SERCA2 Inhibitors
SERCA2 inhibitors constitute a diverse class of chemical compounds designed to modulate the activity of Sarco/Endoplasmic Reticulum Calcium ATPase 2 (SERCA2), a critical regulator of calcium homeostasis in cells. While direct inhibitors like thapsigargin and cyclopiazonic acid directly target the ATP-binding site of SERCA2, others exert their influence indirectly by modulating various cellular pathways associated with SERCA2 function. Thapsigargin, a well-studied SERCA inhibitor, disrupts calcium homeostasis by binding to the ATP-binding site, preventing calcium reuptake into the endoplasmic reticulum. Cyclopiazonic acid, another direct inhibitor, selectively hinders SERCA activity, leading to elevated cytosolic calcium levels. These direct inhibitors provide valuable tools for understanding the consequences of impaired SERCA2 function on cellular processes. Several chemicals, including BHQ, naringin, curcumin, and rutin, indirectly modulate SERCA2 through the PI3K/Akt pathway, showcasing the involvement of signaling pathways in regulating SERCA2 function. These compounds activate Akt, supporting SERCA2 activity and contributing to calcium homeostasis. Additionally, resveratrol, ginsenoside Rd, and genistein influence SERCA2 through SIRT1/AMPK and PI3K/Akt pathways, emphasizing the intricate regulatory mechanisms governing SERCA2.
Antioxidants such as tannic acid and CGP37157 indirectly modulate SERCA2 by preventing oxidative damage and disrupting mitochondrial calcium efflux, respectively. Their mechanisms highlight the interconnected roles of redox status and mitochondrial calcium exchange in regulating SERCA2 function. Nordihydroguaiaretic acid (NDGA) influences SERCA2 through the PI3K/Akt pathway, providing a unique avenue for investigating interventions related to calcium homeostasis.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Thapsigargin | 67526-95-8 | sc-24017 sc-24017A | 1 mg 5 mg | $136.00 $446.00 | 114 | |
Thapsigargin is a potent SERCA inhibitor that disrupts calcium homeostasis. By binding to the ATP-binding site of SERCA, it prevents calcium reuptake into the endoplasmic reticulum, leading to cytosolic calcium elevation. This disruption activates downstream signaling cascades, influencing cellular processes and potentially affecting the function of SERCA2 in various physiological contexts. | ||||||
Cyclopiazonic Acid | 18172-33-3 | sc-201510 sc-201510A | 10 mg 50 mg | $176.00 $624.00 | 3 | |
Cyclopiazonic acid is a mycotoxin that selectively inhibits SERCA activity. By binding to the same site as thapsigargin, it disrupts calcium transport into the endoplasmic reticulum, causing elevated cytosolic calcium levels. This perturbation influences cellular processes and provides insights into the specific roles of SERCA2 in calcium homeostasis. | ||||||
Naringin | 10236-47-2 | sc-203443 sc-203443A | 25 g 50 g | $45.00 $101.00 | 7 | |
Naringin, a flavonoid, indirectly modulates SERCA2 by influencing the PI3K/Akt pathway. It activates Akt, which has been implicated in regulating SERCA2 activity. By enhancing Akt signaling, naringin potentially supports SERCA2 function, contributing to calcium homeostasis. | ||||||
Curcumin | 458-37-7 | sc-200509 sc-200509A sc-200509B sc-200509C sc-200509D sc-200509F sc-200509E | 1 g 5 g 25 g 100 g 250 g 1 kg 2.5 kg | $37.00 $69.00 $109.00 $218.00 $239.00 $879.00 $1968.00 | 47 | |
Curcumin, a polyphenol, indirectly modulates SERCA2 by affecting the NF-κB pathway. It inhibits NF-κB activation, which has been linked to SERCA2 regulation. By suppressing NF-κB signaling, curcumin potentially supports SERCA2 function, contributing to calcium homeostasis. | ||||||
Rutin trihydrate | 250249-75-3 | sc-204897 sc-204897A sc-204897B | 5 g 50 g 100 g | $57.00 $72.00 $126.00 | 7 | |
Rutin, a flavonoid, indirectly modulates SERCA2 by influencing the PI3K/Akt pathway. It activates Akt, which has been implicated in regulating SERCA2 activity. By enhancing Akt signaling, rutin potentially supports SERCA2 function, contributing to calcium homeostasis. | ||||||
Genistein | 446-72-0 | sc-3515 sc-3515A sc-3515B sc-3515C sc-3515D sc-3515E sc-3515F | 100 mg 500 mg 1 g 5 g 10 g 25 g 100 g | $45.00 $164.00 $200.00 $402.00 $575.00 $981.00 $2031.00 | 46 | |
Genistein, an isoflavone, indirectly modulates SERCA2 by influencing the PI3K/Akt pathway. It activates Akt, which has been implicated in regulating SERCA2 activity. By enhancing Akt signaling, genistein potentially supports SERCA2 function, contributing to calcium homeostasis. | ||||||
Ginsenoside Rd | 52705-93-8 | sc-205706 sc-205706A | 1 mg 5 mg | $76.00 $190.00 | ||
Ginsenoside Rd, a compound from Panax ginseng, indirectly modulates SERCA2 through the PI3K/Akt pathway. It activates Akt, which has been implicated in regulating SERCA2 activity. By enhancing Akt signaling, ginsenoside Rd potentially supports SERCA2 function, contributing to calcium homeostasis. | ||||||
Gallotannin | 1401-55-4 | sc-202619 sc-202619A sc-202619B sc-202619C sc-202619D sc-202619E sc-202619F | 1 g 10 g 100 g 250 g 1 kg 2.5 kg 5 kg | $26.00 $37.00 $67.00 $78.00 $234.00 $536.00 $983.00 | 12 | |
Tannic acid modulates SERCA2 through its antioxidant properties. By preventing oxidative damage to SERCA2, tannic acid indirectly supports its function. Oxidative stress can impair SERCA2 activity, leading to disrupted calcium homeostasis. Tannic acid, as an antioxidant, helps maintain SERCA2 function by mitigating oxidative damage. | ||||||
CGP 37157 | 75450-34-9 | sc-202097 sc-202097A | 5 mg 25 mg | $115.00 $463.00 | 3 | |
CGP37157 is a mitochondrial Na+/Ca2+ exchange inhibitor that indirectly modulates SERCA2 by disrupting calcium homeostasis. By inhibiting mitochondrial calcium efflux, CGP37157 leads to elevated cytosolic calcium levels, potentially impacting SERCA2 function. | ||||||
NDGA (Nordihydroguaiaretic acid) | 500-38-9 | sc-200487 sc-200487A sc-200487B | 1 g 5 g 25 g | $109.00 $384.00 $2190.00 | 3 | |
Nordihydroguaiaretic acid (NDGA) indirectly modulates SERCA2 by affecting the PI3K/Akt pathway. It activates Akt, which has been implicated in regulating SERCA2 activity. By enhancing Akt signaling, NDGA potentially supports SERCA2 function, contributing to calcium homeostasis. | ||||||