ERp27 Activators
Chemical activators of ERp27 can initiate a cascade of cellular responses that lead to the functional activation of this protein, which is crucial for maintaining proper protein folding and endoplasmic reticulum (ER) function. Thapsigargin, a potent inhibitor of the sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA), raises cytosolic calcium levels, which in turn can lead to ERp27 activation as part of calcium-dependent signaling pathways. Similarly, cyclopiazonic acid, also an inhibitor of SERCA, disrupts calcium homeostasis and induces ER stress, prompting the activation of ERp27. Tunicamycin blocks N-linked glycosylation, a critical process in protein maturation, leading to the unfolded protein response (UPR) and subsequent activation of ERp27 to aid in protein folding. Brefeldin A disrupts protein transport between the ER and Golgi apparatus, triggering ER stress and the UPR, which involves ERp27 in attempts to restore ER functions.
Moreover, compounds like 4-Phenylbutyric acid act as chemical chaperones to mitigate protein misfolding, consequently activating ERp27 as part of the ER-associated degradation pathway (ERAD). MG132, a proteasome inhibitor, causes the accumulation of misfolded proteins, which also induces ER stress and the UPR, leading to the activation of ERp27. Inhibitors like salubrinal and guanabenz prevent eIF2α dephosphorylation, enhancing UPR activity and thus activating ERp27. Eeyarestatin I, which inhibits ERAD, and Suberoylanilide hydroxamic acid (SAHA), a histone deacetylase inhibitor, can both induce ER stress responses, resulting in the activation of ERp27. Lastly, celastrol induces a heat shock response and chloroquine alters intracellular organelle pH, both conditions that can lead to ER stress and the activation of ERp27 as the cell works to cope with these stressors.
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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 sesquiterpene lactone known to selectively inhibit the sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA). By inhibiting SERCA, thapsigargin increases cytosolic calcium concentration, which can lead to the activation of calcium-dependent signaling pathways that ERp27 is involved in, thus functionally activating ERp27. | ||||||
Tunicamycin | 11089-65-9 | sc-3506A sc-3506 | 5 mg 10 mg | $172.00 $305.00 | 66 | |
Tunicamycin is an antibiotic that inhibits N-linked glycosylation. By preventing this glycosylation, tunicamycin can cause unfolded protein response (UPR) activation, a cellular stress response related to the endoplasmic reticulum. As part of UPR, ERp27 can be activated to assist in protein folding and maintenance of ER function. | ||||||
Brefeldin A | 20350-15-6 | sc-200861C sc-200861 sc-200861A sc-200861B | 1 mg 5 mg 25 mg 100 mg | $31.00 $53.00 $124.00 $374.00 | 25 | |
Brefeldin A is a fungal metabolite that acts as an inhibitor of protein transport from the endoplasmic reticulum to the Golgi apparatus. This disruption can lead to ER stress and the activation of the UPR, which can functionally activate ERp27 as the cell attempts to restore normal function in the ER. | ||||||
4-Phenylbutyric acid | 1821-12-1 | sc-232961 sc-232961A sc-232961B | 25 g 100 g 500 g | $53.00 $136.00 $418.00 | 10 | |
4-Phenylbutyric acid is a chemical chaperone that can reduce protein misfolding and alleviate ER stress. It can activate ER-associated degradation pathway (ERAD) in which ERp27 is functionally involved, thus leading to the activation of ERp27 in the process of managing misfolded proteins. | ||||||
MG-132 [Z-Leu- Leu-Leu-CHO] | 133407-82-6 | sc-201270 sc-201270A sc-201270B | 5 mg 25 mg 100 mg | $60.00 $265.00 $1000.00 | 163 | |
MG132 is a proteasome inhibitor that can lead to the accumulation of misfolded or ubiquitinated proteins within the cell. This accumulation can induce ER stress and the UPR, pathways in which ERp27 is functionally involved, thereby activating ERp27 as part of the cellular response to restore protein homeostasis. | ||||||
Salubrinal | 405060-95-9 | sc-202332 sc-202332A | 1 mg 5 mg | $34.00 $104.00 | 87 | |
Salubrinal is a selective inhibitor of eIF2α dephosphorylation, which leads to an enhancement of the phosphorylation state of eIF2α and activation of the UPR. ERp27 is activated as a component of the UPR to combat stress and restore normal ER functions. | ||||||
Eeyarestatin I | 412960-54-4 | sc-358130B sc-358130 sc-358130A sc-358130C sc-358130D sc-358130E | 5 mg 10 mg 25 mg 50 mg 100 mg 500 mg | $114.00 $203.00 $354.00 $697.00 $1363.00 $5836.00 | 12 | |
Eeyarestatin I is an inhibitor of ER-associated protein degradation (ERAD). By inhibiting this pathway, it can cause ER stress and subsequent UPR activation, leading to functional activation of ERp27, which is implicated in the ERAD process. | ||||||
Guanabenz acetate | 23256-50-0 | sc-203590 sc-203590A sc-203590B sc-203590C sc-203590D | 100 mg 500 mg 1 g 10 g 25 g | $102.00 $468.00 $832.00 $4162.00 $7283.00 | 2 | |
Guanabenz is known to selectively inhibit the dephosphorylation of eIF2α, similar to salubrinal. This inhibition can lead to an increase in UPR activity, thereby activating ERp27 as part of the cell's adaptive response to restore ER function. | ||||||
Suberoylanilide Hydroxamic Acid | 149647-78-9 | sc-220139 sc-220139A | 100 mg 500 mg | $133.00 $275.00 | 37 | |
SAHA, also known as Vorinostat, is a histone deacetylase inhibitor that can affect gene expression and protein acetylation states. This can lead to activation of ER stress responses and UPR, subsequently activating ERp27 as it functions to assist in protein folding and ER stress mitigation. | ||||||
Celastrol, Celastrus scandens | 34157-83-0 | sc-202534 | 10 mg | $158.00 | 6 | |
Celastrol is a quinone methide triterpene that induces heat shock response and has been shown to cause an increase in cellular stress responses. By inducing these responses, celastrol can activate ERp27 as part of the protective mechanisms against protein misfolding and aggregation. | ||||||