EAR2 Inhibitors
The chemical class known as EAR2 inhibitors comprises a diverse array of compounds that exert their inhibitory effects on EAR2 either directly or indirectly. One prominent group includes kinase inhibitors such as SB203580, TAK-715, and PD98059, which target specific signaling pathways related to EAR2 activation. SB203580, a p38 MAPK inhibitor, disrupts EAR2 phosphorylation through the p38 MAPK pathway, thereby impeding EAR2-mediated transcription. Similarly, TAK-715, another p38 MAPK inhibitor, attenuates EAR2 activation by interfering with the p38 MAPK signaling cascade. PD98059, a MEK inhibitor, prevents EAR2 phosphorylation via the MAPK pathway, leading to diminished EAR2 activity. Epigenetic modulators also feature prominently in this class, exemplified by Trichostatin A, a histone deacetylase inhibitor. Trichostatin A induces histone acetylation, altering chromatin structure and impairing EAR2 binding to target genes. Additionally, compounds like Resveratrol and Niclosamide indirectly inhibit EAR2 by modulating cellular processes. Resveratrol activates SIRT1, a deacetylase that enhances EAR2 degradation, while Niclosamide activates AMPK, a negative regulator of EAR2, resulting in decreased EAR2 transcriptional activity.
Furthermore, HSP90 inhibitors like 17-DMAG contribute to this class by targeting the chaperone protein HSP90, crucial for EAR2 stability. Inhibition of HSP90 by 17-DMAG induces EAR2 degradation, leading to reduced EAR2-mediated transcription. These diverse mechanisms collectively define the class of EAR2 inhibitors, offering researchers a toolbox of compounds to modulate EAR2 activity in various cellular contexts. Understanding the intricate interplay between these inhibitors and the specific cellular pathways they affect provides valuable insights for developing targeted interventions in the regulation of EAR2-mediated processes.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Resveratrol | 501-36-0 | sc-200808 sc-200808A sc-200808B | 100 mg 500 mg 5 g | $80.00 $220.00 $460.00 | 64 | |
Resveratrol inhibits EAR2 indirectly by activating SIRT1, a deacetylase that modulates the acetylation status of EAR2, leading to its degradation and reduced transcriptional activity. | ||||||
Thapsigargin | 67526-95-8 | sc-24017 sc-24017A | 1 mg 5 mg | $136.00 $446.00 | 114 | |
Thapsigargin inhibits EAR2 by disrupting calcium homeostasis, as EAR2 activity is calcium-dependent. Thapsigargin induces ER stress, depleting ER calcium stores, and consequently inhibiting EAR2-mediated signaling. | ||||||
SB 203580 | 152121-47-6 | sc-3533 sc-3533A | 1 mg 5 mg | $90.00 $349.00 | 284 | |
SB203580 is a p38 MAPK inhibitor that indirectly inhibits EAR2 by preventing its phosphorylation via the p38 MAPK pathway, a key signaling route regulating EAR2 activity. | ||||||
BAY 11-7082 | 19542-67-7 | sc-200615B sc-200615 sc-200615A | 5 mg 10 mg 50 mg | $62.00 $85.00 $356.00 | 155 | |
BAY 11-7082 inhibits EAR2 by suppressing NF-κB activation. EAR2 expression is influenced by NF-κB, and the inhibition of this transcription factor by BAY 11-7082 leads to reduced EAR2 transcriptional activity. | ||||||
Wortmannin | 19545-26-7 | sc-3505 sc-3505A sc-3505B | 1 mg 5 mg 20 mg | $67.00 $223.00 $425.00 | 97 | |
Wortmannin inhibits EAR2 indirectly by blocking the PI3K/Akt pathway, a signaling cascade that activates EAR2. Inhibition of PI3K/Akt by Wortmannin results in decreased EAR2 activation and downstream effects. | ||||||
(±)-JQ1 | 1268524-69-1 | sc-472932 sc-472932A | 5 mg 25 mg | $231.00 $863.00 | 1 | |
JQ1 inhibits EAR2 by selectively binding to BRD4, a co-factor required for EAR2 transcriptional activity. Disruption of the BRD4-EAR2 interaction hinders EAR2-mediated transcription, providing an indirect inhibitory effect. | ||||||
Rapamycin | 53123-88-9 | sc-3504 sc-3504A sc-3504B | 1 mg 5 mg 25 mg | $63.00 $158.00 $326.00 | 233 | |
Rapamycin inhibits EAR2 through mTOR inhibition. EAR2 expression is modulated by mTOR signaling, and the inhibition of mTOR by Rapamycin results in the suppression of EAR2 activity. | ||||||
Niclosamide | 50-65-7 | sc-250564 sc-250564A sc-250564B sc-250564C sc-250564D sc-250564E | 100 mg 1 g 10 g 100 g 1 kg 5 kg | $38.00 $79.00 $188.00 $520.00 $1248.00 $5930.00 | 8 | |
Niclosamide inhibits EAR2 indirectly by activating AMPK, a negative regulator of EAR2. Activation of AMPK leads to phosphorylation and inhibition of EAR2, diminishing its transcriptional activity. | ||||||
TAK 715 | 303162-79-0 | sc-362799 sc-362799A | 10 mg 50 mg | $185.00 $781.00 | ||
TAK-715 is a p38 MAPK inhibitor that indirectly inhibits EAR2 by interfering with the p38 MAPK pathway, which plays a role in regulating EAR2 activity. TAK-715 attenuates EAR2 activation by blocking this signaling route. | ||||||
Trichostatin A | 58880-19-6 | sc-3511 sc-3511A sc-3511B sc-3511C sc-3511D | 1 mg 5 mg 10 mg 25 mg 50 mg | $152.00 $479.00 $632.00 $1223.00 $2132.00 | 33 | |
Trichostatin A inhibits EAR2 by promoting histone acetylation, leading to altered chromatin accessibility and reduced EAR2 binding to its target genes. This epigenetic modification results in diminished EAR2 activity. | ||||||