SPT5 Inhibitors
The chemical class designated as SPT5 inhibitors includes a variety of compounds that exert their inhibitory effect indirectly through interference with transcriptional elongation or related processes. The mechanisms of action of these compounds range from direct inhibition of the RNA polymerase II to disruption of the phosphorylation events necessary for the transcriptional machinery's progression through gene loci. For instance, inhibitors like α-Amanitin and Triptolide exert their inhibitory effects by binding to RNA polymerase II, which is a direct partner of SPT5 during transcription elongation. Without the processive activity of RNA polymerase II, SPT5's role in transcription elongation is inherently compromised.
Moreover, compounds such as DRB and Flavopiridol target the phosphorylation process crucial for the transition of paused RNA polymerase II into an actively elongating form, which directly impacts SPT5 function as it is contingent on RNA polymerase II activity. These compounds, by inhibiting kinases like CDK9, stop the phosphorylation of SPT5 that is essential for its activity. Other inhibitors in this class function by altering the transcriptional landscape, as with I-BET151, which disrupts the recruitment of transcriptional machinery to chromatin, or by affecting RNA splicing and processing, such as Pladienolide B, which can indirectly influence SPT5's associated functions. Collectively, these inhibitors underscore the multifaceted approach necessary to modulate SPT5 activity, taking into account its critical involvement in RNA polymerase II-dependent transcription and the elaborate control of gene expression. Each compound, while diverse in structure and primary target, converges on the transcriptional pathway to exert an inhibitory effect on SPT5, attesting to the intricate regulatory network that governs transcription elongation and its associated factors.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
α-Amanitin | 23109-05-9 | sc-202440 sc-202440A | 1 mg 5 mg | $269.00 $1050.00 | 26 | |
Alpha-Amanitin binds to and inhibits RNA polymerase II, leading to the suppression of mRNA synthesis. Given that SPT5 functions as a transcription elongation factor, the inhibition of RNA polymerase II can result in a subsequent indirect reduction of SPT5 activity in transcriptional regulation. | ||||||
Triptolide | 38748-32-2 | sc-200122 sc-200122A | 1 mg 5 mg | $90.00 $204.00 | 13 | |
Triptolide is known to inhibit the transcriptional activity by affecting the RNA polymerase II. This disruption can indirectly diminish SPT5 function, as SPT5 is reliant on RNA polymerase II's activity for its role in transcription elongation and processing. | ||||||
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 kinase inhibitor that targets the positive transcription elongation factor b (P-TEFb), which phosphorylates the RNA polymerase II CTD and SPT5, a necessary step for transcription elongation. Inhibition of P-TEFb can reduce SPT5 phosphorylation and thus its activity. | ||||||
Flavopiridol | 146426-40-6 | sc-202157 sc-202157A | 5 mg 25 mg | $78.00 $259.00 | 41 | |
Flavopiridol is an inhibitor of cyclin-dependent kinases (CDKs) including CDK9 which is part of P-TEFb. By inhibiting CDK9, Flavopiridol reduces the phosphorylation of RNA polymerase II and SPT5, which is a prerequisite for their elongation activity, thus indirectly inhibiting SPT5. | ||||||
Actinomycin D | 50-76-0 | sc-200906 sc-200906A sc-200906B sc-200906C sc-200906D | 5 mg 25 mg 100 mg 1 g 10 g | $74.00 $243.00 $731.00 $2572.00 $21848.00 | 53 | |
Actinomycin D intercalates into DNA, inhibiting RNA polymerase movement and hence mRNA synthesis. This action indirectly inhibits SPT5 function by preventing the transcription elongation where SPT5 is fundamentally involved. | ||||||
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 targets the spliceosome, affecting pre-mRNA splicing. As SPT5 is involved in the coupling of transcription and RNA processing, disruption of splicing can indirectly modulate SPT5 activity by affecting its engagement with the transcriptional machinery and nascent RNA. | ||||||
I-BET 151 Hydrochloride | 1300031-49-5 (non HCl Salt) | sc-391115 | 10 mg | $450.00 | 2 | |
I-BET151 is a BET bromodomain inhibitor that displaces BET proteins from chromatin by competing for acetylated histones, affecting transcriptional regulation. SPT5 activity can be indirectly inhibited as the initiation and elongation phases of transcription are disrupted. | ||||||
CX-5461 | 1138549-36-6 | sc-507275 | 5 mg | $245.00 | ||
CX-5461 selectively inhibits RNA polymerase I, indirectly affecting the global transcriptional landscape, which could reduce SPT5 activity due to its reliance on active transcription machinery. | ||||||
Cordycepin | 73-03-0 | sc-203902 | 10 mg | $101.00 | 5 | |
Cordycepin, a nucleoside analog, terminates mRNA elongation. This can indirectly affect SPT5 activity by disrupting the transcription elongation process in which SPT5 is critically involved. | ||||||
BETd-246 | 2140289-17-2 | sc-507288 | 5 mg | $1071.00 | ||
As a BET degrader, BETd-246 promotes the degradation of BET proteins, leading to transcriptional repression. SPT5, being associated with transcription elongation, may be indirectly inhibited due to the reduced transcriptional activity. | ||||||