ABCG2 Activators
ABCG2 activators represent a diverse group of chemicals that exert their influence on the ABCG2 transporter, a vital player in cellular detoxification and drug efflux. These activators can be broadly categorized based on their modes of action, which predominantly involve indirect modulation of cellular signaling pathways. One notable group includes tyrosine kinase inhibitors like Gefitinib and Imatinib. These chemicals indirectly activate ABCG2 by disrupting signaling cascades associated with EGFR and c-Kit, highlighting the interconnectedness of tyrosine kinase pathways with ABCG2 regulation. Another class comprises natural polyphenols such as Curcumin and Resveratrol.
These compounds indirectly activate ABCG2 by modulating intracellular signaling pathways like NF-κB and SIRT1/AMPK. Curcumin, for instance, prevents NF-κB-mediated transcription, leading to decreased ABCG2 expression, while Resveratrol activates AMPK, resulting in the suppression of mTOR-dependent ABCG2 regulation. This showcases the intricate interplay between dietary compounds and cellular signaling in controlling ABCG2 activity.Histone deacetylase inhibitors like Valproic Acid and Vorinostat represent yet another group of ABCG2 activators. Through epigenetic modulation, these chemicals induce hyperacetylation of histones, positively regulating ABCG2 expression.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
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, a natural polyphenol found in turmeric, activates ABCG2 indirectly by modulating the NF-κB signaling pathway. It inhibits the degradation of IκBα, preventing its phosphorylation and subsequent proteasomal degradation. | ||||||
Resveratrol | 501-36-0 | sc-200808 sc-200808A sc-200808B | 100 mg 500 mg 5 g | $60.00 $185.00 $365.00 | 64 | |
Resveratrol, a natural polyphenol, activates ABCG2 indirectly by modulating the SIRT1/AMPK pathway. It enhances SIRT1 activity, leading to deacetylation and activation of AMPK. Activated AMPK negatively regulates mTOR, which in turn suppresses ABCG2 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 | $150.00 $286.00 $479.00 $1299.00 $8299.00 $915.00 | 22 | |
Sulforaphane activates ABCG2 indirectly by targeting the NRF2/ARE pathway. It stabilizes NRF2 and promotes its nuclear translocation, leading to the transcriptional activation of ABCG2. | ||||||
Thioridazine | 50-52-2 | sc-473180 | 50 mg | $500.00 | ||
Thioridazine indirectly activates ABCG2 by influencing the p53 pathway. It stabilizes and activates p53, a transcription factor known to upregulate ABCG2 expression. | ||||||
Valproic Acid | 99-66-1 | sc-213144 | 10 g | $85.00 | 9 | |
Valproic Acid indirectly activates ABCG2 by inhibiting the HDAC pathway. It functions as a histone deacetylase (HDAC) inhibitor, leading to hyperacetylation of histones. | ||||||
Betulinic Acid | 472-15-1 | sc-200132 sc-200132A | 25 mg 100 mg | $115.00 $337.00 | 3 | |
Betulinic Acid activates ABCG2 indirectly by modulating the JNK/c-Jun pathway. It activates JNK, leading to the phosphorylation and activation of c-Jun. Activated c-Jun, in turn, enhances ABCG2 expression by binding to its promoter region. | ||||||
Ciclopirox | 29342-05-0 | sc-217893 | 25 mg | $207.00 | 2 | |
Ciclopirox activates ABCG2 indirectly by inhibiting the HIF-1α pathway. It suppresses the stabilization and transactivation of HIF-1α, which negatively regulates ABCG2 expression. | ||||||
Raloxifene | 84449-90-1 | sc-476458 | 1 g | $802.00 | 3 | |
Raloxifene indirectly activates ABCG2 by modulating the Wnt/β-catenin pathway. It inhibits Wnt signaling, preventing the nuclear translocation of β-catenin. | ||||||
Suberoylanilide Hydroxamic Acid | 149647-78-9 | sc-220139 sc-220139A | 100 mg 500 mg | $130.00 $270.00 | 37 | |
Suberoylanilide Hydroxamic Acid activates ABCG2 indirectly by inhibiting the HDAC pathway. As a histone deacetylase inhibitor, Vorinostat induces hyperacetylation of histones, leading to the upregulation of ABCG2 expression. | ||||||