Date published: 2025-9-12

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WCRF Activators

WCRF Activators consist of various chemical entities that enhance the functional activity of WCRF through a series of intracellular signaling events. Forskolin, by elevating intracellular cAMP, activates Protein Kinase A (PKA), which might phosphorylate and activate WCRF or a related regulatory protein that controls WCRF's activity. The same pathway is targeted by 8-Bromo-cAMP and Dibutyryl-cAMP, both analogs of cAMP that penetrate cellular membranes to raise PKA activity, potentially leading to the activation of WCRF. Additionally, Isoproterenol, a beta-adrenergic agonist, increases cAMP levels, indirectly promoting PKA-mediated phosphorylation pathways which could include WCRF activation. Furthermore, the PDE5 inhibitor Sildenafil augments cAMP as well as cGMP levels, which may trigger PKA or PKG to phosphorylate proteins involved in WCRF's activation.

The activity of WCRF is also potentially influenced by modifications in calcium signaling, induced by calcium ionophores like Ionomycin and A23187, which heighten intracellular calcium concentrations and may activate calcium-dependent kinases capable of phosphorylating WCRF. Calcium channel activators such as FPL 64176 and Bay K 8644, likewise, elevate intracellular calcium, leading to the activation of kinases that could target WCRF or associated proteins. Inhibitors of Protein Kinase C (PKC), Bisindolylmaleimide I and Calphostin C, through selective inhibition of PKC isoforms, might paradoxically enhance WCRF activity if WCRF is controlled by PKC-mediated phosphorylation. This collection of compounds, each modulating distinct signaling pathways, converges on the activation of WCRF, thereby amplifying its functional role within the cell.

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