HIF-3α inhibitors consist of a broad range of compounds that interfere with the HIF signaling pathway at different levels, including DNA binding, protein stability, and transcriptional activity. These inhibitors do not target HIF-3α directly but modulate the hypoxia signaling pathway, resulting in reduced HIF-3α activity. For example, echinomycin acts by directly blocking the DNA-binding site of HIF, thus preventing transcriptional activation of hypoxia-responsive genes. Similarly, YC-1 and digoxin disrupt the synthesis and stability of HIF-α subunits, which can lead to a decrease in HIF-3α levels or activity due to the disruption of homeostatic feedback loops within the HIF family.
Some inhibitors, like topotecan and chetomin, target the molecular machinery that HIFs depend on for their transcriptional activity, while others, such as KC7F2 and PX-478, modulate the transcriptional activity of HIFs. SAHA, celastrol, and berberine engage in indirect inhibition through epigenetic modulation or by affecting proteasomal degradation pathways, which impact HIF-3α among a multitude of cellular targets.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Quinomycin A | 512-64-1 | sc-202306 | 1 mg | $166.00 | 4 | |
A small molecule that binds to the hypoxia-response element (HRE) in DNA, blocking the transcriptional activity of HIFs, including HIF-3α, by preventing their binding to the HRE. | ||||||
2-Methoxyestradiol | 362-07-2 | sc-201371 sc-201371A | 10 mg 50 mg | $71.00 $288.00 | 6 | |
Although initially considered a potential HIF activator, it also destabilizes microtubules and can suppress HIF transcriptional activity, potentially affecting HIF-3α as well. | ||||||
YC-1 | 170632-47-0 | sc-202856 sc-202856A sc-202856B sc-202856C | 1 mg 5 mg 10 mg 50 mg | $33.00 $124.00 $218.00 $947.00 | 9 | |
Inhibits HIF-1α and potentially other HIF subunits by increasing their degradation and decreasing their synthesis, which may lead to downregulation of HIF-3α through indirect mechanisms or signaling pathways. | ||||||
Topotecan Hydrochloride | 119413-54-6 | sc-204919 sc-204919A | 1 mg 5 mg | $45.00 $102.00 | 2 | |
A topoisomerase inhibitor that can reduce HIF-1α levels and might affect HIF-3α indirectly due to the interdependency of the HIF-α subunits within the cellular environment. | ||||||
Chetomin | 1403-36-7 | sc-202535 sc-202535A | 1 mg 5 mg | $186.00 $674.00 | 10 | |
Disrupts the interaction between HIF-α subunits and the p300 transcriptional coactivator, potentially reducing HIF-3α activity as a downstream effect. | ||||||
N,N′-(Dithiodi-2,1-ethanediyl)bis[2,5-dichloro-benzenesulfonamide | 927822-86-4 | sc-497219 | 25 mg | $330.00 | ||
A small molecule that inhibits HIF-1α transcriptional activity and could similarly affect HIF-3α by attenuating its transcriptional output. | ||||||
12β-Hydroxydigitoxin | 20830-75-5 | sc-213604 sc-213604A | 1 g 5 g | $143.00 $694.00 | ||
Traditionally used for cardiac conditions, 12β-Hydroxydigitoxin can also inhibit HIF-1α synthesis, which might lead to a reduction in HIF-3α levels due to compensatory regulatory mechanisms between HIF subunits. | ||||||
Acriflavine | 8048-52-0 | sc-214489 sc-214489A | 25 g 100 g | $50.00 $171.00 | 2 | |
Can interfere with HIF-1α dimerization; though it might lead to compensatory increases in other HIF subunits, it can also inhibit the overall HIF signaling, including HIF-3α under certain conditions. | ||||||
PX-478 | 685898-44-6 | sc-507409 | 10 mg | $175.00 | ||
Inhibits HIF-1α and can lead to the inhibition of the HIF pathway more broadly, potentially decreasing HIF-3α activity. | ||||||
Suberoylanilide Hydroxamic Acid | 149647-78-9 | sc-220139 sc-220139A | 100 mg 500 mg | $133.00 $275.00 | 37 | |
A histone deacetylase inhibitor that affects various transcription factors and might indirectly decrease HIF-3α levels by modifying the acetylation status of chromatin and transcriptional machinery. | ||||||