Gγ4 Activators
Following the initial HTS, the identified candidate compounds would be subjected to a series of more refined assays to confirm their specificity and direct effect on Gγ4. These secondary assays might include direct binding studies, such as surface plasmon resonance or isothermal titration calorimetry, which can confirm physical interactions between the Gγ4 protein and the candidate activators. Additionally, further biochemical assays would be conducted to determine the precise effect of the compounds on the protein's function. Once a direct interaction is confirmed, detailed structural studies could be performed. Techniques like X-ray crystallography, NMR spectroscopy, or cryo-electron microscopy might be used to determine the three-dimensional structure of the Gγ4 protein in complex with the activator compound, revealing the molecular details of the activation mechanism.
These structural insights could then guide the synthesis of more potent and specific activator molecules, as they would provide precise information about the activator binding sites and any conformational changes in Gγ4 that are induced upon binding. Complementary to these experimental techniques, computational modeling and molecular dynamics simulations would offer predictions about how the activators interact with Gγ4 at the atomic level, which can be crucial for understanding the activation process and for designing improved compounds with greater efficacy in modulating the protein's activity.
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Items 1 to 10 of 11 total
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Forskolin | 66575-29-9 | sc-3562 sc-3562A sc-3562B sc-3562C sc-3562D | 5 mg 50 mg 1 g 2 g 5 g | $76.00 $150.00 $725.00 $1385.00 $2050.00 | 73 | |
Forskolin directly stimulates adenylyl cyclase, leading to increased production of cyclic AMP (cAMP), a second messenger crucial in many biological processes. The elevated cAMP levels activate protein kinase A (PKA), which can phosphorylate various targets, including G protein-coupled receptors (GPCRs). This can enhance the functional activity of Gγ4 by promoting the assembly and function of Gβγ complexes, which play an essential role in GPCR signaling. | ||||||
PMA | 16561-29-8 | sc-3576 sc-3576A sc-3576B sc-3576C sc-3576D | 1 mg 5 mg 10 mg 25 mg 100 mg | $40.00 $129.00 $210.00 $490.00 $929.00 | 119 | |
PMA acts as a diacylglycerol analog to activate PKC isoforms, initiating signaling pathways that can lead to the activation of transcription factors responsible for the upregulation of Gγ4 expression. | ||||||
Crenolanib | 670220-88-9 | sc-364470 sc-364470A | 5 mg 10 mg | $600.00 $1000.00 | ||
GTPγS is a non-hydrolyzable analog of GTP. It binds to G proteins, preventing the hydrolysis of GTP to GDP and thus keeping G proteins in their active state. This prolonged activation can enhance the functional activity of Gγ4 by ensuring it remains associated with Gα subunits, part of the active G protein complex that transduces signals from GPCRs. | ||||||
Retinoic Acid, all trans | 302-79-4 | sc-200898 sc-200898A sc-200898B sc-200898C | 500 mg 5 g 10 g 100 g | $65.00 $319.00 $575.00 $998.00 | 28 | |
Retinoic acid engages with its nuclear receptors to initiate transcriptional events that can stimulate the expression of target genes, possibly including Gγ4, by remodeling chromatin accessibility. | ||||||
Mastoparan | 72093-21-1 | sc-200831 | 1 mg | $97.00 | ||
Mastoparan is a peptide that directly activates G proteins by mimicking the effect of GPCR agonists. It stimulates Gα subunits to exchange GDP for GTP, leading to activation of Gβγ complexes, including those containing Gγ4. This activation can influence various downstream signaling pathways, such as the modulation of ion channels and second messenger systems, thereby enhancing the functional activity of Gγ4. | ||||||
Aluminum Fluoride | 7784-18-1 | sc-291881 sc-291881A | 10 g 50 g | $66.00 $245.00 | ||
Aluminum fluoride acts as a phosphate analog and stabilizes the transition state of GTP hydrolysis, which leads to the activation of G proteins. This can indirectly enhance the functional activity of Gγ4 by promoting the active G protein complex formation, facilitating the transmission of signals from GPCRs. | ||||||
8-Bromoadenosine 3′,5′-cyclic monophosphate | 23583-48-4 | sc-217493B sc-217493 sc-217493A sc-217493C sc-217493D | 25 mg 50 mg 100 mg 250 mg 500 mg | $106.00 $166.00 $289.00 $550.00 $819.00 | 2 | |
8-Bromo-cAMP is a cell-permeable cAMP analog that activates PKA. By stimulating PKA, it can phosphorylate targets involved in GPCR signaling, leading to enhanced functional activity of Gγ4 by promoting the interaction and effectiveness of Gβγ subunits in signaling cascades. | ||||||
Vardenafil | 224785-90-4 | sc-362054 sc-362054A sc-362054B | 100 mg 1 g 50 g | $516.00 $720.00 $16326.00 | 7 | |
Vardenafil is a phosphodiesterase type 5 (PDE5) inhibitor that prevents the breakdown of cAMP and cGMP, leading to their accumulation. This can indirectly enhance the functional activity of Gγ4 by increasing PKA activity, which influences Gβγ subunit signaling, including the Gγ4-containing complexes, in processes such as smooth muscle relaxation and vasodilation. | ||||||
IBMX | 28822-58-4 | sc-201188 sc-201188B sc-201188A | 200 mg 500 mg 1 g | $159.00 $315.00 $598.00 | 34 | |
IBMX is a non-specific inhibitor of phosphodiesterases, enzymes that degrade cAMP and cGMP. By inhibiting these enzymes, IBMX can lead to elevated levels of cAMP and cGMP, enhancing the activation of PKA and PKG, respectively. This can indirectly increase the functional activity of Gγ4 by promoting Gβγ-mediated signaling pathways. | ||||||
Okadaic Acid | 78111-17-8 | sc-3513 sc-3513A sc-3513B | 25 µg 100 µg 1 mg | $285.00 $520.00 $1300.00 | 78 | |
Okadaic acid is a potent inhibitor of protein phosphatases PP1 and PP2A. Inhibition of these phosphatases can lead to increased phosphorylation levels of proteins involved in GPCR signaling, potentially enhancing the activity of Gβγ subunits, including Gγ4, by promoting their role in signal transduction pathways. | ||||||