ZBRK1 Inhibitors
Chemical inhibitors of ZBRK1 interfere with its function by targeting the pathways and interactions essential for its role as a transcriptional co-repressor. Chetomin, for instance, disrupts the interaction between hypoxia-inducible factor-1 (HIF-1) and coactivator p300, a crucial step for ZBRK1 to exert its influence on gene expression under low oxygen conditions. Similarly, Echinomycin acts as a quinoxaline antibiotic that prevents HIF-1 from binding to its DNA consensus sequence, thereby impairing ZBRK1's capacity to collaborate with HIF-1 in gene regulation. Another inhibitor, YC-1, prevents the accumulation of HIF-1α, the subunit of HIF-1 that is essential for its activity. This suppression leads directly to a decreased ability for ZBRK1 to function effectively as a transcriptional repressor in cooperation with HIF-1.
Further inhibiting ZBRK1, LW6 promotes the degradation of HIF-1α, undercutting the ability of ZBRK1 to act as a co-repressor. PX-478 takes a similar yet distinct approach by inhibiting the expression of HIF-1α itself, thereby limiting the interaction between HIF-1α and ZBRK1. KC7F2 targets the protein synthesis of HIF-1α, which in turn diminishes ZBRK1's regulatory activities that depend on the presence of HIF-1α. Acriflavine adds to this suite of inhibitory mechanisms by preventing HIF-1 dimerization, a process necessary for ZBRK1 to function as a co-repressor. ML228 activates a cellular stress pathway under hypoxia that indirectly inhibits HIF-1α activity, consequently inhibiting ZBRK1's associated functions. Lastly, Topotecan and Etoposide, both topoisomerase inhibitors, create a context of DNA damage, where ZBRK1's role in DNA repair, through its interaction with BRCA1, is hindered, thus preventing ZBRK1 from performing its role in the maintenance of genomic stability.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Chidamide | 743420-02-2 | sc-364462 sc-364462A sc-364462B | 1 mg 5 mg 25 mg | $61.00 $245.00 $1173.00 | ||
Chetomin disrupts the interaction between hypoxia-inducible factor-1 (HIF-1) and the coactivator p300, a process ZBRK1 is involved in. By inhibiting this interaction, Chetomin can inhibit ZBRK1's ability to function as a transcriptional co-repressor in hypoxia-inducible gene expression. | ||||||
Quinomycin A | 512-64-1 | sc-202306 | 1 mg | $163.00 | 4 | |
Quinomycin A is a quinoxaline antibiotic that inhibits the binding of HIF-1 to its DNA consensus sequence. ZBRK1 collaborates with HIF-1 in gene regulation, and the inhibition of HIF-1 DNA binding by Echinomycin results in the functional inhibition of ZBRK1's co-repressor activity on hypoxia-responsive genes. | ||||||
YC-1 | 170632-47-0 | sc-202856 sc-202856A sc-202856B sc-202856C | 1 mg 5 mg 10 mg 50 mg | $32.00 $122.00 $214.00 $928.00 | 9 | |
YC-1 inhibits the HIF-1 pathway by preventing HIF-1α accumulation. Since ZBRK1 functions in tandem with HIF-1 in hypoxia-mediated transcriptional repression, the inhibition of HIF-1α by YC-1 can lead to a decrease in ZBRK1-mediated transcriptional repression. | ||||||
Hypoxia inducible factor-1α inhibitor | 934593-90-5 | sc-205346 sc-205346A sc-205346B sc-205346C | 1 mg 5 mg 10 mg 25 mg | $32.00 $112.00 $190.00 $403.00 | 40 | |
LW6 inhibits the accumulation of HIF-1α by promoting its degradation. As ZBRK1 activity is linked to the HIF-1 pathway, particularly under hypoxic conditions, the reduction of HIF-1α by LW6 impairs the functional ability of ZBRK1 to act as a co-repressor in this context. | ||||||
PX-478 | 685898-44-6 | sc-507409 | 10 mg | $175.00 | ||
PX-478 is an inhibitor of HIF-1α expression. Without the proper expression of HIF-1α, ZBRK1 cannot properly interact and modulate hypoxia-responsive gene transcription, thus PX-478 can lead to the functional inhibition of ZBRK1 by hindering its ability to engage in its co-repressive role with HIF-1α. | ||||||
Acriflavine | 8048-52-0 | sc-214489 sc-214489A | 25 g 100 g | $49.00 $168.00 | 2 | |
Acriflavine inhibits HIF-1 dimerization, and since ZBRK1's repressive function on certain genes is mediated through its interaction with HIF-1, inhibition of HIF-1 dimerization by Acriflavine can result in the functional inhibition of ZBRK1's ability to act as a transcriptional co-repressor. | ||||||
N-([1,1′-Biphenyl]-4-ylmethyl)-6-phenyl-3-(pyridin-2-yl)-1,2,4-triazin-5-amine | 1357171-62-0 | sc-503580 | 1 mg | $245.00 | ||
ML228 is an activator of the cellular stress pathway under hypoxic conditions, which indirectly leads to the inhibition of HIF-1α activity. ZBRK1 works in concert with HIF-1α, and thus, ML228's action on HIF-1α can inhibit the functional activities of ZBRK1 related to gene repression in hypoxic cells. | ||||||
Topotecan | 123948-87-8 | sc-338718 | 100 mg | $571.00 | ||
Topotecan inhibits topoisomerase I, an enzyme that relieves torsional stress in DNA during replication. ZBRK1 is known to interact with BRCA1, a protein involved in DNA damage repair where topoisomerase I plays a role. Inhibition of topoisomerase I by Topotecan could therefore impair ZBRK1's ability to participate in DNA repair processes. | ||||||
Etoposide (VP-16) | 33419-42-0 | sc-3512B sc-3512 sc-3512A | 10 mg 100 mg 500 mg | $32.00 $170.00 $385.00 | 63 | |
Etoposide is a topoisomerase II inhibitor which can prevent the religation of DNA strands, leading to DNA damage and affecting DNA repair pathways. ZBRK1 is involved in DNA damage response through its interaction with BRCA1 | ||||||