Jumonji Inhibitors
Jumonji inhibitors are a class of chemical compounds that target Jumonji domain-containing proteins, which are a subgroup of the histone demethylase family. These enzymes are involved in the removal of methyl groups from histones, specifically at lysine residues, influencing chromatin structure and gene expression. Jumonji proteins contain a catalytic Jumonji C (JmjC) domain, which requires iron (Fe²⁺) and alpha-ketoglutarate (α-KG) as cofactors to catalyze oxidative demethylation reactions. By modulating the activity of these enzymes, Jumonji inhibitors influence the methylation status of histones, leading to alterations in chromatin accessibility and the transcriptional activity of specific genes. The chemical structures of Jumonji inhibitors often mimic α-KG or interfere with Fe²⁺ binding to inhibit the catalytic function of the JmjC domain.
The inhibition of Jumonji demethylases leads to the retention of methyl groups on histones, generally resulting in transcriptional repression of genes marked by these modifications. This has significant implications for controlling gene expression programs associated with cell differentiation, proliferation, and other essential cellular processes. Jumonji inhibitors vary in their specificity, with some targeting a broad range of Jumonji proteins, while others exhibit selectivity for particular members within the family. The chemical properties of these inhibitors are designed to optimize their binding to the JmjC domain, utilizing structural motifs that block the enzyme's active site or destabilize its interaction with necessary cofactors. Researchers use Jumonji inhibitors to explore epigenetic regulation mechanisms and study chromatin dynamics.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Dimethyloxaloylglycine (DMOG) | 89464-63-1 | sc-200755 sc-200755A sc-200755B sc-200755C | 10 mg 50 mg 100 mg 500 mg | $84.00 $301.00 $374.00 $779.00 | 25 | |
DMOG inhibits prolyl hydroxylases, leading to the stabilization of HIF-1α. Stabilized HIF-1α may downregulate Jumonji protein expression by altering transcriptional programs in response to hypoxia, which is known to reshape chromatin landscapes and gene expression profiles. | ||||||
Disulfiram | 97-77-8 | sc-205654 sc-205654A | 50 g 100 g | $53.00 $89.00 | 7 | |
Disulfiram has the ability to chelate copper, which is a cofactor for some Jumonji demethylases. By sequestering copper, Disulfiram could decrease the catalytic efficiency of these enzymes, potentially resulting in the reduced expression of Jumonji proteins due to compromised enzymatic activity. | ||||||
5-Aza-2′-Deoxycytidine | 2353-33-5 | sc-202424 sc-202424A sc-202424B | 25 mg 100 mg 250 mg | $218.00 $322.00 $426.00 | 7 | |
As a DNA methyltransferase inhibitor, 5-Aza-2′-deoxycytidine can induce genome-wide hypomethylation, which could theoretically lead to the reactivation of epigenetically silenced genes that suppress Jumonji protein expression, thereby reducing the levels of Jumonji proteins. | ||||||
Parthenolide | 20554-84-1 | sc-3523 sc-3523A | 50 mg 250 mg | $81.00 $306.00 | 32 | |
Parthenolide, through its inhibition of the NF-κB pathway, could decrease the transcription of NF-κB target genes that may include those encoding Jumonji proteins, resulting in the reduced expression of these proteins. | ||||||
Suberoylanilide Hydroxamic Acid | 149647-78-9 | sc-220139 sc-220139A | 100 mg 500 mg | $133.00 $275.00 | 37 | |
Vorinostat, as a histone deacetylase inhibitor, could promote the acetylation of histones, thereby enhancing chromatin accessibility. This could lead to the downregulation of Jumonji protein expression if the chromatin changes make the Jumonji gene loci less permissive for transcription. | ||||||
Retinoic Acid, all trans | 302-79-4 | sc-200898 sc-200898A sc-200898B sc-200898C | 500 mg 5 g 10 g 100 g | $66.00 $325.00 $587.00 $1018.00 | 28 | |
Retinoic acid, by binding to its receptors, can initiate a cascade of transcriptional events that repress the transcription of genes encoding Jumonji proteins, thus reducing their expression. | ||||||
Genistein | 446-72-0 | sc-3515 sc-3515A sc-3515B sc-3515C sc-3515D sc-3515E sc-3515F | 100 mg 500 mg 1 g 5 g 10 g 25 g 100 g | $45.00 $164.00 $200.00 $402.00 $575.00 $981.00 $2031.00 | 46 | |
Genistein, a tyrosine kinase inhibitor, could disrupt cellular signaling pathways that, when activated, result in increased expression of Jumonji proteins. By inhibiting these kinases, Genistein could decrease Jumonji protein expression. | ||||||
Curcumin | 458-37-7 | sc-200509 sc-200509A sc-200509B sc-200509C sc-200509D sc-200509F sc-200509E | 1 g 5 g 25 g 100 g 250 g 1 kg 2.5 kg | $37.00 $69.00 $109.00 $218.00 $239.00 $879.00 $1968.00 | 47 | |
Curcumin has been observed to inhibit the activation of various transcription factors such as NF-κB and AP-1, which could lead to the decreased expression of Jumonji proteins if these factors drive Jumonji gene transcription. | ||||||
(−)-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 | $43.00 $73.00 $126.00 $243.00 $530.00 $1259.00 | 11 | |
EGCG might downregulate Jumonji protein expression by inhibiting the activity of DNA methyltransferases and histone acetyltransferases, leading to alterations in the chromatin structure that render the Jumonji gene less active. | ||||||
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, a potent histone deacetylase inhibitor, could induce hyperacetylation of histones, potentially leading to the downregulation of Jumonji protein expression by modifying the transcriptional accessibility of genes involved in the expression of these proteins. | ||||||