IRE1α Activators
IRE1α, or inositol-requiring enzyme 1 alpha, is a crucial protein involved in the unfolded protein response (UPR), a cellular stress response mechanism aimed at restoring cellular homeostasis in the endoplasmic reticulum (ER). As an endoribonuclease, IRE1α plays a central role in the UPR pathway by initiating the splicing of XBP1 mRNA, leading to the production of the active transcription factor XBP1s. This transcription factor then upregulates the expression of various ER chaperones, foldases, and components involved in ER-associated degradation (ERAD), facilitating the clearance of misfolded proteins and restoring ER function.
Activation of IRE1α typically occurs in response to ER stress, triggered by the accumulation of unfolded or misfolded proteins within the ER lumen. Under normal conditions, IRE1α is maintained in an inactive state through its interaction with the ER chaperone BiP. However, during ER stress, BiP dissociates from IRE1α, allowing it to oligomerize and undergo autophosphorylation, leading to its activation. Once activated, IRE1α catalyzes the unconventional splicing of XBP1 mRNA, resulting in the production of XBP1s. Additionally, activated IRE1α can also initiate a process known as regulated IRE1-dependent decay (RIDD), where it cleaves other ER-localized mRNAs, thereby reducing the load of protein translation in the ER. Overall, the activation of IRE1α is a crucial adaptive response mechanism that enables cells to cope with ER stress and maintain cellular homeostasis.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
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 activates IRE1α by inhibiting the function of ADP ribosylation factor (ARF), a small GTPase involved in vesicular trafficking. Inhibition of ARF leads to the disruption of ER-Golgi transport, causing accumulation of misfolded proteins in the ER and triggering the unfolded protein response (UPR), which subsequently activates IRE1α. | ||||||
Tunicamycin | 11089-65-9 | sc-3506A sc-3506 | 5 mg 10 mg | $172.00 $305.00 | 66 | |
Tunicamycin activates IRE1α by inducing ER stress through inhibition of N-linked glycosylation, leading to the accumulation of misfolded proteins in the ER. The unfolded protein response (UPR) is then triggered as a compensatory mechanism to restore ER homeostasis, resulting in the activation of IRE1α and subsequent initiation of downstream signaling pathways. | ||||||
Thapsigargin | 67526-95-8 | sc-24017 sc-24017A | 1 mg 5 mg | $136.00 $446.00 | 114 | |
Thapsigargin activates IRE1α by disrupting calcium homeostasis in the endoplasmic reticulum (ER), leading to ER stress. The accumulation of unfolded or misfolded proteins in the ER triggers the unfolded protein response (UPR), which activates IRE1α as part of the cellular adaptive response to restore ER function and alleviate stress conditions. | ||||||
2-Deoxy-D-glucose | 154-17-6 | sc-202010 sc-202010A | 1 g 5 g | $70.00 $215.00 | 26 | |
2-Deoxy-D-glucose activates IRE1α by inhibiting glycolysis and disrupting cellular energy metabolism, leading to the accumulation of misfolded proteins in the endoplasmic reticulum (ER) and induction of ER stress. This triggers the unfolded protein response (UPR), which activates IRE1α as part of the cellular adaptive response to restore ER function and alleviate stress conditions. | ||||||
Geldanamycin | 30562-34-6 | sc-200617B sc-200617C sc-200617 sc-200617A | 100 µg 500 µg 1 mg 5 mg | $39.00 $59.00 $104.00 $206.00 | 8 | |
Geldanamycin activates IRE1α by inhibiting heat shock protein 90 (HSP90), leading to the destabilization of client proteins involved in protein folding and quality control. Disruption of protein folding homeostasis results in the accumulation of misfolded proteins in the endoplasmic reticulum (ER), triggering the unfolded protein response (UPR) and subsequent activation of IRE1α as part of the adaptive cellular response. | ||||||
A23187 | 52665-69-7 | sc-3591 sc-3591B sc-3591A sc-3591C | 1 mg 5 mg 10 mg 25 mg | $55.00 $131.00 $203.00 $317.00 | 23 | |
A23187 activates IRE1α by inducing calcium release from intracellular stores, leading to disruption of calcium homeostasis in the endoplasmic reticulum (ER) and induction of ER stress. The accumulation of unfolded or misfolded proteins in the ER triggers the unfolded protein response (UPR), which activates IRE1α as part of the cellular adaptive response to restore ER function and alleviate stress conditions. | ||||||
4-Hydroxyphenylretinamide | 65646-68-6 | sc-200900 sc-200900A | 5 mg 25 mg | $104.00 $315.00 | ||
4-Hydroxyphenylretinamide activates IRE1α by inducing reactive oxygen species (ROS) production, leading to oxidative stress and accumulation of misfolded proteins in the endoplasmic reticulum (ER). This triggers the unfolded protein response (UPR), which activates IRE1α as part of the cellular adaptive response to restore ER function and alleviate stress conditions. | ||||||
Sodium (meta)arsenite | 7784-46-5 | sc-250986 sc-250986A | 100 g 1 kg | $108.00 $780.00 | 3 | |
Sodium arsenite activates IRE1α by inducing oxidative stress and disrupting redox homeostasis, leading to the accumulation of misfolded proteins in the endoplasmic reticulum (ER) and induction of ER stress. This triggers the unfolded protein response (UPR), which activates IRE1α as part of the cellular adaptive response to restore ER function and alleviate stress conditions. | ||||||
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 activates IRE1α by inhibiting the protein disulfide isomerase (PDI), leading to the accumulation of misfolded proteins in the endoplasmic reticulum (ER) and induction of ER stress. This triggers the unfolded protein response (UPR), which activates IRE1α as part of the cellular adaptive response to restore ER function and alleviate stress conditions. | ||||||
Hydrogen Peroxide | 7722-84-1 | sc-203336 sc-203336A sc-203336B | 100 ml 500 ml 3.8 L | $31.00 $61.00 $95.00 | 28 | |
H2O2 activates IRE1α by inducing oxidative stress and disrupting redox homeostasis, leading to the accumulation of misfolded proteins in the endoplasmic reticulum (ER) and induction of ER stress. This triggers the unfolded protein response (UPR), which activates IRE1α as part of the cellular adaptive response to restore ER function and alleviate stress conditions. | ||||||