ENL Activators
ENL Activators are a collection of chemical compounds that serve to enhance the functional activity of the protein ENL through a variety of intracellular signaling pathways and biochemical mechanisms. For instance, compounds such as Bisindolylmaleimide I and 8-Bromo-cAMP function by inhibiting PKC and activating PKA, respectively, which can alter the phosphorylation state and thereby the functional activity of ENL, promoting its role in transcriptional regulation. Similarly, Trichostatin A and Sodium Butyrate, both HDAC inhibitors, leadto an open chromatin structure, which may enhance the recruitment and activity of ENL in modulating transcription. By inhibiting protein degradation, MG132 helps in sustaining ENL levels within the cell, which is crucial for maintaining its transcriptional coactivation activity. 5-Azacytidine, through its DNA methyltransferase inhibitory action, activates genes that facilitate ENL recruitment to chromatin, thereby enhancing ENL's transcriptional coactivation functions.
The activity of ENL is further refined through the modulation of cellular energy dynamics and kinase signaling pathways. Oligomycin A, by inhibiting ATP synthesis, triggers AMPK activation, which can lead to subtle shifts in transcriptional regulation and consequently augment ENL's role as a coactivator. Kinase inhibitors such as ZM 336372, PD 98059, SB 203580, and Y-27632, each act upon distinct kinases like RAF, MEK, p38 MAPK, and ROCK, respectively, and modulate various signaling pathways that impact the transcriptional machinery. The inhibition of these kinases can lead to a favorable environment for ENL's coactivator function by modulating the phosphorylation patterns of transcription factors and coactivators. Additionally, Forskolin, by raising intracellular cAMP levels, indirectly enhances ENL's function by promoting a favorable phosphorylation status through PKA activation. These chemical activators, through their targeted actions, serve to potentiate ENL's role in transcriptional regulation, expanding its capacity to interact with chromatin and transcription factors without necessitating an increase in ENL expression or direct activation.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Bisindolylmaleimide I (GF 109203X) | 133052-90-1 | sc-24003A sc-24003 | 1 mg 5 mg | $103.00 $237.00 | 36 | |
Bisindolylmaleimide I is a potent and selective inhibitor of protein kinase C (PKC). PKC has been implicated in the phosphorylation of ENL, influencing its interaction with transcriptional machinery. Through the inhibition of PKC, Bisindolylmaleimide I may enhance the role of ENL in transcriptional regulation by stabilizing its association with chromatin. | ||||||
8-Bromo-cAMP | 76939-46-3 | sc-201564 sc-201564A | 10 mg 50 mg | $97.00 $224.00 | 30 | |
8-Bromo-cAMP is a cell-permeable cAMP analog that activates protein kinase A (PKA). PKA phosphorylation can influence transcriptional coactivators such as ENL by modulating their binding to transcription factors and chromatin. This activation can, therefore, enhance the function of ENL as a transcriptional coactivator. | ||||||
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 | $149.00 $470.00 $620.00 $1199.00 $2090.00 | 33 | |
Trichostatin A is a histone deacetylase (HDAC) inhibitor. HDACs typically repress transcription by condensing chromatin structure. By inhibiting HDACs, Trichostatin A can lead to a more relaxed chromatin state, potentially enhancing ENL's ability to interact with transcriptional activation complexes. | ||||||
MG-132 [Z-Leu- Leu-Leu-CHO] | 133407-82-6 | sc-201270 sc-201270A sc-201270B | 5 mg 25 mg 100 mg | $56.00 $260.00 $980.00 | 163 | |
MG132 is a proteasome inhibitor. By preventing protein degradation, MG132 may indirectly enhance the function of ENL by maintaining its levels within the cell, promoting its transcriptional coactivation activity. | ||||||
5-Azacytidine | 320-67-2 | sc-221003 | 500 mg | $280.00 | 4 | |
5-Azacytidine is a DNA methyltransferase inhibitor. By inducing hypomethylation of DNA, it can activate genes that may be involved in the recruitment and function of ENL, enhancing its role in chromatin interaction and transcriptional activation. | ||||||
Oligomycin A | 579-13-5 | sc-201551 sc-201551A sc-201551B sc-201551C sc-201551D | 5 mg 25 mg 100 mg 500 mg 1 g | $175.00 $600.00 $1179.00 $5100.00 $9180.00 | 26 | |
Oligomycin A is an ATP synthase inhibitor. By inhibiting ATP production, it causes AMPK activation, which can lead to changes in transcriptional dynamics. This shift could potentially enhance the transcriptional coactivator function of ENL by altering its interaction with transcriptional machinery. | ||||||
ZM 336372 | 208260-29-1 | sc-202857 | 1 mg | $46.00 | 2 | |
ZM 336372 is a RAF kinase inhibitor. By inhibiting RAF, it can lead to alterations in the MAPK/ERK pathway, which may indirectly enhance the function of ENL in transcription regulation by affecting the phosphorylation status of transcription factors and coactivators. | ||||||
PD 98059 | 167869-21-8 | sc-3532 sc-3532A | 1 mg 5 mg | $39.00 $90.00 | 212 | |
PD 98059 is an inhibitor of MEK, which operates upstream in the MAPK/ERK pathway. By inhibiting MEK, PD 98059 can alter the phosphorylation of downstream targets that interact with ENL, enhancing its coactivator function. | ||||||
SB 203580 | 152121-47-6 | sc-3533 sc-3533A | 1 mg 5 mg | $88.00 $342.00 | 284 | |
SB 203580 is a specific inhibitor of p38 MAPK. Inhibition of p38 may enhance the activity of transcriptional coactivators like ENL by affecting the phosphorylation status of factors that recruit ENL to chromatin. | ||||||
Y-27632, free base | 146986-50-7 | sc-3536 sc-3536A | 5 mg 50 mg | $182.00 $693.00 | 88 | |
Y-27632 is a selective inhibitor of ROCK kinases. By inhibiting ROCK, it may affect cytoskeletal dynamics, which can influence nuclear processes including transcription. This may indirectly enhance ENL's interaction with transcriptional machinery. | ||||||