ER81 Inhibitors
ER81, also known as ETS-related gene 81, is a transcription factor belonging to the ETS (E26 transformation-specific) family, which plays a critical role in various cellular processes including cell differentiation, proliferation, development, and apoptosis. As a transcription factor, ER81 binds to specific DNA sequences to regulate the expression of genes involved in these processes. It is particularly important in the development of the nervous system and has been implicated in the maturation of specific neuron populations. Additionally, ER81 is involved in the regulation of angiogenesis and has been linked to the progression of certain types of cancer due to its role in cell cycle regulation and tumor cell proliferation. Its activity is therefore crucial for the proper development and function of various tissues, and its dysregulation can contribute to disease pathogenesis, highlighting the importance of precisely regulating ER81 activity within cells.
The inhibition of ER81 involves mechanisms that can either directly interfere with its DNA-binding ability, alter its transcriptional activity, or modulate its expression levels. One common approach to inhibiting ER81 is through the use of small molecules or peptides that block its interaction with DNA, thereby preventing the transcription of target genes. Additionally, post-translational modifications such as phosphorylation, acetylation, or ubiquitination can also regulate the activity of ER81, affecting its stability, localization, or affinity for DNA. For example, phosphorylation by specific kinases may either enhance or inhibit ER81's transcriptional activity, depending on the context and the specific residues modified. Furthermore, the expression of ER81 can be downregulated by microRNAs or by competitive inhibition from other transcription factors, offering additional layers of control over its activity.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
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, a histone deacetylase (HDAC) inhibitor, indirectly inhibits ER81 by modulating chromatin structure. By inhibiting HDAC, Trichostatin A increases histone acetylation, leading to a more open chromatin conformation. This alteration in chromatin accessibility can impact the binding and activity of ER81, influencing its transcriptional regulation. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $123.00 $400.00 | 148 | |
LY-294002, a phosphoinositide 3-kinase (PI3K) inhibitor, indirectly inhibits ER81 by disrupting the PI3K/AKT signaling pathway. PI3K is involved in various cellular processes, including cell survival and proliferation. By inhibiting PI3K with LY-294002, the downstream signaling events that intersect with ER81 regulation are affected. | ||||||
PD 98059 | 167869-21-8 | sc-3532 sc-3532A | 1 mg 5 mg | $40.00 $92.00 | 212 | |
PD98059, a MEK inhibitor, indirectly inhibits ER81 by affecting the MAPK/ERK signaling pathway. MEK is a crucial component of this pathway, and its inhibition by PD98059 disrupts the normal signaling cascade. This disruption leads to downstream effects on cellular processes involving ER81, representing an indirect modulation of ER81 activity through alterations in the MAPK/ERK signaling pathway. | ||||||
SB 203580 | 152121-47-6 | sc-3533 sc-3533A | 1 mg 5 mg | $90.00 $349.00 | 284 | |
SB203580, a p38 MAPK inhibitor, indirectly influences ER81 by modulating the p38 MAPK signaling pathway. By inhibiting p38 MAPK, SB203580 disrupts the normal signaling cascade, affecting downstream events associated with ER81 regulation. This compound represents a potential indirect inhibitor by modulating the cellular pathways connected to ER81 activity. | ||||||
(–)-Nutlin-3 | 675576-98-4 | sc-222086 sc-222086A | 1 mg 5 mg | $122.00 $219.00 | 2 | |
Nutlin-3, a small molecule, indirectly inhibits ER81 by disrupting the p53-MDM2 interaction. Nutlin-3 disrupts the negative feedback loop between p53 and MDM2, leading to p53 stabilization and activation. As ER81 is a downstream target of p53, the modulation of p53 activity by Nutlin-3 indirectly impacts ER81 expression. | ||||||
(±)-JQ1 | 1268524-69-1 | sc-472932 sc-472932A | 5 mg 25 mg | $231.00 $863.00 | 1 | |
JQ1, a bromodomain and extraterminal (BET) protein inhibitor, indirectly inhibits ER81 by targeting the BET family of proteins. BET proteins are involved in chromatin remodeling, and their inhibition by JQ1 alters the chromatin landscape. This epigenetic modulation impacts the accessibility of ER81 to its target genes, leading to indirect inhibition of ER81 activity. | ||||||
SB-216763 | 280744-09-4 | sc-200646 sc-200646A | 1 mg 5 mg | $71.00 $202.00 | 18 | |
SB216763, a glycogen synthase kinase-3 (GSK-3) inhibitor, indirectly inhibits ER81 by affecting the Wnt signaling pathway. GSK-3 is a key component of the Wnt pathway, and its inhibition by SB216763 leads to the stabilization of β-catenin. This modulation of Wnt signaling can influence ER81 expression and activity, demonstrating the potential for indirect inhibition through the manipulation of the Wnt pathway. | ||||||
SP600125 | 129-56-6 | sc-200635 sc-200635A | 10 mg 50 mg | $40.00 $150.00 | 257 | |
SP600125, a JNK inhibitor, indirectly influences ER81 by targeting the JNK signaling pathway. JNK is involved in cellular stress responses and growth regulation. By inhibiting JNK, SP600125 disrupts the normal signaling cascade, affecting downstream events associated with ER81 regulation. . | ||||||
Histone Lysine Methyltransferase Inhibitor Inhibitor | 935693-62-2 (free base) | sc-202651 | 5 mg | $151.00 | 4 | |
BIX01294, a G9a histone methyltransferase inhibitor, indirectly inhibits ER81 by influencing histone methylation. G9a is involved in the methylation of histone H3 lysine 9 (H3K9), and its inhibition by BIX01294 leads to alterations in chromatin structure. This epigenetic modulation can impact the accessibility of ER81 to its target genes, representing an indirect inhibition through the regulation of histone methylation. | ||||||
C646 | 328968-36-1 | sc-364452 sc-364452A | 10 mg 50 mg | $265.00 $944.00 | 5 | |
C646, a histone acetyltransferase (HAT) inhibitor, indirectly inhibits ER81 by affecting histone acetylation. By inhibiting HAT, C646 disrupts the acetylation of histones, leading to alterations in chromatin structure. This epigenetic modulation can impact the accessibility of ER81 to its target genes, representing an indirect inhibition through the regulation of histone acetylation. | ||||||