PE-1 Inhibitors
PE-1 Inhibitors are a specialized class of chemical compounds that target the transcription factor PE-1, also known as ETV3 (ETS Variant 3). ETV3 is a member of the ETS family of transcription factors, which are characterized by a conserved ETS domain that binds to specific DNA sequences, regulating the expression of genes involved in critical cellular processes such as differentiation, proliferation, and apoptosis. By modulating the activity of ETV3, PE-1 Inhibitors can influence the transcriptional programs controlled by this factor, thereby affecting cellular functions at a molecular level.
These inhibitors operate through various mechanisms. One approach involves designing molecules that directly bind to the ETS domain of ETV3, preventing it from interacting with its target DNA sequences. This can be achieved by creating small molecules or peptides that mimic the DNA binding sites or fit into the DNA-binding groove of the ETS domain, effectively blocking DNA access. Another strategy is to disrupt essential protein-protein interactions required for ETV3's transcriptional activity. Since ETV3 may form complexes with cofactors or other proteins to regulate gene expression, interfering with these interactions can inhibit its function. Additionally, some PE-1 Inhibitors may promote the degradation of the ETV3 protein by targeting it for ubiquitination and subsequent proteasomal degradation. Chemically, these inhibitors are designed to interact specifically with structural features unique to ETV3, ensuring selectivity and minimizing off-target effects. Research into PE-1 Inhibitors enhances the understanding of transcriptional regulation by ETS family proteins and sheds light on the complex networks that control gene expression and cellular behavior.
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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 | $149.00 $470.00 $620.00 $1199.00 $2090.00 | 33 | |
Trichostatin A may downregulate PE-1 by inhibiting histone deacetylases, leading to a more condensed chromatin state around the PE-1 promoter, which can suppress the initiation of transcription. | ||||||
5-Azacytidine | 320-67-2 | sc-221003 | 500 mg | $280.00 | 4 | |
This compound could decrease PE-1 expression by causing hypomethylation of its gene promoter, thereby altering the transcriptional control of the PE-1 gene. | ||||||
Actinomycin D | 50-76-0 | sc-200906 sc-200906A sc-200906B sc-200906C sc-200906D | 5 mg 25 mg 100 mg 1 g 10 g | $73.00 $238.00 $717.00 $2522.00 $21420.00 | 53 | |
Actinomycin D is known to intercalate into DNA, and it could specifically hinder the binding of RNA polymerase II to the PE-1 gene, resulting in a reduction of PE-1 mRNA synthesis. | ||||||
α-Amanitin | 23109-05-9 | sc-202440 sc-202440A | 1 mg 5 mg | $260.00 $1029.00 | 26 | |
By selectively inhibiting RNA polymerase II, α-Amanitin would decrease the transcriptional output of the PE-1 gene, leading to lower PE-1 protein levels. | ||||||
(±)-JQ1 | 1268524-69-1 | sc-472932 sc-472932A | 5 mg 25 mg | $226.00 $846.00 | 1 | |
JQ1 could displace BET domain-containing proteins from chromatin, potentially leading to the downregulation of PE-1 expression due to the loss of positive transcriptional regulators at the PE-1 locus. | ||||||
Flavopiridol | 146426-40-6 | sc-202157 sc-202157A | 5 mg 25 mg | $78.00 $254.00 | 41 | |
Flavopiridol may reduce PE-1 expression by inhibiting cyclin-dependent kinases that are necessary for the transition from transcription initiation to elongation, a critical step for PE-1 gene expression. | ||||||
Rapamycin | 53123-88-9 | sc-3504 sc-3504A sc-3504B | 1 mg 5 mg 25 mg | $62.00 $155.00 $320.00 | 233 | |
By inhibiting mTOR, Rapamycin may lead to a cellular state that is unfavorable for PE-1 gene transcription, thus indirectly leading to decreased PE-1 protein levels. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $121.00 $392.00 | 148 | |
LY 294002, a PI3K inhibitor, could decrease the expression of PE-1 by disrupting downstream signaling pathways that control the activity of transcription factors responsible for PE-1 gene transcription. | ||||||
Chloroquine | 54-05-7 | sc-507304 | 250 mg | $68.00 | 2 | |
Chloroquine may lead to the accumulation of dysfunctional proteins and organelles, which could create a stressed cellular state that indirectly leads to the downregulation of PE-1 expression. | ||||||
Mithramycin A | 18378-89-7 | sc-200909 | 1 mg | $54.00 | 6 | |
Mithramycin A can bind to specific DNA sequences and could inhibit the binding of transcriptional machinery to the promoter region of PE-1, thus decreasing its expression. | ||||||