RARα2 Inhibitors
RARα2 inhibitors are a class of chemical compounds specifically designed to target and inhibit the function of the retinoic acid receptor alpha isoform 2 (RARα2), a nuclear receptor that plays a crucial role in regulating gene expression in response to retinoic acid. RARα2, as a subtype of the RARα protein, binds to retinoic acid, a derivative of vitamin A, and forms heterodimers with retinoid X receptors (RXRs). This complex binds to specific DNA sequences known as retinoic acid response elements (RAREs), promoting or repressing the transcription of target genes involved in key biological processes such as cell growth, differentiation, and development. The expression of RARα2 is tightly regulated and varies in different tissues, contributing to the precise control of gene regulation in response to retinoic acid. Inhibitors of RARα2 function by binding to the receptor's ligand-binding domain or interfering with its ability to interact with DNA, effectively blocking its activity in gene transcription.
The inhibition of RARα2 disrupts the normal retinoic acid-mediated signaling pathways, leading to changes in the expression of genes that are crucial for cell differentiation, proliferation, and homeostasis. By blocking the activity of RARα2, these inhibitors can interfere with the regulation of genes involved in various developmental and metabolic processes, particularly those responsive to retinoic acid levels. Researchers use RARα2 inhibitors to study the specific role of this receptor isoform in gene regulation and to understand its contributions to retinoic acid signaling networks. These inhibitors provide valuable insights into the functional specificity of RARα2 compared to other isoforms of the retinoic acid receptor family, allowing scientists to explore how each isoform uniquely impacts cellular processes. Additionally, the study of RARα2 inhibitors offers a deeper understanding of the mechanisms by which nuclear receptors regulate gene expression in response to external signals, contributing to the broader knowledge of transcriptional regulation in various physiological contexts.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
AM 580 | 102121-60-8 | sc-203505 sc-203505A | 5 mg 25 mg | $99.00 $390.00 | 2 | |
AM 580, a synthetic retinoid, selectively activates RAR isoforms other than RARα2, potentially initiating a negative feedback loop that could downregulate the expression of RARα2 by decreasing its transcriptional activity. | ||||||
AM 80 | 94497-51-5 | sc-203816 sc-203816A | 10 mg 50 mg | $155.00 $620.00 | 1 | |
AM 80, by preferentially binding to RARβ and RARγ, could decrease the expression of RARα2 indirectly by competitive inhibition, thereby shifting the retinoic acid signaling away from RARα2. | ||||||
CH 55 | 110368-33-7 | sc-203884 sc-203884A | 10 mg 50 mg | $141.00 $599.00 | ||
The compound CH 55, while acting as a retinoid agonist, could disrupt RARα2 expression by altering the equilibrium of retinoic acid receptor-mediated transcription, leading to reduced RARα2 activity. | ||||||
LE 135 | 155877-83-1 | sc-204053 sc-204053A | 10 mg 50 mg | $168.00 $707.00 | 5 | |
LE 135, by antagonizing RARβ, has the potential to indirectly decrease RARα2 expression, as it may cause a shift in the balance of retinoic acid receptor activities away from RARα2. | ||||||
BMS 493 | 215030-90-3 | sc-361124 sc-361124A | 10 mg 50 mg | $459.00 $1428.00 | 7 | |
BMS 493, as a pan-RAR inverse agonist, could inhibit the transcriptional activation capabilities of RARα2, resulting in a reduction of its expression and activity within the cell. | ||||||
SR 11237 | 146670-40-8 | sc-296418 sc-296418A | 5 mg 50 mg | $211.00 $877.00 | ||
SR 11237, as a selective RARγ agonist, could downregulate RARα2 expression by redirecting retinoic acid signaling to RARγ, thereby reducing the transcriptional activity of RARα2. | ||||||
Erythromycin | 114-07-8 | sc-204742 sc-204742A sc-204742B sc-204742C | 5 g 25 g 100 g 1 kg | $57.00 $245.00 $831.00 $1331.00 | 4 | |
Erythromycin might indirectly reduce RARα2 expression by triggering cellular stress responses that lead to changes in gene expression patterns, including those of nuclear receptors. | ||||||
Ketoconazole | 65277-42-1 | sc-200496 sc-200496A | 50 mg 500 mg | $63.00 $265.00 | 21 | |
Ketoconazole, known to inhibit cytochrome P450 enzymes, could lead to decreased RARα2 expression by interfering with the metabolic pathways responsible for synthesizing the retinoids that regulate RARα2 activity. | ||||||