NELF Activators
NELF Activators are a collection of chemical compounds designed to specifically influence the biochemical pathways and cellular processes that lead to the enhanced functional activity of NELF, a protein that regulates transcription elongation by pausing RNA polymerase II. Forskolin and Rolipram work synergistically to raise intracellular cAMP levels, thereby activating PKA, which in turn phosphorylates NELF, reducing its ability to pause RNA polymerase II. This results in an increase in transcription elongation for genes under the regulatory control of NELF. IBMX further potentiates this effect by non-selectively inhibiting phosphodiesterases, ensuring sustained cAMP levels and continuous PKA activity. Similarly, Epigallocatechin Gallate, through its inhibitory action on DNA methyltransferases, and 5-Azacytidine, by decreasing DNA methylation, render the chromatin more accessible to transcription machinery, effectively bypassing the need for direct NELF activation. PMA's activation of PKC leads to phosphorylation of the RNA polymerase II C-terminal domain, which may weaken NELF's interaction with the polymerase, facilitating transcriptional progression.
On a parallel note, Trichostatin A and S-Adenosylmethionine contribute to the activation of NELF-regulated genes by modulating chromatin structure and protein methylation, respectively, creating a transcriptionally conducive environment. Chlorophenylthio-cAMP, a cAMP analog, directly stimulates PKA, echoing the actions of Forskolin and Rolipram in diminishing NELF's repressive effects on transcription elongation. These chemicals act in concert to ensure that the regulatory influence of NELF on gene expression is modulated in such a way that allows for the enhanced transcription of NELF target genes, highlighting a diverse yet interconnected network of cellular signaling that governs NELF activity.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Forskolin | 66575-29-9 | sc-3562 sc-3562A sc-3562B sc-3562C sc-3562D | 5 mg 50 mg 1 g 2 g 5 g | $76.00 $150.00 $725.00 $1385.00 $2050.00 | 73 | |
Forskolin increases intracellular cAMP levels, which in turn activates PKA. PKA can phosphorylate NELF, leading to the release of NELF from paused RNA polymerase II complexes, thus enhancing transcription elongation. | ||||||
Rolipram | 61413-54-5 | sc-3563 sc-3563A | 5 mg 50 mg | $75.00 $212.00 | 18 | |
Rolipram is a selective inhibitor of phosphodiesterase 4 (PDE4), which breaks down cAMP. By inhibiting PDE4, Rolipram increases cAMP levels, which subsequently activates PKA. Activated PKA can then phosphorylate components of the NELF complex, leading to its dissociation from chromatin and an increase in transcription elongation of NELF target genes. | ||||||
IBMX | 28822-58-4 | sc-201188 sc-201188B sc-201188A | 200 mg 500 mg 1 g | $159.00 $315.00 $598.00 | 34 | |
Isobutylmethylxanthine (IBMX) is a non-selective inhibitor of phosphodiesterases, enzymes that degrade cAMP. Elevated cAMP levels activate PKA, which can lead to phosphorylation and inactivation of NELF, thereby enhancing transcription elongation of genes under NELF regulation. | ||||||
(−)-Epigallocatechin Gallate | 989-51-5 | sc-200802 sc-200802A sc-200802B sc-200802C sc-200802D sc-200802E | 10 mg 50 mg 100 mg 500 mg 1 g 10 g | $42.00 $72.00 $124.00 $238.00 $520.00 $1234.00 | 11 | |
Epigallocatechin gallate (EGCG) is a catechin found in green tea that has been shown to inhibit DNA methyltransferases. Hypomethylated gene promoters are more accessible to transcription machinery. By reducing promoter methylation, EGCG can enhance the transcription of genes where NELF is known to pause RNA polymerase II, thus increasing NELF-mediated transcription. | ||||||
PMA | 16561-29-8 | sc-3576 sc-3576A sc-3576B sc-3576C sc-3576D | 1 mg 5 mg 10 mg 25 mg 100 mg | $40.00 $129.00 $210.00 $490.00 $929.00 | 119 | |
Phorbol 12-myristate 13-acetate (PMA) activates protein kinase C (PKC), which can phosphorylate serine residues on RNA polymerase II C-terminal domain (CTD). Phosphorylation of RNA polymerase II CTD by PKC may reduce the ability of NELF to pause RNA polymerase, therefore enhancing transcription elongation. | ||||||
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 an inhibitor of histone deacetylases (HDAC). Inhibition of HDAC increases acetylation of histones, leading to a more open chromatin structure. This allows for greater access of RNA polymerase II to DNA, resulting in higher transcription levels of genes, including those that are regulated by NELF-mediated pausing. | ||||||
5-Azacytidine | 320-67-2 | sc-221003 | 500 mg | $280.00 | 4 | |
5-Azacytidine inhibits DNA methyltransferase, leading to decreased DNA methylation. Reduced methylation enhances the transcription of genes that are subject to NELF-mediated regulation by allowing greater access of the transcription machinery to DNA and reducing the recruitment of NELF to the promoter regions of these genes. | ||||||
Caffeine | 58-08-2 | sc-202514 sc-202514A sc-202514B sc-202514C sc-202514D | 5 g 100 g 250 g 1 kg 5 kg | $32.00 $66.00 $95.00 $188.00 $760.00 | 13 | |
Caffeine is a phosphodiesterase inhibitor, leading to increased cAMP levels. Elevated cAMP activates PKA, which can phosphorylate NELF, reducing its ability to pause RNA polymerase II, thus potentially increasing the transcription elongation process. | ||||||
Ademetionine | 29908-03-0 | sc-278677 sc-278677A | 100 mg 1 g | $180.00 $655.00 | 2 | |
S-Adenosylmethionine (SAM) serves as a methyl donor in various methylation reactions. By donating methyl groups, SAM can enhance the methylation of certain proteins that interact with NELF, potentially altering NELF's ability to pause RNA polymerase II and thus facilitating increased transcriptional activity. | ||||||