eIF2Bγ Activators
eIF2Bγ Activators are a distinct class of chemical compounds that specifically target and enhance the activity of eIF2Bγ, a subunit of the eukaryotic initiation factor 2B complex involved in the initiation phase of protein synthesis. eIF2Bγ, encoded by the gene EIF2B3, plays a pivotal role in the regulation of protein synthesis by catalyzing the exchange of GDP for GTP on eIF2, resetting the eIF2-GTP-tRNAiMet ternary complex, which is essential for the translation initiation process. Activators of eIF2Bγ function by stabilizing the active form of eIF2B or by enhancing its GDP-GTP exchange activity. In doing so, these molecules facilitate the rate at which the initiation complex assembles, ultimately leading to increased general protein synthesis. This upregulation of protein synthesis is not due to an increase in the expression of eIF2Bγ but rather due to the direct enhancement of its existing functional capacity.
The biochemical mechanisms through which eIF2Bγ Activators exert their effect are complex and involve precise molecular interactions. These activators often bind to allosteric sites on the eIF2B complex, inducing conformational changes that result in a higher affinity for eIF2 and GDP, thereby expediting the exchange process. In some instances, the activators may also protect eIF2Bγ from phosphorylation-mediated inhibition, which is a common regulatory mechanism under stress conditions. By maintaining eIF2Bγ in a more consistently active state, these compounds ensure that the eIF2-GTP-tRNAiMet ternary complex is readily available, leading to a more robust and efficient initiation of translation. This direct impact on the initiation phase of protein synthesis underscores their specificity and the significance of their role in the fine-tuning of cellular protein production.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Guanabenz HCl | 23113-43-1 | sc-507500 | 100 mg | $246.00 | ||
Guanabenz, an alpha-2 adrenergic agonist, has been found to inhibit the dephosphorylation of eIF2α, thus indirectly maintaining the eIF2α–eIF2B complex in an inactive state. This leads to the preservation of eIF2Bγ activity when eIF2α is phosphorylated under stress conditions, ensuring proper regulation of protein synthesis. | ||||||
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. It acts indirectly to enhance eIF2Bγ activity by preventing the dephosphorylation of eIF2α, thereby maintaining the eIF2α–eIF2B interaction and preventing eIF2Bγ inhibition. | ||||||
Halofuginone | 55837-20-2 | sc-507290 | 100 mg | $1775.00 | ||
Halofuginone stimulates the amino acid starvation response, leading to eIF2α phosphorylation. This enhances the eIF2Bγ-mediated stress response, as the phosphorylated eIF2α has a reduced inhibitory effect on eIF2Bγ, thus promoting translational control during amino acid deprivation. | ||||||
Trazodone Hydrochloride | 25332-39-2 | sc-213097 sc-213097A | 100 mg 1 g | $194.00 $194.00 | ||
Trazodone has been reported to have an effect on the stress response pathway by inhibiting the dephosphorylation of eIF2α, indirectly maintaining eIF2Bγ activity by preserving the phosphorylated state of eIF2α which interacts less with eIF2Bγ, allowing it to function optimally. | ||||||
Nelfinavir | 159989-64-7 | sc-507314 | 10 mg | $168.00 | ||
Nelfinavir, an HIV protease inhibitor, has been shown to lead to eIF2α phosphorylation. It indirectly enhances eIF2Bγ activity by maintaining the phosphorylation of eIF2α, thereby reducing its inhibitory effect on the eIF2B complex. | ||||||
Sulfasalazine | 599-79-1 | sc-204312 sc-204312A sc-204312B sc-204312C | 1 g 2.5 g 5 g 10 g | $61.00 $77.00 $128.00 $209.00 | 8 | |
Sulfasalazine is known to induce oxidative stress, which can lead to eIF2α phosphorylation, thereby indirectly enhancing eIF2Bγ activity by reducing the inhibitory interaction between eIF2α and the eIF2B complex. | ||||||
Homoharringtonine | 26833-87-4 | sc-202652 sc-202652A sc-202652B | 1 mg 5 mg 10 mg | $52.00 $125.00 $182.00 | 11 | |
Homoharringtonine induces phosphorylation of eIF2α, consequently enhancing eIF2Bγ activity by ensuring that eIF2B is less inhibited by its interaction with phosphorylated eIF2α, thus promoting protein synthesis under stress conditions. | ||||||
1,1-Dimethylbiguanide, Hydrochloride | 1115-70-4 | sc-202000F sc-202000A sc-202000B sc-202000C sc-202000D sc-202000E sc-202000 | 10 mg 5 g 10 g 50 g 100 g 250 g 1 g | $20.00 $43.00 $63.00 $156.00 $260.00 $510.00 $31.00 | 37 | |
Metformin activates AMP-activated protein kinase (AMPK), which can lead to the phosphorylation of eIF2α. This phosphorylation indirectly enhances eIF2Bγ activity by maintaining the eIF2α–eIF2B interaction in a state that is less inhibitory to eIF2Bγ. | ||||||
Ginkgolide B | 15291-77-7 | sc-201037B sc-201037 sc-201037C sc-201037A | 5 mg 10 mg 25 mg 50 mg | $46.00 $64.00 $114.00 $201.00 | 8 | |
Ginkgolide B is known to induce the phosphorylation of eIF2α through oxidative stress mechanisms, thereby indirectly enhancing eIF2Bγ activity by reducing the inhibitory effect of eIF2α on the eIF2B complex. | ||||||