KDEL ER Marker Inhibitors
KDEL ER Marker inhibitors, as discussed, do not represent a discrete chemical class but a conceptual group of compounds that can modulate the ER stress response pathways, thereby indirectly influencing the proteins tagged with the KDEL retention sequence. The chemicals listed above engage with the ER stress response at various stages, either by exacerbating the stress through the inhibition of proper protein glycosylation, calcium homeostasis, and trafficking or by stabilizing misfolded proteins within the ER, leading to increased demands on the KDEL chaperone system. This increase in demand overloads the system, rendering the KDEL retention less effective.
Furthermore, these compounds can influence the protein processing and folding environment within the ER, affecting the oxidative state or the balance of protein synthesis and degradation. For instance, agents that modulate the phosphorylation state of eIF2α or act as chemical chaperones alter the load of newly synthesized polypeptides entering the ER, thus changing the functional dynamics of KDEL-tagged proteins. Other compounds, such as those affecting the p97 ATPase or the heat shock protein network, can stabilize misfolded proteins, indirectly impinging upon the KDEL-dependent retrieval and degradation systems.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Tunicamycin | 11089-65-9 | sc-3506A sc-3506 | 5 mg 10 mg | $169.00 $299.00 | 66 | |
Tunicamycin inhibits N-linked glycosylation in the ER, leading to protein misfolding and induction of ER stress. By blocking the addition of sugar moieties to nascent proteins, it exacerbates the protein load within the ER, potentially overloading the KDEL retrieval system and indirectly influencing KDEL-tagged protein retention. | ||||||
Thapsigargin | 67526-95-8 | sc-24017 sc-24017A | 1 mg 5 mg | $94.00 $349.00 | 114 | |
Thapsigargin is a sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) pump inhibitor, leading to depletion of ER calcium stores and induction of ER stress. The sustained elevation of cytosolic calcium affects protein folding capacities, potentially impairing KDEL-tagged chaperones and their associated protein retrieval mechanisms. | ||||||
Brefeldin A | 20350-15-6 | sc-200861C sc-200861 sc-200861A sc-200861B | 1 mg 5 mg 25 mg 100 mg | $30.00 $52.00 $122.00 $367.00 | 25 | |
Brefeldin A disrupts ER to Golgi transport by inhibiting ADP-ribosylation factor, leading to Golgi disassembly. This blockade can cause an accumulation of proteins within the ER, possibly overwhelming KDEL receptor-mediated retrieval and influencing KDEL-tagged protein trafficking. | ||||||
β-Lapachone | 4707-32-8 | sc-200875 sc-200875A | 5 mg 25 mg | $110.00 $450.00 | 8 | |
Beta-Lapachone activates NAD(P)H quinone dehydrogenase 1, leading to an atypical ER stress response. This compound indirectly impacts the oxidative folding environment within the ER, potentially altering the efficacy of KDEL-tagged chaperones in managing misfolded proteins. | ||||||
Salubrinal | 405060-95-9 | sc-202332 sc-202332A | 1 mg 5 mg | $33.00 $102.00 | 87 | |
Salubrinal selectively inhibits phosphatases targeting the eIF2α phosphorylation, which is involved in the ER stress response. By preventing dephosphorylation, it leads to prolonged eIF2α-mediated attenuation of translation, potentially impacting the load of KDEL-tagged proteins required for recovery from ER stress. | ||||||
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 | $100.00 $459.00 $816.00 $4080.00 $7140.00 | 2 | |
Guanabenz selectively activates the unfolded protein response, indirectly enhancing the demand on KDEL-tagged chaperone proteins within the ER. This could impact the homeostasis and functioning of the KDEL retrieval system by increasing the burden on the chaperone cycle. | ||||||
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 | $112.00 $199.00 $347.00 $683.00 $1336.00 $5722.00 | 12 | |
Eeyarestatin I inhibits the p97 ATPase and the associated degradation of misfolded proteins within the ER, leading to ER stress. By stabilizing misfolded proteins, it may influence the KDEL-tagged proteins’ chaperone capacity and their involvement in the ER-associated degradation pathway. | ||||||