GRP 78 Activators
GRP 78 Activators represent a specialized class of chemical compounds that induce the expression or enhance the activity of Glucose-Regulated Protein 78 (GRP 78), a chaperone protein localized primarily in the endoplasmic reticulum (ER). These activators are often involved in modulating cellular stress pathways, particularly the unfolded protein response (UPR), which is activated under conditions of ER stress. ER stress occurs when there is an imbalance in the ER's protein-folding capacity, often due to the accumulation of misfolded or unfolded proteins, imbalances in calcium homeostasis, or oxidative stress. Chemical compounds belonging to this class usually induce this type of cellular stress, triggering the UPR and subsequently leading to an upregulation of GRP 78. This protein plays a vital role in maintaining cellular homeostasis by assisting in protein folding, assembly, and translocation.
The mechanisms by which GRP 78 Activators work can vary widely. Some compounds inhibit specific enzymatic activities crucial for maintaining the ER's normal functioning, thereby inducing stress. For example, inhibitors of the sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) can disrupt calcium homeostasis in the ER, leading to the upregulation of GRP 78. Others may act as chemical chaperones that paradoxically induce ER stress under specific conditions, thus leading to increased expression of GRP 78. Yet others may disrupt cellular redox balance, leading to oxidative stress and the induction of the ER stress response. Overall, GRP 78 Activators are an interesting and diverse class of compounds that offer valuable insights into the complex cellular mechanisms surrounding ER stress and protein folding.
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| 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 non-competitive inhibitor of the sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA). By inhibiting SERCA, it causes an increase in cytosolic calcium, thereby inducing ER stress and subsequently upregulating GRP 78. | ||||||
Tunicamycin | 11089-65-9 | sc-3506A sc-3506 | 5 mg 10 mg | $172.00 $305.00 | 66 | |
Tunicamycin inhibits N-linked glycosylation, an essential post-translational modification, causing the accumulation of unfolded proteins in the ER. This ER stress triggers the upregulation of GRP 78. | ||||||
Sodium phenylbutyrate | 1716-12-7 | sc-200652 sc-200652A sc-200652B sc-200652C sc-200652D | 1 g 10 g 100 g 1 kg 10 kg | $77.00 $166.00 $622.00 $5004.00 $32783.00 | 43 | |
Sodium phenylbutyrate acts as a chemical chaperone that helps in the proper folding of proteins, but paradoxically, it can also lead to ER stress at higher concentrations, thus inducing GRP 78 expression. | ||||||
Auranofin | 34031-32-8 | sc-202476 sc-202476A sc-202476B | 25 mg 100 mg 2 g | $153.00 $214.00 $4000.00 | 39 | |
Auranofin is an inhibitor of thioredoxin reductase, an enzyme that maintains cellular redox balance. Inhibition leads to oxidative stress and ER stress, causing an increase in GRP 78 expression. | ||||||
Tamoxifen | 10540-29-1 | sc-208414 | 2.5 g | $272.00 | 18 | |
Tamoxifen affects calcium homeostasis and leads to the accumulation of unfolded proteins in the ER, thus triggering ER stress and upregulating GRP 78. | ||||||
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 can disrupt cellular calcium levels and also generate reactive oxygen species, both of which can induce ER stress and lead to the upregulation of GRP 78. | ||||||
Resveratrol | 501-36-0 | sc-200808 sc-200808A sc-200808B | 100 mg 500 mg 5 g | $80.00 $220.00 $460.00 | 64 | |
Resveratrol can modulate the oxidative state of the cell, thus creating a condition of ER stress that induces the expression of GRP 78. | ||||||
Naringenin | 480-41-1 | sc-219338 | 25 g | $245.00 | 11 | |
Naringenin can induce oxidative stress and interfere with calcium homeostasis, which leads to ER stress and subsequently increases the expression of GRP 78. | ||||||
Arsenic(III) oxide | 1327-53-3 | sc-210837 sc-210837A | 250 g 1 kg | $89.00 $228.00 | ||
Arsenic trioxide induces oxidative stress and interferes with thiol redox balance, thereby causing ER stress and upregulating GRP 78 expression. | ||||||
Caffeine | 58-08-2 | sc-202514 sc-202514A sc-202514B sc-202514C sc-202514D | 50 g 100 g 250 g 1 kg 5 kg | $33.00 $67.00 $97.00 $192.00 $775.00 | 13 | |
Caffeine inhibits phosphodiesterase, leading to an increase in cAMP and intracellular calcium levels, which can induce ER stress and upregulate GRP 78. | ||||||