PHF3 Inhibitors
Chemical inhibitors of PHF3 include a diverse set of compounds that target various biological pathways and processes to achieve functional inhibition of the protein. Okadaic Acid, for instance, maintains PHF3 in a hyperphosphorylated state by inhibiting protein phosphatases PP1 and PP2A, which would normally dephosphorylate PHF3. This hyperphosphorylation can hinder the functional roles of PHF3. Similarly, MG-132 acts by inhibiting the proteasome pathway, preventing the degradation of ubiquitinated proteins, potentially leading to an accumulation of misfolded proteins that sequester PHF3 in non-functional complexes. Trichostatin A and SAHA (Vorinostat), both HDAC inhibitors, increase acetylation of histones, which can disrupt PHF3's interaction with chromatin, as such interactions often depend on the acetylation status of histones.
Furthermore, 5-Azacytidine and Mithramycin A can interfere with the chromatin-associated functions of PHF3 by altering DNA methylation patterns and binding to DNA, respectively, thereby imposing steric or allosteric constraints on PHF3's ability to modulate gene expression. Alpha-Amanitin directly inhibits RNA polymerase II, affecting the transcriptional landscape in which PHF3 operates. Compounds like I-CBP112 and JQ1, which target BET bromodomain proteins, can indirectly influence the transcriptional networks involving PHF3, leading to a reduction in PHF3's regulatory functions. Pladienolide B, by inhibiting the spliceosome, disrupts RNA splicing processes where PHF3 is implicated, while PF-477736's inhibition of Chk1 can broadly affect cell cycle-regulated processes that involve PHF3. Lastly, UNC0638 targets histone methyltransferases G9a and GLP, altering histone methylation and potentially disrupting PHF3's interactions with these epigenetic markers, which can inhibit PHF3's chromatin-related activities.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Okadaic Acid | 78111-17-8 | sc-3513 sc-3513A sc-3513B | 25 µg 100 µg 1 mg | $291.00 $530.00 $1800.00 | 78 | |
Okadaic Acid is a potent inhibitor of protein phosphatases PP1 and PP2A. PHF3 is known to be phosphorylated, and the inhibition of these phosphatases can prevent the dephosphorylation of PHF3, thereby maintaining PHF3 in a hyperphosphorylated state which can inhibit its function. | ||||||
MG-132 [Z-Leu- Leu-Leu-CHO] | 133407-82-6 | sc-201270 sc-201270A sc-201270B | 5 mg 25 mg 100 mg | $60.00 $265.00 $1000.00 | 163 | |
MG-132 functions as a proteasome inhibitor. By preventing the degradation of ubiquitinated proteins, it can lead to an accumulation of proteins within the cell, which can sequester PHF3 in non-functional complexes or disrupt its normal turnover, leading to functional inhibition. | ||||||
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 | $152.00 $479.00 $632.00 $1223.00 $2132.00 | 33 | |
Trichostatin A inhibits histone deacetylases (HDACs). Given that PHF3 has been implicated in chromatin remodeling through interaction with histones, HDAC inhibition can alter histone acetylation status and chromatin structure, thus potentially inhibiting the ability of PHF3 to interact with chromatin effectively. | ||||||
5-Azacytidine | 320-67-2 | sc-221003 | 500 mg | $280.00 | 4 | |
5-Azacytidine is an inhibitor of DNA methyltransferases. PHF3 is thought to interact with chromatin and DNA methylation patterns can influence chromatin structure and gene expression. Altered methylation can therefore hinder the chromatin-associated functions of PHF3. | ||||||
Suberoylanilide Hydroxamic Acid | 149647-78-9 | sc-220139 sc-220139A | 100 mg 500 mg | $133.00 $275.00 | 37 | |
SAHA is another HDAC inhibitor, which can lead to increased acetylation of histones. This change in the chromatin landscape can disrupt the normal function of chromatin-interacting proteins such as PHF3, potentially inhibiting its role in transcriptional regulation. | ||||||
Mithramycin A | 18378-89-7 | sc-200909 | 1 mg | $55.00 | 6 | |
Mithramycin A binds to GC-rich DNA sequences and inhibits RNA polymerase II. As PHF3 is involved in transcriptional regulation, this binding can interfere with PHF3's ability to regulate gene expression by steric hindrance or allosteric effects. | ||||||
α-Amanitin | 23109-05-9 | sc-202440 sc-202440A | 1 mg 5 mg | $269.00 $1050.00 | 26 | |
Alpha-Amanitin is a potent inhibitor of RNA polymerase II. By inhibiting this enzyme, the transcription of certain genes is halted. Since PHF3 is involved in transcriptional regulation, inhibiting RNA polymerase II can indirectly inhibit the function of PHF3 in gene regulation. | ||||||
I-CBP112 | 1640282-31-0 | sc-507494 | 25 mg | $400.00 | ||
I-CBP112 is a selective inhibitor of the BET family of bromodomain proteins. Although PHF3 is not a bromodomain protein, the inhibition of BET family members can alter the expression of genes that are co-regulated by PHF3, potentially leading to an indirect inhibition of its function. | ||||||
(±)-JQ1 | 1268524-69-1 | sc-472932 sc-472932A | 5 mg 25 mg | $231.00 $863.00 | 1 | |
JQ1 is a small molecule that inhibits the binding of BET bromodomain proteins to acetylated histones. By disrupting this interaction, JQ1 can alter the transcriptional network in which PHF3 is involved, leading to an indirect functional inhibition of PHF3. | ||||||
Pladienolide B | 445493-23-2 | sc-391691 sc-391691B sc-391691A sc-391691C sc-391691D sc-391691E | 0.5 mg 10 mg 20 mg 50 mg 100 mg 5 mg | $299.00 $5699.00 $11099.00 $25500.00 $66300.00 $2875.00 | 63 | |
Pladienolide B is an inhibitor of the spliceosome complex. PHF3 has been implicated in RNA splicing, and the inhibition of the spliceosome can disrupt the splicing machinery where PHF3 exerts its function, thus inhibiting its role in RNA processing. | ||||||