UGT1A5 Activators
Chemical activators of UGT1A5 represent a diverse array of molecules strategically designed to enhance the expression or activity of the enzyme through intricate signaling pathways. These activators play a crucial role in influencing the transcriptional regulation of the UGT1A5 gene, ultimately leading to an upsurge in the levels of this essential enzyme within cellular environments. One prominent group of UGT1A5 activators includes Phenobarbital and clofibric acid, which selectively target nuclear receptors CAR and PPARα, respectively. The activation process commences with the binding of these activators to their respective receptors, initiating a complex cascade of events. This cascade culminates in the recruitment of transcriptional co-activators to the UGT1A5 gene promoter, effectively enhancing the transcriptional machinery responsible for UGT1A5 gene expression. This intricate molecular dance orchestrated by the activators ensures a substantial increase in UGT1A5 enzyme levels, consequently amplifying its role in cellular detoxification and metabolism.
Indole-3-carbinol, chrysin, and citrus flavonoids represent another cohort of UGT1A5 activators that operate through the modulation of the AhR and PXR pathways. Activation of these pathways facilitates the translocation of AhR and PXR receptors to the nucleus, where they engage specific response elements on the UGT1A5 promoter. This engagement serves as a molecular trigger, promoting the transcriptional machinery to kick into action, resulting in heightened UGT1A5 gene expression. Through these pathways, indole-3-carbinol, chrysin, and citrus flavonoids intricately influence the cellular landscape, enhancing UGT1A5-mediated processes involved in detoxification and metabolism. Furthermore, activators impacting the Nrf2 pathway, exemplified by oltipraz and sulforaphane, bring an additional layer of complexity to UGT1A5 modulation. Activation of the Nrf2 pathway induces the nuclear translocation of Nrf2, which subsequently binds to antioxidant response elements (AREs) in the UGT1A5 promoter region. This molecular interaction sets the stage for an increased expression of UGT1A5, reinforcing its role in cellular detoxification processes.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Indole-3-carbinol | 700-06-1 | sc-202662 sc-202662A sc-202662B sc-202662C sc-202662D | 1 g 5 g 100 g 250 g 1 kg | $39.00 $61.00 $146.00 $312.00 $1032.00 | 5 | |
Indole-3-carbinol upregulates UGT1A5 expression through its metabolite, 3,3'-Diindolylmethane (DIM), which modulates the aryl hydrocarbon receptor (AhR) pathway. Activation of AhR leads to increased transcription of UGT1A5 by enhancing the binding of AhR to the xenobiotic response elements (XREs) in the promoter region of the gene encoding UGT1A5. | ||||||
Chrysin | 480-40-0 | sc-204686 | 1 g | $38.00 | 13 | |
Chrysin is a flavonoid that enhances UGT1A5 activity by modulating the nuclear receptor PXR. It binds to PXR and induces its translocation to the nucleus where it can enhance the transcription of UGT1A5 by binding to response elements upstream of the UGT1A5 gene. | ||||||
Oltipraz | 64224-21-1 | sc-205777 sc-205777A | 500 mg 1 g | $286.00 $622.00 | ||
Oltipraz, a dithiolethione, activates Nrf2 signaling, which in turn leads to the transcriptional upregulation of UGT1A5. It facilitates the release of Nrf2 from its cytoplasmic inhibitor Keap1, allowing Nrf2 translocation to the nucleus where it binds to antioxidant response elements (ARE) in the UGT1A5 promoter region, promoting gene expression. | ||||||
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 | $153.00 $292.00 $489.00 $1325.00 $8465.00 $933.00 | 22 | |
Sulforaphane activates the Nrf2 pathway similar to oltipraz. By inducing the release and nuclear translocation of Nrf2, it promotes the transcription of UGT1A5 via interaction with ARE in the gene's promoter. | ||||||
5-Aminosalicylic acid | 89-57-6 | sc-202890 | 5 g | $27.00 | 4 | |
5-Aminosalicylic acid induces the expression of UGT1A5 through its action on PPARγ receptors. The activated PPARγ receptors can dimerize with retinoid X receptor (RXR) and bind to PPAR response elements (PPREs) on the UGT1A5 gene promoter, stimulating its transcription. | ||||||
Clofibric acid | 882-09-7 | sc-203000 sc-203000A | 10 g 50 g | $24.00 $40.00 | 1 | |
Clofibric acid, a PPARα agonist, indirectly enhances UGT1A5 activity by activating PPARα. The activated PPARα/RXR complex can bind to PPREs in the UGT1A5 gene promoter, resulting in the induction of UGT1A5 expression. | ||||||
Ellagic Acid, Dihydrate | 476-66-4 | sc-202598 sc-202598A sc-202598B sc-202598C | 500 mg 5 g 25 g 100 g | $58.00 $95.00 $245.00 $727.00 | 8 | |
Ellagic acid stimulates the transcription of UGT1A5 by activating Nrf2. Upon activation, Nrf2 translocates to the nucleus and binds to AREs within the UGT1A5 gene promoter, driving its expression. | ||||||
Benzo[a]pyrene | 50-32-8 | sc-257130 | 1 g | $612.00 | 4 | |
Benzo[a]pyrene, though a procarcinogen, activates UGT1A5 by binding to and activating AhR, which in turn translocates to the nucleus and binds to XREs on the UGT1A5 promoter, enhancing its transcription. | ||||||
Retinoic Acid, all trans | 302-79-4 | sc-200898 sc-200898A sc-200898B sc-200898C | 500 mg 5 g 10 g 100 g | $66.00 $325.00 $587.00 $1018.00 | 28 | |
Retinoic acid increases UGT1A5 expression by binding to retinoic acid receptors (RARs) which heterodimerize with RXR and bind to retinoic acid response elements (RAREs) in the UGT1A5 gene promoter, promoting its transcription. | ||||||