Date published: 2025-10-12

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TSR-1 Activators

TSR-1 Activators are a meticulously selected array of chemical compounds that influence cellular signaling pathways, resulting in the enhanced functional activity of TSR-1. Forskolin, by increasing cAMP levels, and Thapsigargin, by raising intracellular calcium levels, both indirectly promote TSR-1's role by activating PKA and calcium-dependent kinases, which are known to phosphorylate substrates that could positively regulate TSR-1 activity. The tyrosine kinase inhibitor Genistein, and sphingolipid Sphingosine-1-phosphate, augment TSR-1's function by reducing phosphorylation-based negative regulation and by initiating positive signaling cascades, respectively. PMA and Epigallocatechin gallate serve to activate PKC or inhibit kinases that would otherwise decrease TSR-1 activity, thereby ensuring an enhancement of its function. LY294002 and Wortmannin, by inhibiting PI3K, diminish negative feedback loops, allowing TSR-1 to maintain or increase its activity.

In addition to these, the p38 MAPK inhibitor SB203580 and the MEK1/2 inhibitor U0126, by attenuating phosphorylation events that would usually downregulate TSR-1, indirectly facilitate its activation. Calcium ionophore A23187 directly heightens calcium signaling, which plays a pivotal role in theactivation of TSR-1 by modulating calcium-dependent processes. Lastly, the broad-spectrum kinase inhibitor Staurosporine has the potential to selectively inhibit kinases that negatively influence TSR-1, thereby indirectly enhancing its activity. Collectively, these TSR-1 Activators exemplify the intricate interplay of cellular signaling where the modulation of various pathways, through phosphorylation, inhibition of kinases, or alteration of intracellular molecule levels, converges to elevate the activity level of TSR-1 without necessitating an increase in its expression or direct stimulation.

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