TFIIA Inhibitors
Chemical inhibitors of Transcription Factor IIA (TFIIA) operate through various mechanisms to impede the proper functioning of this essential protein in the transcription initiation process. Triptolide is one such inhibitor that disrupts the transcriptional activity at the core level by preventing the assembly of transcription machinery at the promoter site, thereby blocking TFIIA binding to the DNA complex. Similarly, Distamycin B (DrB) binds to the minor groove of DNA, creating a physical barrier to TFIIA and thus deterring its access to DNA binding sites. This action results in the functional inhibition of TFIIA in the transcription initiation complex. Actinomycin D exerts its inhibitory effect by intercalating into DNA at the transcription initiation complex site, obstructing RNA polymerase II and consequently impeding the elongation of the RNA chain which TFIIA is involved in initiating. Another DNA intercalating agent, Mitoxantrone, also hinders TFIIA function by causing DNA breaks and obstructing transcription processes.
Oxaliplatin, which forms DNA adducts and cross-links, similarly affects TFIIA functionality by altering DNA structure and preventing the necessary complex formation for transcription initiation. α-Amanitin specifically targets RNA polymerase II, thereby indirectly inhibiting TFIIA's role in transcription initiation by hindering the machinery it assists. Etoposide and Camptothecin, which target topoisomerase II and I respectively, lead to DNA damage and the stabilization of DNA-topoisomerase complexes, thus preventing the necessary DNA unwinding for TFIIA to function effectively. Cordycepin, a nucleoside analog, terminates RNA chain elongation prematurely, indirectly inhibiting TFIIA by stopping the transcription process it facilitates. Flavopiridol inhibits CDK9, part of the P-TEFb complex, which is necessary for transcription elongation beyond promoter-proximal pause sites, thereby reducing transcription initiation where TFIIA is active. Lastly, Brefeldin A disrupts intracellular trafficking, which indirectly leads to TFIIA inhibition by affecting the transport and localization of essential transcription factors and co-factors.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Triptolide | 38748-32-2 | sc-200122 sc-200122A | 1 mg 5 mg | $90.00 $204.00 | 13 | |
Triptolide inhibits the transcriptional activity of TFIIA by interfering with the assembly of the transcriptional machinery at the promoter of DNA, directly impeding the binding of TFIIA to the DNA complex. | ||||||
α-Amanitin | 23109-05-9 | sc-202440 sc-202440A | 1 mg 5 mg | $269.00 $1050.00 | 26 | |
α-Amanitin targets RNA polymerase II, the enzyme responsible for mRNA synthesis. Since TFIIA is a transcription factor that forms a complex with RNA polymerase II during the initiation of transcription, inhibition of RNA polymerase II by α-Amanitin would result in a functional inhibition of TFIIA by preventing its role in transcription initiation. | ||||||
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 binds to the minor groove of DNA and can prevent transcription factor binding, including TFIIA. By blocking the access of TFIIA to its DNA binding sites, DrB functionally inhibits the activity of TFIIA in the transcription initiation complex. | ||||||
Flavopiridol Hydrochloride | 131740-09-5 | sc-207687 | 10 mg | $317.00 | ||
Flavopiridol inhibits CDK9, a component of the positive transcription elongation factor b (P-TEFb), which is required for transcription elongation past the promoter-proximal pause site. Since TFIIA is involved in the early stages of transcription initiation, inhibition of P-TEFb indirectly results in reduced transcription initiation and hence functional inhibition of TFIIA. | ||||||
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 at the transcription initiation complex and prevents the elongation of RNA chain by RNA polymerase II. This drug thereby inhibits the function of TFIIA which is part of the transcription initiation complex. | ||||||
Oxaliplatin | 61825-94-3 | sc-202270 sc-202270A | 5 mg 25 mg | $112.00 $394.00 | 8 | |
Oxaliplatin forms DNA adducts and cross-links within the DNA, which can impede transcription factor binding. By modifying the DNA structure and hindering the formation of the transcription initiation complex, oxaliplatin can inhibit the function of TFIIA. | ||||||
Camptothecin | 7689-03-4 | sc-200871 sc-200871A sc-200871B | 50 mg 250 mg 100 mg | $58.00 $186.00 $94.00 | 21 | |
Camptothecin inhibits the enzyme topoisomerase I, which is required for DNA unwinding. By stabilizing the complex between topoisomerase I and DNA, it prevents the relaxation of supercoiled DNA, which is necessary for transcription to proceed, thereby indirectly inhibiting TFIIA function. | ||||||
Etoposide (VP-16) | 33419-42-0 | sc-3512B sc-3512 sc-3512A | 10 mg 100 mg 500 mg | $51.00 $231.00 $523.00 | 63 | |
Etoposide inhibits topoisomerase II, leading to DNA breaks and the disruption of transcription. As TFIIA is involved in transcription initiation, its function is inhibited by the impediment in the transcription process caused by etoposide-induced DNA damage. | ||||||
Mitoxantrone | 65271-80-9 | sc-207888 | 100 mg | $285.00 | 8 | |
Mitoxantrone intercalates into DNA and inhibits topoisomerase II, causing DNA breaks and halting transcription processes. This inhibits the function of TFIIA by preventing the assembly of transcription initiation complexes at promoter sites. | ||||||
Cordycepin | 73-03-0 | sc-203902 | 10 mg | $101.00 | 5 | |
Cordycepin, a nucleoside analog, terminates the RNA chain elongation by RNA polymerase II. As TFIIA is a transcription initiation factor, the premature termination of the RNA chain indirectly inhibits the function of TFIIA by halting the process it initiates. | ||||||