Date published: 2025-10-11

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Mer Activators

Mer activators are a suite of chemical entities that serve to amplify the activity of the Mer protein through diverse yet specific cellular signaling conduits. Forskolin, by catalyzing an upsurge in intracellular cAMP, activates protein kinase A (PKA), which in turn phosphorylates substrates that can directly augment the activity of Mer signaling pathways. IBMX complements this by inhibiting cAMP degradation, thereby sustaining PKA activation and extending its positive effect on Mer activity. Epigallocatechin gallate contributes to this regulatory tapestry by stalling multiple kinases, thereby diminishing competitive signaling and inadvertently potentiating pathways in which Mer is central. The PI3K inhibitor LY294002 and the MEK inhibitor U0126 manipulate their respective pathways, modulating the signal traffic to favor Mer's involvement, while PMA engages PKC in a similar capacity, further solidifying the influence on Mer's operational sphere.

Continuing this orchestrated chemical symphony, Sphingosine-1-phosphate mobilizes lipid signaling mechanisms that intersect with Mer's domain, subtly enhancing its functional participation. A23187 and Thapsigargin both harness the regulatory potential of intracellular calcium to amplify pathways that Mer is implicated in, with A23187 facilitating calcium influx as an ionophore, and Thapsigargin impeding calcium sequestration by targeting the SERCA pump. SB203580's selective p38 MAPK inhibition redirects the signaling equilibrium, inadvertently fostering an environment conducive to Mer activation. Genistein's tyrosine kinase inhibition relieves Mer pathways from competitive phosphorylation, inadvertently augmenting Mer's activity. Meanwhile, Staurosporine's broad kinase inhibition spectrum might suppress kinases that otherwise temper Mer's pathway engagement, thus indirectly enhancing the functional activity of Mer through a refined mechanism of action.

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