EML5 Activators
EML5 activators encompass an array of chemical compounds that facilitate the enhancement of EML5's activity by indirectly influencing the microtubule stability and dynamics within cells. Forskolin, for instance, raises intracellular cAMP levels, which in turn activates PKA; this kinase can phosphorylate substrates that may interact with EML5, thus boosting its role in microtubule network stabilization. Similarly, PMA, as a PKC activator, and EGCG, through kinase inhibition, orchestrate a cellular environment conducive to the enhanced activity of EML5 by modifying the phosphorylation status of proteins that interact with microtubules. The bioactive lipid sphingosine-1-phosphate triggers a cascade via G-protein-coupled receptors, culminating in the activation of kinases like ERK and Akt, which could offer a conducive signaling milieu for EML5 activity related to microtubule dynamics. In conjunction with these, LY294002 and Wortmannin, both PI3K inhibitors, along with U0126, a MEK inhibitor, and SB203580, a p38 MAPK inhibitor, collectively contribute to the fine-tuning of intracellular signaling pathways. This modulation can reduce phosphorylation events that negatively influence EML5, facilitating an increase in its microtubule-stabilizing behavior.
The second set of EML5 activators includes compounds that alter cellular ion balance and protein interactions, further enriching the functional spectrum of EML5 in cytoskeletal dynamics. Thapsigargin, by impairing calcium sequestration, leads to an upsurge in cytosolic calcium, which activates calcium-dependent kinases, potentially bolstering EML5's engagement with microtubules. A23187, another agent that elevates intracellular calcium, may similarly orchestrate the activation of EML5 through calcium-dependent signaling pathways. Staurosporine, although a broad-spectrum kinase inhibitor, might paradoxically enhance EML5 activity by mitigating the suppressive phosphorylation exerted by specific kinases on microtubule-associated processes where EML5 is a pivotal player. Lastly, zoledronic acid disrupts protein prenylation, thereby potentially alleviating competitive or regulatory protein interactions that affect EML5's functionality in microtubule support. These compounds, through their distinct yet interconnected pathways, synergistically enhance the microtubule-associated activity of EML5 without necessitating direct upregulation or conformational activation of the protein itself.
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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 activates adenylate cyclase, thereby increasing the levels of cAMP in the cell. Elevated cAMP levels activate PKA, which can then phosphorylate various target proteins, including those that may interact with EML5, leading to its enhanced functional activity within the cellular microtubule network. | ||||||
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 is a potent activator of protein kinase C (PKC), which can phosphorylate a wide range of target proteins. PKC-mediated phosphorylation events could alter the binding affinity of EML5 to microtubules or regulatory factors, thus enhancing its activity in stabilizing microtubule dynamics. | ||||||
(−)-Epigallocatechin Gallate | 989-51-5 | sc-200802 sc-200802A sc-200802B sc-200802C sc-200802D sc-200802E | 10 mg 50 mg 100 mg 500 mg 1 g 10 g | $42.00 $72.00 $124.00 $238.00 $520.00 $1234.00 | 11 | |
EGCG is known to inhibit certain types of protein kinases. By inhibiting these kinases, EGCG may reduce the competitive phosphorylation of microtubule-associated proteins, potentially increasing the affinity of EML5 for microtubules and enhancing its activity in microtubule stabilization. | ||||||
D-erythro-Sphingosine-1-phosphate | 26993-30-6 | sc-201383 sc-201383D sc-201383A sc-201383B sc-201383C | 1 mg 2 mg 5 mg 10 mg 25 mg | $162.00 $316.00 $559.00 $889.00 $1693.00 | 7 | |
Sphingosine-1-phosphate acts through G-protein-coupled receptors to activate downstream kinases, such as ERK and Akt, which could indirectly enhance the activity of EML5 by modulating the cellular signaling environment that affects microtubule dynamics. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $121.00 $392.00 | 148 | |
LY294002 is a PI3K inhibitor that alters AKT signaling pathways. By dampening PI3K/AKT signaling, LY294002 may reduce phosphorylation events that negatively regulate EML5, leading to its increased activity in supporting microtubule architecture. | ||||||
U-0126 | 109511-58-2 | sc-222395 sc-222395A | 1 mg 5 mg | $63.00 $241.00 | 136 | |
U0126 is an inhibitor of MEK1/2, which in turn can lead to reduced ERK phosphorylation. By inhibiting this pathway, U0126 could shift the signaling equilibrium in a way that enhances the association and function of EML5 with the microtubule network, as EML5 activity can be regulated by ERK-dependent signaling. | ||||||
SB 203580 | 152121-47-6 | sc-3533 sc-3533A | 1 mg 5 mg | $88.00 $342.00 | 284 | |
SB203580 is a specific inhibitor of p38 MAPK. Inhibition of p38 may upregulate pathways that facilitate EML5 interaction with microtubules by altering the cellular response to stress and microtubule dynamics regulation. | ||||||
Thapsigargin | 67526-95-8 | sc-24017 sc-24017A | 1 mg 5 mg | $94.00 $349.00 | 114 | |
Thapsigargin disrupts calcium homeostasis by blocking the sarco/endoplasmic reticulum Ca2+-ATPase (SERCA). The resultant increase in cytosolic calcium levels can activate calcium-dependent kinases, which may enhance the stabilizing effect of EML5 on the microtubule cytoskeleton. | ||||||
Wortmannin | 19545-26-7 | sc-3505 sc-3505A sc-3505B | 1 mg 5 mg 20 mg | $66.00 $219.00 $417.00 | 97 | |
Wortmannin is another PI3K inhibitor that can lead to a decrease in AKT signaling. This reduction may indirectly promote EML5 activity by alleviating inhibitory phosphorylation events on microtubule-associated proteins, thus enhancing EML5's role in microtubule stabilization. | ||||||
Staurosporine | 62996-74-1 | sc-3510 sc-3510A sc-3510B | 100 µg 1 mg 5 mg | $82.00 $150.00 $388.00 | 113 | |
Staurosporine is a broad-spectrum kinase inhibitor, which could lead to the selective enhancement of EML5 activity by inhibiting kinases that negatively regulate the association of EML5 with microtubules or its ability to stabilize microtubules. | ||||||