PMR1 Activators
Chemical activators of PMR1 can influence the protein's activity by altering the intracellular environment, particularly the ion concentrations that PMR1 is responsible for regulating. Bafilomycin A1, by inhibiting V-ATPases, leads to a disruption in proton gradients and subsequently ionic imbalances that PMR1 may respond to by increasing its ion transport activity to restore equilibrium. Similarly, Thapsigargin and Cyclopiazonic Acid both impede the function of SERCA pumps, causing a rise in cytosolic calcium levels that can activate PMR1 to counteract this by pumping calcium out of the cytosol. Ryanodine modulates calcium release from the endoplasmic reticulum, creating fluctuations in calcium levels that PMR1 addresses by adjusting its transport activity to stabilize these levels.
Carbachol indirectly influences PMR1 by raising cytosolic calcium through G protein-coupled receptor pathways, prompting PMR1 to increase its activity in an effort to control the calcium concentration. The calcium ionophore A23187 directly elevates intracellular calcium, which PMR1 can respond to by enhancing its calcium efflux functionality. Ionophore X-537A also causes calcium influx, requiring PMR1 to become more active to mitigate the effects of increased intracellular calcium. Verapamil, although primarily a blocker of calcium influx, can affect intracellular calcium stores in a manner that necessitates PMR1 activity. Caffeine triggers the release of calcium from intracellular stores, subsequently activating PMR1 as it works to reconstitute the calcium gradient. Dantrolene and Nifedipine, through their interactions with ryanodine receptors and voltage-gated calcium channels respectively, alter intracellular calcium dynamics, which can activate PMR1 to adjust its activity accordingly. Lastly, Digoxin's inhibition of Na+/K+-ATPase disrupts cellular ionic balance, potentially causing a compensatory increase in PMR1 activity to correct the resulting excess intracellular calcium. Each of these chemicals can lead to conditions that necessitate the active role of PMR1 in re-establishing ion homeostasis within the cell.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Bafilomycin A1 | 88899-55-2 | sc-201550 sc-201550A sc-201550B sc-201550C | 100 µg 1 mg 5 mg 10 mg | $96.00 $250.00 $750.00 $1428.00 | 280 | |
Bafilomycin A1 specifically inhibits V-ATPases, which can lead to a build-up of ions in cellular compartments, indirectly requiring PMR1 to compensate by increasing its functional activity to restore ion balance. | ||||||
Thapsigargin | 67526-95-8 | sc-24017 sc-24017A | 1 mg 5 mg | $94.00 $349.00 | 114 | |
Thapsigargin inhibits the sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) pump, leading to elevated cytosolic calcium levels that could necessitate increased activity of PMR1 to efflux excess Ca2+ to maintain cellular homeostasis. | ||||||
Cyclopiazonic Acid | 18172-33-3 | sc-201510 sc-201510A | 10 mg 50 mg | $173.00 $612.00 | 3 | |
As an inhibitor of SERCA pumps, cyclopiazonic acid can cause an increase in cytosolic calcium levels, which may activate PMR1 as a compensatory response to regulate calcium levels. | ||||||
Ryanodine | 15662-33-6 | sc-201523 sc-201523A | 1 mg 5 mg | $219.00 $765.00 | 19 | |
Ryanodine modulates the release of Ca2+ from sarcoplasmic/endoplasmic reticulum by binding to ryanodine receptors, which could enhance the functional demand on PMR1 to manage the altered Ca2+ dynamics. | ||||||
Carbachol | 51-83-2 | sc-202092 sc-202092A sc-202092C sc-202092D sc-202092B sc-202092E | 1 g 10 g 25 g 50 g 100 g 250 g | $120.00 $275.00 $380.00 $670.00 $1400.00 $3000.00 | 12 | |
Carbachol is a cholinergic agonist that can increase intracellular Ca2+ levels through G protein-coupled receptor signaling, indirectly stimulating PMR1 activity to counterbalance the elevated Ca2+ levels. | ||||||
A23187 | 52665-69-7 | sc-3591 sc-3591B sc-3591A sc-3591C | 1 mg 5 mg 10 mg 25 mg | $54.00 $128.00 $199.00 $311.00 | 23 | |
A23187 is a calcium ionophore that increases intracellular Ca2+ concentration, which likely necessitates an upsurge in PMR1 activity to extrude the surplus calcium from the cytosol. | ||||||
Verapamil | 52-53-9 | sc-507373 | 1 g | $367.00 | ||
Verapamil is a calcium channel blocker that, while known to reduce Ca2+ influx, its effects on intracellular Ca2+ stores can indirectly stimulate PMR1 to maintain Ca2+ homeostasis. | ||||||
Caffeine | 58-08-2 | sc-202514 sc-202514A sc-202514B sc-202514C sc-202514D | 5 g 100 g 250 g 1 kg 5 kg | $32.00 $66.00 $95.00 $188.00 $760.00 | 13 | |
Caffeine induces the release of Ca2+ from intracellular stores, which could secondarily increase the activity of PMR1 as it works to re-establish the Ca2+ gradient. | ||||||
Dantrolene | 7261-97-4 | sc-500165 | 25 mg | $350.00 | 7 | |
Dantrolene interacts with ryanodine receptors to attenuate Ca2+ release from the sarcoplasmic reticulum, which might activate PMR1 to counteract the perturbation in Ca2+ homeostasis. | ||||||
Nifedipine | 21829-25-4 | sc-3589 sc-3589A | 1 g 5 g | $58.00 $170.00 | 15 | |
Nifedipine blocks voltage-gated calcium channels, leading to altered intracellular calcium levels that could indirectly necessitate increased PMR1 activity to restore equilibrium. | ||||||