LEDGF Inhibitors
LEDGF inhibitors are a class of chemical compounds that specifically target the protein Lens Epithelium-Derived Growth Factor (LEDGF), also known as p75. LEDGF is a transcription coactivator that is involved in a variety of cellular processes, including gene regulation and protection of cells from stress-induced damage. It is particularly known for its role in binding chromatin and interacting with a variety of cellular and viral proteins. LEDGF interacts with Integrase, a viral enzyme, through its integrase-binding domain (IBD), promoting its tethering to the chromatin. This interaction is crucial for certain biological processes, making LEDGF an attractive target for inhibition to disrupt specific pathways related to DNA interaction and binding. LEDGF inhibitors work by disrupting this interaction, usually by binding to the IBD, thereby blocking its role in protein-protein interactions.
Chemically, LEDGF inhibitors can take various structural forms, including small molecules with heterocyclic cores that are capable of forming strong hydrogen bonds or hydrophobic interactions with the integrase-binding domain of LEDGF. These inhibitors may contain functional groups like amines, carboxyls, or aromatic rings that enhance their affinity for LEDGF through hydrogen bonding or π-π stacking interactions. Some inhibitors are designed to interfere with LEDGF's DNA binding ability by altering its interaction with the chromatin. By disrupting these interactions, LEDGF inhibitors can affect the stability and localization of proteins that rely on LEDGF for chromatin association. Researchers studying LEDGF inhibitors often explore diverse chemical libraries to optimize the structural properties of these molecules for specific molecular interactions with LEDGF.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
5-Azacytidine | 320-67-2 | sc-221003 | 500 mg | $280.00 | 4 | |
This chemical could hypothetically decrease LEDGF expression by reducing methylation levels of the PSIP1 gene promoter, leading to altered transcriptional activity. | ||||||
Suberoylanilide Hydroxamic Acid | 149647-78-9 | sc-220139 sc-220139A | 100 mg 500 mg | $130.00 $270.00 | 37 | |
Suberoylanilide Hydroxamic Acid may lead to the acetylation of histones associated with the PSIP1 gene, potentially resulting in a loosening of chromatin structure and a subsequent decrease in LEDGF synthesis. | ||||||
5-Aza-2′-Deoxycytidine | 2353-33-5 | sc-202424 sc-202424A sc-202424B | 25 mg 100 mg 250 mg | $214.00 $316.00 $418.00 | 7 | |
By demethylating CpG islands within the PSIP1 promoter region, 5-Aza-2′-Deoxycytidine could hypothetically lower LEDGF expression by enhancing the promoter's accessibility to transcriptional repressors. | ||||||
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 | $36.00 $68.00 $107.00 $214.00 $234.00 $862.00 $1968.00 | 47 | |
Curcumin could potentially downregulate LEDGF expression by altering the activity of specific transcription factors responsible for the upregulation of the PSIP1 gene. | ||||||
Resveratrol | 501-36-0 | sc-200808 sc-200808A sc-200808B | 100 mg 500 mg 5 g | $60.00 $185.00 $365.00 | 64 | |
Resveratrol may lead to a downregulation of LEDGF by changing the activity of sirtuins, thereby possibly inducing histone modifications that repress PSIP1 gene transcription. | ||||||
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 | |
By inhibiting histone deacetylase activity, Trichostatin A could contribute to the hyperacetylation of histones near the PSIP1 gene, potentially reducing LEDGF expression levels. | ||||||
Disulfiram | 97-77-8 | sc-205654 sc-205654A | 50 g 100 g | $52.00 $87.00 | 7 | |
Disulfiram could indirectly lead to a reduction in LEDGF expression by altering the ubiquitin-proteasome system, potentially increasing the degradation of transcriptional activators of PSIP1. | ||||||
Quercetin | 117-39-5 | sc-206089 sc-206089A sc-206089E sc-206089C sc-206089D sc-206089B | 100 mg 500 mg 100 g 250 g 1 kg 25 g | $11.00 $17.00 $108.00 $245.00 $918.00 $49.00 | 33 | |
Quercetin might decrease LEDGF expression by hindering the phosphorylation states of transcription factors and coactivators involved in the transcription of the PSIP1 gene. | ||||||
D,L-Sulforaphane | 4478-93-7 | sc-207495A sc-207495B sc-207495C sc-207495 sc-207495E sc-207495D | 5 mg 10 mg 25 mg 1 g 10 g 250 mg | $150.00 $286.00 $479.00 $1299.00 $8299.00 $915.00 | 22 | |
DL-Sulforaphane might reduce LEDGF expression by attenuating NF-κB mediated transcriptional activation of the PSIP1 gene, through the suppression of inflammatory signaling pathways. | ||||||
Retinoic Acid, all trans | 302-79-4 | sc-200898 sc-200898A sc-200898B sc-200898C | 500 mg 5 g 10 g 100 g | $65.00 $319.00 $575.00 $998.00 | 28 | |
Retinoic acid might downregulate LEDGF production by altering the transcriptional landscape, including repression of genes involved in cell growth and differentiation, such as PSIP1. | ||||||