular architecture allows for tailored interactions with the enzyme's active site, influencing signal transduction pathways. | ||||||
UCN-02 | 121569-61-7 | sc-202377 sc-202377A sc-202377B | 500 µg 1 mg 5 mg | $220.00 $400.00 $1600.00 | 1 | |
UCN-02 acts as a selective inhibitor of PKC beta, showcasing a remarkable ability to modulate enzyme dynamics through unique allosteric interactions. By binding to a specific site, it induces conformational changes that hinder substrate binding and enzymatic activity. Its reaction kinetics suggest a non-competitive inhibition model, effectively altering downstream signaling cascades. The compound's structural features facilitate precise interactions with the enzyme, impacting cellular regulatory mechanisms. | ||||||
Ro-31-8220 in solution | 138489-18-6 | sc-358721 | 1 mg | $106.00 | 2 | |
Ro-31-8220 is a potent inhibitor of PKC beta, characterized by its ability to disrupt protein-protein interactions essential for kinase activation. This compound exhibits a unique binding affinity that stabilizes an inactive conformation of the enzyme, thereby impeding its catalytic function. Its kinetic profile indicates a mixed inhibition mechanism, influencing the phosphorylation of target substrates and altering cellular signaling pathways. The compound's hydrophobic regions enhance its interaction with lipid membranes, further modulating PKC beta activity. | ||||||
Sotrastaurin | 425637-18-9 | sc-474229 sc-474229A | 5 mg 10 mg | $300.00 $540.00 | ||
Sotrastaurin is an active PKC inhibitor with selectivity for PKC β. It has been studied in research models for immunosuppressive and anti-inflammatory effects in autoimmune diseases and transplant rejection. | ||||||
UCN-01 | 112953-11-4 | sc-202376 | 500 µg | $251.00 | 10 | |
UCN-01 is a selective inhibitor of PKC beta, notable for its ability to interfere with the enzyme's regulatory domains, leading to altered conformational dynamics. This compound engages in specific hydrogen bonding interactions that stabilize a non-active state, effectively reducing substrate phosphorylation rates. Its unique structural features allow for enhanced solubility in cellular environments, facilitating its penetration into lipid bilayers and impacting downstream signaling cascades. | ||||||
Ruboxistaurin-d6 Hydrochloride | 169939-93-9 (unlabeled) | sc-491936 | 10 mg | $11000.00 | ||
Ruboxistaurin-d6 Hydrochloride acts as a selective modulator of PKC beta, characterized by its unique ability to disrupt protein-protein interactions within the kinase domain. This compound exhibits distinct kinetic properties, influencing the phosphorylation cascade by altering enzyme activation thresholds. Its isotopic labeling enhances tracking in metabolic studies, providing insights into cellular signaling pathways. Additionally, its hydrophilic nature promotes interaction with membrane-associated proteins, affecting cellular localization and function. | ||||||
Parthenolide | 20554-84-1 | sc-3523 sc-3523A | 50 mg 250 mg | $81.00 $306.00 | 32 | |
While not a specific PKC β inhibitor, parthenolide is a natural compound found in feverfew (Tanacetum parthenium) and has been shown to inhibit PKC β activity, among other signaling pathways. It has been studied for its potential anti-cancer and anti-inflammatory effects. | ||||||