POLR2D Activators
Chemical activators of POLR2D work through a variety of mechanisms to influence the activity of this subunit of RNA polymerase II. Amiloride functions by inhibiting sodium channels, leading to an increase in intracellular sodium concentrations. This alteration in the cellular ionic environment can enhance the activity of POLR2D as part of the cellular response to maintain ionic homeostasis. DRB and Flavopiridol, on the other hand, target the transcription elongation process. DRB inhibits the positive transcription elongation factor b (P-TEFb), which is essential for RNA polymerase II activation. This inhibition results in a compensatory activation of POLR2D to sustain essential transcriptional processes. Similarly, Flavopiridol inhibits CDK9 within the P-TEFb complex, which leads to the release of paused RNA polymerase II, subsequently increasing POLR2D activity as transcription is resumed.
Other chemical activators influence chromatin structure and gene expression, thereby affecting POLR2D activity. Trichostatin A, for example, inhibits histone deacetylases, resulting in a more open chromatin configuration that facilitates POLR2D access to DNA for transcription. I-BET151 and JQ1 disrupt the interaction between acetylated histones and bromodomains, enhancing the recruitment of the RNA polymerase II complex that includes POLR2D to the chromatin. C646 selectively inhibits histone acetyltransferase p300, leading to transcriptional changes that can increase the recruitment and activation of POLR2D. BIX-01294 inhibits G9a histone methyltransferase, altering chromatin in a manner that may enhance POLR2D activity. MG132, a proteasome inhibitor, results in the accrual of proteins, some of which may interact with and activate POLR2D. Cycloheximide blocks protein synthesis, leading to an increase in transcriptional activity that includes POLR2D activation. Lastly, VP16 causes DNA damage, activating POLR2D as part of the cellular response to transcribe DNA repair genes, and Pyridostatin stabilizes G-quadruplex structures, challenging the progression of RNA polymerase II and subsequently leading to POLR2D activation to resolve these structures and continue transcription.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Amiloride | 2609-46-3 | sc-337527 | 1 g | $290.00 | 7 | |
Amiloride, a diuretic agent, inhibits sodium channels which indirectly can enhance the activity of POLR2D by increasing intracellular sodium concentration, leading to altered cellular processes that may include activation of the RNA polymerase II complex to which POLR2D belongs. | ||||||
DRB | 53-85-0 | sc-200581 sc-200581A sc-200581B sc-200581C | 10 mg 50 mg 100 mg 250 mg | $42.00 $185.00 $310.00 $650.00 | 6 | |
DRB inhibits the positive transcription elongation factor b (P-TEFb), which is necessary for RNA polymerase II activation. Inhibition of P-TEFb leads to a compensatory mechanism that results in the activation of POLR2D-containing RNA polymerase II to maintain essential transcription. | ||||||
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 | $149.00 $470.00 $620.00 $1199.00 $2090.00 | 33 | |
Trichostatin A inhibits histone deacetylases (HDACs), leading to a more relaxed chromatin structure, which allows easier access for the transcription machinery, including POLR2D, facilitating its activation in the transcription process. | ||||||
Flavopiridol | 146426-40-6 | sc-202157 sc-202157A | 5 mg 25 mg | $78.00 $254.00 | 41 | |
Flavopiridol inhibits CDK9 which is part of the P-TEFb complex, leading to the release of paused RNA polymerase II. This can result in the upregulation of POLR2D activity as the complex it is part of is released to resume transcription. | ||||||
I-BET 151 Hydrochloride | 1300031-49-5 (non HCl Salt) | sc-391115 | 10 mg | $450.00 | 2 | |
I-BET151 disrupts the interaction between acetylated histones and BET family bromodomains, impacting transcription regulation and potentially facilitating the activation of POLR2D by allowing RNA polymerase II complexes to initiate transcription more efficiently. | ||||||
(±)-JQ1 | 1268524-69-1 | sc-472932 sc-472932A | 5 mg 25 mg | $226.00 $846.00 | 1 | |
JQ1 binds to BET bromodomains, preventing the recognition of acetylated lysines on histone tails, which may result in POLR2D activation as the RNA polymerase II machinery is recruited to chromatin for transcription initiation. | ||||||
C646 | 328968-36-1 | sc-364452 sc-364452A | 10 mg 50 mg | $260.00 $925.00 | 5 | |
C646 is a selective inhibitor of histone acetyltransferase p300, which can lead to changes in chromatin structure and gene expression, potentially enhancing the recruitment and activation of POLR2D as a part of the RNA polymerase II complex. | ||||||
MG-132 [Z-Leu- Leu-Leu-CHO] | 133407-82-6 | sc-201270 sc-201270A sc-201270B | 5 mg 25 mg 100 mg | $56.00 $260.00 $980.00 | 163 | |
MG132 inhibits proteasomes, leading to the accumulation of proteins that may include factors that interact with and activate POLR2D as part of RNA polymerase II, promoting transcription. | ||||||
Cycloheximide | 66-81-9 | sc-3508B sc-3508 sc-3508A | 100 mg 1 g 5 g | $40.00 $82.00 $256.00 | 127 | |
Cycloheximide inhibits eukaryotic protein synthesis which can lead to a compensatory increase in transcriptional activity, thereby possibly increasing the functional activity of POLR2D within the RNA polymerase II complex. | ||||||
BIX01294 hydrochloride | 1392399-03-9 | sc-293525 sc-293525A sc-293525B | 1 mg 5 mg 25 mg | $36.00 $110.00 $400.00 | ||
BIX-01294 is an inhibitor of G9a histone methyltransferase, potentially resulting in alterations in chromatin that could facilitate the activation of POLR2D by enabling enhanced assembly or stability of the RNA polymerase II complex on DNA. | ||||||