EF-HC1 Activators
Chemical activators of EF-HC1 can initiate a cascade of intracellular signaling events that culminate in the protein's activation. Calcium ionophores like A23187 and Ionomycin work by increasing intracellular calcium concentrations, directly influencing EF-HC1, which is sensitive to such changes. The elevated calcium levels foster the binding of EF-HC1 to calcium ions, which is a crucial step for its activation. This process is pivotal for its role in cellular signaling pathways. Similarly, Calcium Chloride can increase extracellular calcium, leading to an influx of this ion into the cell and subsequent activation of EF-HC1. Thapsigargin, another chemical in this group, indirectly raises cytosolic calcium levels by inhibiting the SERCA pump, resulting in calcium release from the endoplasmic reticulum and activation of EF-HC1. Bay K8644 further augments this cascade by acting as an agonist to L-type calcium channels, facilitating additional calcium influx into the cells, thereby activating EF-HC1. BAPTA-AM, while a calcium chelator that buffers calcium levels, can also, under certain circumstances, trigger a compensatory calcium influx that activates EF-HC1, illustrating the complex interplay within calcium regulation mechanisms.
On the other hand, the activation of EF-HC1 can also be modulated through phosphorylation by kinases. Phorbol 12-myristate 13-acetate (PMA) is a potent activator of protein kinase C (PKC), which phosphorylates various proteins, including EF-HC1, thus leading to its activation. The analogs 4-α-Phorbol 12,13-didecanoate (4αPDD) and OAG (1-Oleoyl-2-acetyl-sn-glycerol) serve similar functions by activating PKC, which in turn activates EF-HC1. Forskolin and 8-Bromo-cAMP act by increasing the levels of cAMP within the cell, which activates protein kinase A (PKA). PKA then phosphorylates EF-HC1, leading to its activation. This phosphorylation by PKA or PKC can induce conformational changes in EF-HC1, enhancing its functional activity within the cell's signaling pathways. These chemical activators, by modulating calcium levels or activating kinases, serve to regulate the activity of EF-HC1 through distinct but converging biochemical pathways.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
A23187 | 52665-69-7 | sc-3591 sc-3591B sc-3591A sc-3591C | 1 mg 5 mg 10 mg 25 mg | $55.00 $131.00 $203.00 $317.00 | 23 | |
Calcium ionophore, such as A23187, directly increases intracellular calcium levels. Elevated calcium can activate EF-HC1 as it is a calcium-responsive protein. This increase in calcium concentration can lead to the activation of EF-HC1 by enhancing its ability to bind to calcium, which is essential for its function in modulating neuronal firing and neurotransmitter release. | ||||||
PMA | 16561-29-8 | sc-3576 sc-3576A sc-3576B sc-3576C sc-3576D | 1 mg 5 mg 10 mg 25 mg 100 mg | $41.00 $132.00 $214.00 $500.00 $948.00 | 119 | |
PMA is a potent activator of protein kinase C (PKC), which is known to phosphorylate a multitude of proteins. Through the phosphorylation cascade, PKC can lead to the functional activation of EF-HC1 by phosphorylating residues on EF-HC1 or associated regulatory proteins that modulate its activity, leading to its full activation. | ||||||
8-Bromo-cAMP | 76939-46-3 | sc-201564 sc-201564A | 10 mg 50 mg | $126.00 $328.00 | 30 | |
8-Bromo-cAMP is a cell-permeable cAMP analog that can activate PKA. Activation of PKA may lead to the phosphorylation and subsequent activation of EF-HC1, as phosphorylation can result in conformational changes in EF-HC1 that enhance its functional activity. | ||||||
Ionomycin | 56092-82-1 | sc-3592 sc-3592A | 1 mg 5 mg | $78.00 $270.00 | 80 | |
Ionomycin is a calcium ionophore that selectively binds to and transports calcium ions across cell membranes, thereby increasing intracellular calcium levels. Elevated intracellular calcium can activate EF-HC1 by promoting its calcium-binding activity, which is central to its role in the regulation of neuronal excitability and signaling. | ||||||
Phorbol | 17673-25-5 | sc-253267 | 5 mg | $270.00 | 1 | |
4αPDD activates PKC isoforms. Through the activation of PKC, EF-HC1 can be phosphorylated, which may lead to its functional activation, as PKC-mediated phosphorylation is known to regulate the activity of various proteins involved in cellular signaling. | ||||||
Calcium chloride anhydrous | 10043-52-4 | sc-207392 sc-207392A | 100 g 500 g | $66.00 $262.00 | 1 | |
Calcium chloride, when used to increase extracellular calcium concentrations, can lead to an influx of calcium ions into the cell. The rise in intracellular calcium can then activate EF-HC1 by promoting its binding to calcium, which may directly enhance its activity as EF-HC1 is responsive to calcium levels within the cell. | ||||||
Thapsigargin | 67526-95-8 | sc-24017 sc-24017A | 1 mg 5 mg | $136.00 $446.00 | 114 | |
Thapsigargin inhibits the sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA), leading to an increase in cytosolic calcium levels. Elevated cytosolic calcium can activate EF-HC1 by facilitating its binding to calcium, thereby enhancing its functional role in the cell. | ||||||
(±)-Bay K 8644 | 71145-03-4 | sc-203324 sc-203324A sc-203324B | 1 mg 5 mg 50 mg | $84.00 $196.00 $817.00 | ||
Bay K8644 acts as a calcium channel agonist, specifically binding to and activating L-type calcium channels, which leads to an increased influx of calcium ions. This elevation in intracellular calcium can activate EF-HC1, as it is a calcium-sensitive protein, and its activation is crucial for its role in regulating neuronal activity. | ||||||
1-Oleoyl-2-acetyl-sn-glycerol (OAG) | 86390-77-4 | sc-200417 sc-200417A | 10 mg 50 mg | $119.00 $453.00 | 1 | |
OAG is an analog of diacylglycerol (DAG), which can activate PKC. Through the activation of PKC, OAG can lead to the phosphorylation and subsequent functional activation of EF-HC1, as PKC-mediated phosphorylation can change the activity state of proteins within cells. | ||||||
BAPTA/AM | 126150-97-8 | sc-202488 sc-202488A | 25 mg 100 mg | $138.00 $458.00 | 61 | |
BAPTA-AM is a cell-permeable calcium chelator that, once inside cells, is hydrolyzed by intracellular esterases to yield BAPTA, a calcium-binding agent. While it primarily acts to buffer calcium levels, it can paradoxically lead to calcium influx through feedback mechanisms intended to restore calcium levels, thus potentially leading to the activation of EF-HC1 by enhancing calcium sensitivity. | ||||||