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 |
|---|---|---|---|---|---|---|
Rottlerin | 82-08-6 | sc-3550 sc-3550B sc-3550A sc-3550C sc-3550D sc-3550E | 10 mg 25 mg 50 mg 1 g 5 g 20 g | $82.00 $163.00 $296.00 $2050.00 $5110.00 $16330.00 | 51 | |
Rottlerin is a selective inhibitor of PKC beta, characterized by its unique ability to disrupt specific protein interactions within signaling pathways. It preferentially targets the regulatory domain of PKC beta, leading to altered conformational states that affect enzyme activity. This compound exhibits distinct binding kinetics, allowing for a nuanced modulation of phosphorylation processes. Its interactions with lipid bilayers further influence membrane-associated signaling, highlighting its role in cellular communication. | ||||||
Enzastaurin | 170364-57-5 | sc-364488 sc-364488A sc-364488B | 10 mg 50 mg 200 mg | $254.00 $600.00 $1687.00 | 3 | |
Enzastaurin is an available small molecule inhibitor that targets PKC β. It has shown promise in research studies for its potential anticancer effects and has been investigated in research models for various cancer types. | ||||||
Bisindolylmaleimide VIII | 138516-31-1 | sc-24005 | 1 mg | $47.00 | 6 | |
Bisindolylmaleimide VIII is a potent inhibitor of PKC beta, distinguished by its ability to selectively bind to the ATP-binding site of the enzyme. This interaction stabilizes a closed conformation, effectively blocking substrate access and altering downstream signaling cascades. Its unique structure facilitates specific hydrogen bonding and hydrophobic interactions, enhancing its selectivity. Additionally, the compound's influence on protein-protein interactions can modulate cellular responses, underscoring its role in fine-tuning signal transduction pathways. | ||||||
Gö 6983 | 133053-19-7 | sc-203432 sc-203432A sc-203432B | 1 mg 5 mg 10 mg | $103.00 $293.00 $465.00 | 15 | |
Gö 6983 is a selective inhibitor of PKC beta, characterized by its unique ability to disrupt the enzyme's activity through competitive inhibition at the ATP-binding site. This compound exhibits distinct molecular interactions, including specific van der Waals forces and electrostatic interactions, which enhance its binding affinity. By altering the conformational dynamics of PKC beta, Gö 6983 effectively modulates downstream signaling pathways, influencing cellular processes and responses. | ||||||
Ro 31-8220 | 138489-18-6 | sc-200619 sc-200619A | 1 mg 5 mg | $90.00 $240.00 | 17 | |
Ro 31-8220 is a potent inhibitor of PKC beta, distinguished by its selective binding to the enzyme's regulatory domain. This compound engages in unique hydrogen bonding and hydrophobic interactions, stabilizing a conformation that impedes PKC beta's activation. Its kinetic profile reveals a rapid onset of inhibition, significantly affecting the phosphorylation of target substrates. By modulating the enzyme's activity, Ro 31-8220 intricately influences various signaling cascades within the cell. | ||||||
LY-333,531 Hydrochloride | 169939-93-9 | sc-364215 sc-364215A | 1 mg 5 mg | $92.00 $281.00 | 6 | |
LY333531 is another small molecule inhibitor of PKC β. It may help in managing diabetic nephropathy and other diabetes-related issues. | ||||||
Bisindolylmaleimide I (GF 109203X) | 133052-90-1 | sc-24003A sc-24003 | 1 mg 5 mg | $103.00 $237.00 | 36 | |
Bisindolylmaleimide I (GF 109203X) is a selective inhibitor of PKC beta, characterized by its ability to disrupt the enzyme's catalytic activity through specific interactions with its active site. This compound exhibits a unique mechanism of action, where it alters the conformational dynamics of PKC beta, leading to a decrease in substrate phosphorylation rates. Its distinct binding affinity and kinetic properties allow for precise modulation of intracellular signaling pathways, impacting cellular responses. | ||||||
Bisindolylmaleimide I, HCl | 176504-36-2 | sc-24004 | 1 mg | $145.00 | 13 | |
Bisindolylmaleimide I, HCl is a potent inhibitor of PKC beta, distinguished by its unique ability to engage in specific hydrogen bonding and hydrophobic interactions within the enzyme's active site. This compound influences the allosteric regulation of PKC beta, effectively modulating its conformational states. The resulting changes in enzyme dynamics lead to altered phosphorylation cascades, providing a nuanced control over various cellular signaling networks. Its selective binding profile enhances its efficacy in targeting specific pathways. | ||||||
DAPH-7 | 145915-60-2 | sc-200699 | 1 mg | $71.00 | 1 | |
DAPH-7 is a potent and selective PKC β inhibitor that has been investigated in research studies for its role in attenuating diabetic complications and inflammation. | ||||||
Gö 6976 | 136194-77-9 | sc-221684 | 500 µg | $223.00 | 8 | |
Gö 6976 is a selective inhibitor of PKC beta, characterized by its unique ability to disrupt the enzyme's phosphorylation activity through competitive binding. This compound exhibits distinct molecular interactions, including π-π stacking and van der Waals forces, which stabilize its binding within the active site. By altering the enzyme's kinetic parameters, Gö 6976 effectively modulates downstream signaling pathways, influencing cellular responses and regulatory mechanisms. Its specificity allows for targeted intervention in complex biochemical networks. | ||||||