BC032203 Activators
Chemical activators of BRD4IN-B can influence the protein's activity through various interactions with chromatin structure and histone modifications. Trichostatin A and MS-275 act as histone deacetylase inhibitors, increasing the acetylation levels of histone proteins, thereby creating a more accessible chromatin state that can facilitate BRD4IN-B to bind acetylated histones and carry out its chromatin remodeling functions. On the other hand, JQ1, (+)-JQ1, I-BET151, CPI-0610, OTX015, PFI-1, RVX-208, and GSK525762 function by inhibiting the bromodomains of BRD4, a protein closely associated with chromatin. The displacement of BRD4 from the chromatin by these small molecules creates a scenario where BRD4IN-B's role becomes more prominent, as it is then recruited to carry out the necessary chromatin remodeling activities, compensating for the inhibited action of BRD4.
Additionally, LMK-235, by inhibiting histone deacetylase, can also lead to increased histone acetylation, which in turn can promote the association of BRD4IN-B with chromatin due to its affinity for acetylated lysine residues. PF-CBP1, which selectively inhibits the CREBBP/EP300 bromodomains, creates a similar effect by indirectly enhancing the role of BRD4IN-B in maintaining chromatin structure and function. These chemical activators, through their unique mechanisms, can lead to a state where the chromatin remodeling capabilities of BRD4IN-B are essential to sustain the dynamic nature of chromatin, ensuring the accessibility of genetic information for various cellular processes.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
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 a histone deacetylase inhibitor that promotes acetylation of histones, leading to a relaxed chromatin structure. This relaxed state can facilitate BRD4 interacting chromatin remodeling complex associated protein like (BRD4IN-B) to access and bind acetylated histones, thereby activating its chromatin remodeling function. | ||||||
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 interferes with the binding of BRD4 to acetylated histones. The inhibition of BRD4 can trigger a feedback mechanism where BRD4IN-B is upregulated and becomes more active to maintain chromatin responses. | ||||||
(±)-JQ1 | 1268524-69-1 | sc-472932 sc-472932A | 5 mg 25 mg | $231.00 $863.00 | 1 | |
(+)-JQ1 is the enantiomer of JQ1 with higher specificity and affinity for BRD4 bromodomains. Binding of (+)-JQ1 to BRD4 leads to the dissociation of BRD4 from chromatin, potentially increasing the recruitment and activation of BRD4IN-B for chromatin remodeling and transcriptional regulation. | ||||||
MS-275 | 209783-80-2 | sc-279455 sc-279455A sc-279455B | 1 mg 5 mg 25 mg | $24.00 $90.00 $212.00 | 24 | |
MS-275, also known as Entinostat, is a selective histone deacetylase inhibitor that leads to hyperacetylation of histones. Hyperacetylated histones can enhance the activity of BRD4IN-B as it interacts with acetylated lysine residues, promoting chromatin remodeling. | ||||||
CPI-0610 | 1380087-89-7 | sc-507490 | 10 mg | $495.00 | ||
CPI-0610 is a potent BET bromodomain inhibitor that selectively disrupts the interaction of BRD4 with chromatin. The subsequent alteration in chromatin dynamics can lead to the enhanced recruitment and activation of BRD4IN-B to help sustain necessary chromatin functions. | ||||||
(S)-2-(4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(4-hydroxyphenyl)acetamide | 202590-98-5 | sc-501130 | 2.5 mg | $330.00 | ||
OTX015, also known as MK-8628, is a small molecule inhibitor targeting the BET family of bromodomains. By inhibiting BRD4, OTX015 may lead to the compensatory activation of BRD4IN-B to fulfill essential chromatin remodeling roles. | ||||||
PFI-1 | 1403764-72-6 | sc-478504 | 5 mg | $98.00 | ||
PFI-1 is a BET bromodomain inhibitor that prevents BRD4 from associating with chromatin. This can enhance the necessity for BRD4IN-B's chromatin remodeling activity, effectively activating its function to compensate for the loss of BRD4 activity. | ||||||
RVX 208 | 1044870-39-4 | sc-472700 | 10 mg | $340.00 | ||
RVX-208, also known as Apabetalone, is a small molecule that targets BET bromodomains. It can perturb the normal function of BRD4, potentially leading to the activation of alternative chromatin remodeling complexes including BRD4IN-B. | ||||||
GSK 525762A | 1260907-17-2 | sc-490339 sc-490339A sc-490339B sc-490339C sc-490339D | 5 mg 10 mg 50 mg 100 mg 1 g | $300.00 $540.00 $940.00 $1680.00 $5900.00 | ||
GSK525762, also known as I-BET762, is a BET bromodomain inhibitor that can disrupt the interaction between BRD4 and chromatin. This disruption may lead to the activation of BRD4IN-B as it may be required to facilitate chromatin remodeling in the absence of BRD4. | ||||||