DR1 inhibitors, in the absence of direct chemical inhibitors, rely on a variety of methods to interfere with DR1's role in transcriptional regulation. A prominent set of inhibitors targets the general transcriptional machinery, impacting RNA polymerase II and various transcription factors. Actinomycin D, for example, inhibits RNA synthesis by binding to DNA. α-Amanitin specifically inhibits RNA polymerase II, thus affecting DR1's interaction with the enzyme. Flavopiridol inhibits CDK9 and thereby influences the phosphorylation of the RNA polymerase II C-terminal domain, a crucial interaction point for DR1.
A second category focuses on broader cellular processes that indirectly influence transcriptional regulation where DR1 plays a role. This category includes Wortmannin, an inhibitor of PI3K, and Nutlin-3, which inhibits MDM2, affecting p53 levels. Both of these cellular pathways have wide-ranging effects, including on transcription. JQ1, a BET bromodomain inhibitor, affects chromatin readers which indirectly impacts DR1's ability to regulate transcription. Triptolide inhibits the XPB subunit of TFIIH, another component of the general transcriptional machinery. These compounds may not directly inhibit DR1, but their impact on cellular pathways or transcriptional complexes closely associated with DR1 can serve as indirect inhibitors.
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Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
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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 | $73.00 $238.00 $717.00 $2522.00 $21420.00 | 53 | |
Actinomycin D binds DNA and inhibits RNA synthesis. By affecting the overall transcriptional machinery, it can have an impact on DR1’s ability to regulate transcription. | ||||||
Triptolide | 38748-32-2 | sc-200122 sc-200122A | 1 mg 5 mg | $88.00 $200.00 | 13 | |
Triptolide inhibits the XPB subunit of TFIIH, thus affecting the general transcriptional machinery and consequently DR1's function. | ||||||
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 CK2 kinase which is involved in phosphorylation events in the transcription initiation complex. This can inhibit DR1’s function in repressing transcription. | ||||||
Flavopiridol Hydrochloride | 131740-09-5 | sc-207687 | 10 mg | $311.00 | ||
Inhibits CDK9, affecting the phosphorylation of the RNA polymerase II C-terminal domain. As DR1 interacts with RNA polymerase II, this can interfere with DR1’s activity. | ||||||
α-Amanitin | 23109-05-9 | sc-202440 sc-202440A | 1 mg 5 mg | $260.00 $1029.00 | 26 | |
Inhibits RNA polymerase II. Given that DR1's role in regulating transcription involves interaction with RNA polymerase II, this compound can affect DR1 indirectly. | ||||||
(±)-JQ1 | 1268524-69-1 | sc-472932 sc-472932A | 5 mg 25 mg | $226.00 $846.00 | 1 | |
A BET bromodomain inhibitor, JQ1 interferes with chromatin readers, thus affecting transcriptional regulation and potentially DR1's function. | ||||||
Wortmannin | 19545-26-7 | sc-3505 sc-3505A sc-3505B | 1 mg 5 mg 20 mg | $66.00 $219.00 $417.00 | 97 | |
Wortmannin inhibits PI3K which plays a role in various cellular processes including transcription. This can interfere with DR1's function. | ||||||
MLN 4924 | 905579-51-3 | sc-484814 | 1 mg | $280.00 | 1 | |
MLN4924 inhibits NEDD8-activating enzyme, affecting various cellular processes, including transcription. DR1’s role in transcription regulation can thus be affected. | ||||||
Cordycepin | 73-03-0 | sc-203902 | 10 mg | $99.00 | 5 | |
An adenosine analogue that is incorporated into RNA, affecting its stability. Given DR1's role in transcription, cordycepin can indirectly inhibit its function. | ||||||
Stat3 inhibitor V, stattic | 19983-44-9 | sc-202818 sc-202818A sc-202818B sc-202818C sc-202818D sc-202818E sc-202818F | 25 mg 100 mg 250 mg 500 mg 1 g 2.5 g 5 g | $127.00 $192.00 $269.00 $502.00 $717.00 $1380.00 $2050.00 | 114 | |
Inhibits STAT3, a transcription factor that can be involved in similar pathways to DR1. This can indirectly affect DR1's role in transcription. |