WDR61 Activators
WDR61 Activators are chemical compounds that indirectly enhance the functional activity of WDR61 by influencing various pathways and cellular processes that WDR61 is involved in. WDR61, as part of the RNA polymerase II-associated Paf1 complex, plays a significant role in transcription elongation. Compounds such as BAY 11-7082 and TPCA-1 inhibit the NF-κB, leading to the stabilization of transcriptional machinery components and thus enhancing the activity of WDR61 by reducing competition for these resources. Cycloheximide and Triptolide, both transcription inhibitors through different mechanisms, can lead to an accumulation of RNA polymerase II at transcription start sites or stalled RNA polymerase II, respectively. This accumulation requires the Paf1 complex, including WDR61, to orchestrate the transition to productive elongation, thus indirectly enhancing its activity. Similarly, Trichostatin A, by altering chromatin structure, and JQ1, by interfering with chromatin remodeling, create a demand for WDR61's role in the Paf1 complex to facilitate transcription elongation in a more open chromatin environment.
Moreover, the activity of WDR61 is indirectly enhanced by compounds such as Flavopiridol, DRB, and Dinaciclib, which are CDK inhibitors. These inhibitors lead to a paused or regulated transcription elongation process that necessitates the Paf1 complex's involvement, and therefore WDR61, to resume and regulate RNA polymerase II activity. MLN4924 works by inhibiting a different pathway, the neddylation of cullin-RING E3 ubiquitin ligases, which can stabilize factors that participate in transcription, indirectly enhancing WDR61's role in this process. Ribociclib and PF-477736 affect the cell cycle and DNA damage response, respectively, which can alter the dynamics of the transcriptional machinery, thereby increasing the dependence on WDR61's function within the Paf1 complex.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
BAY 11-7082 | 19542-67-7 | sc-200615B sc-200615 sc-200615A | 5 mg 10 mg 50 mg | $62.00 $85.00 $356.00 | 155 | |
BAY 11-7082 is an NF-κB pathway inhibitor known to block IκBα phosphorylation, leading to the inhibition of NF-κB translocation to the nucleus. As WDR61 is a component of the RNA polymerase II-associated factor 1 complex (Paf1C), involved in transcription elongation, its activity is enhanced when the NF-κB pathway is inhibited, as this pathway can sequester components of the transcription machinery. | ||||||
Cycloheximide | 66-81-9 | sc-3508B sc-3508 sc-3508A | 100 mg 1 g 5 g | $41.00 $84.00 $275.00 | 127 | |
Cycloheximide is a protein synthesis inhibitor that leads to the accumulation of RNA polymerase II at the transcription start sites. This accumulation can enhance WDR61 function as it is essential for the transition of RNA polymerase II into productive elongation, part of the Paf1C complex. | ||||||
MLN 4924 | 905579-51-3 | sc-484814 | 1 mg | $286.00 | 1 | |
MLN4924 is a NEDD8-activating enzyme inhibitor, leading to the suppression of cullin-RING E3 ubiquitin ligases. This inhibition can stabilize transcription-related factors and thereby potentially enhance the activity of WDR61 as part of the Paf1C, which is critical for the transcriptional elongation. | ||||||
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 is an HDAC inhibitor that alters chromatin structure, enhancing transcription elongation. WDR61, as a Paf1C complex component, is involved in the transition into productive elongation, and its function can be enhanced by the more accessible chromatin state induced by Trichostatin A. | ||||||
Flavopiridol | 146426-40-6 | sc-202157 sc-202157A | 5 mg 25 mg | $78.00 $259.00 | 41 | |
Flavopiridol is a CDK9 inhibitor that leads to the suppression of transcription elongation. Paradoxically, this can enhance WDR61 activity by increasing the requirement for Paf1C complex components to regulate paused RNA polymerase II, which is crucial during transcription regulation. | ||||||
(±)-JQ1 | 1268524-69-1 | sc-472932 sc-472932A | 5 mg 25 mg | $231.00 $863.00 | 1 | |
JQ1 is a BET bromodomain inhibitor that interferes with chromatin remodeling. By doing so, JQ1 can enhance WDR61 function indirectly by necessitating greater involvement of the Paf1C complex in transcription elongation where WDR61 operates. | ||||||
Triptolide | 38748-32-2 | sc-200122 sc-200122A | 1 mg 5 mg | $90.00 $204.00 | 13 | |
Triptolide is a transcription inhibitor that targets the XPB subunit of TFIIH and can enhance WDR61 activity. The inhibition of XPB leads to increased demand for Paf1C complex activity in which WDR61 is essential, to assist stalled RNA polymerase II. | ||||||
DRB | 53-85-0 | sc-200581 sc-200581A sc-200581B sc-200581C | 10 mg 50 mg 100 mg 250 mg | $43.00 $189.00 $316.00 $663.00 | 6 | |
DRB is a CDK9 inhibitor that prevents RNA polymerase II phosphorylation, causing transcription elongation to pause. This pause necessitates the functional activity of the Paf1C, thereby enhancing the activity of WDR61, which is crucial for resuming transcription. | ||||||
IKK-2 Inhibitor IV | 507475-17-4 | sc-203083 | 500 µg | $133.00 | 12 | |
TPCA-1 is an IKK-2 inhibitor that impedes the NF-κB signaling pathway. By inhibiting this pathway, TPCA-1 can enhance WDR61 activity by reducing competition for transcriptional machinery, where WDR61 plays a pivotal role as part of the Paf1C. | ||||||
Ribociclib | 1211441-98-3 | sc-507367 | 10 mg | $450.00 | ||
Ribociclib is a CDK4/6 inhibitor that indirectly affects the cell cycle and can enhance the activity of WDR61 by altering the availability of transcriptional machinery, as Paf1C complex members like WDR61 are critical for RNA polymerase II function. | ||||||