NSD2 Inhibitors
NSD2 inhibitors are a class of chemical compounds specifically designed to target and inhibit the function of NSD2, also known as WHSC1 or MMSET. NSD2 is a histone methyltransferase enzyme that plays a critical role in epigenetic regulation by catalyzing the methylation of histone H3 on lysine 36 (H3K36). This post-translational modification is crucial for regulating chromatin structure and gene expression. NSD2 is involved in various cellular processes, including transcriptional activation, DNA repair, and chromatin remodeling, by modifying the histone code, which in turn affects the accessibility of the DNA to transcription factors and other regulatory proteins. By inhibiting NSD2, researchers can disrupt these epigenetic modifications, providing a powerful tool to study the specific contributions of NSD2 to gene regulation and chromatin dynamics.
In research, NSD2 inhibitors are valuable for exploring the role of histone methylation in gene expression and understanding how NSD2-mediated methylation affects chromatin structure and function. By blocking NSD2 activity, scientists can investigate how the loss of H3K36 methylation impacts the transcriptional landscape of cells, including the activation or repression of specific genes. These inhibitors also allow researchers to study the broader implications of NSD2 inhibition on cellular processes such as DNA damage response, where histone modifications play a crucial role in the recruitment and activity of repair proteins. Additionally, NSD2 inhibitors provide insights into the interactions between NSD2 and other chromatin-modifying enzymes, helping to unravel the complex networks of protein-protein interactions that regulate epigenetic states and cellular identity. Through these studies, the use of NSD2 inhibitors enhances our understanding of the molecular mechanisms underlying epigenetic regulation, the importance of histone methylation in maintaining chromatin integrity, and the broader consequences of epigenetic alterations on cellular function and development.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Chaetocin | 28097-03-2 | sc-200893 | 200 µg | $126.00 | 5 | |
Chaetocin is a histone methyltransferase inhibitor, known to target the SUV39H1 but may have off-target effects on NSD2. | ||||||
Histone Lysine Methyltransferase Inhibitor Inhibitor | 935693-62-2 (free base) | sc-202651 | 5 mg | $151.00 | 4 | |
BIX-01294 primarily inhibits G9a and GLP histone methyltransferases but may exhibit indirect effects on NSD2 activity. | ||||||
UNC0638 | 1255580-76-7 | sc-397012 | 10 mg | $315.00 | ||
UNC0638 is an inhibitor of G9a and GLP, and its broad action on histone methyltransferases might influence NSD2. | ||||||
Epz004777 | 1338466-77-5 | sc-507560 | 100 mg | $575.00 | ||
EPZ004777 targets DOT1L, another histone methyltransferase, and could have indirect effects on NSD2's function. | ||||||
9-[5-Deoxy-5-[[cis-3-[2-[6-(1,1-dimethylethyl)-1H-benzimidazol-2-yl]ethyl]cyclobutyl](1-methylethyl)amino]-β-D-ribofuranosyl]-9H-purin-6-amine | 1380288-87-8 | sc-500607 | 50 mg | $13500.00 | ||
EPZ5676, a DOT1L inhibitor, might indirectly affect NSD2 activity through broader histone methylation changes. | ||||||
GSK343 | 1346704-33-3 | sc-397025 sc-397025A | 5 mg 25 mg | $151.00 $461.00 | 1 | |
GSK343 is an EZH2 inhibitor, potentially influencing NSD2 through epigenetic regulation mechanisms. | ||||||
JIB 04 | 199596-05-9 | sc-397040 | 20 mg | $177.00 | ||
JIB-04 is a pan-histone demethylase inhibitor, potentially impacting NSD2 through broader histone modification changes. | ||||||
N-[3-[[2-[[4-[[1-(2-Fluoroethyl)-3-azetidinyl]amino]-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-2-propenamide | 1375465-09-0 | sc-499486 | 5 mg | $340.00 | ||
MM-102 is a WDR5-interacting protein inhibitor, potentially impacting NSD2 activity indirectly through protein-protein interactions. | ||||||