H3-K9-HMTase Activators
H3-K9-HMTase Activators are a unique class of compounds that function primarily by influencing the methylation of histone H3 at lysine 9 (H3K9). The compounds A-366, UNC0642, EPZ-6438, GSK126, UNC1999, EPZ-5676, and SGC0946 all interact with various histone methyltransferases (HMTs) that compete with H3-K9-HMTase for H3K9 methylation, thereby enhancing the activity of H3-K9-HMTase. By inhibiting these competing HMTs, the compounds effectively amplify the action of H3-K9-HMTase, leading to a change in the methylation status of H3K9 and the subsequent regulation of gene transcription.
Compounds like EPZ-6438 and GSK126 inhibit EZH2, another HMT that targets H3K9 for methylation. Inhibiting EZH2 can lead to enhanced activity of H3-K9-HMTase. Additionally, compounds such as EPZ-5676 and SGC0946 inhibit DOT1L, which although primarily associated with H3K79 methylation, could indirectly affect the availability of H3K9 for methylation by H3-K9-HMTase. The specificity of these compounds towards particular HMTs provides a unique and focused method of enhancing the functional activity of H3-K9-HMTase.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
UNC 0642 | 1481677-78-4 | sc-397059 | 10 mg | $235.00 | 3 | |
UNC0642 is a potent, selective and cell-penetrant chemical probe for G9a and GLP histone methyltransferases. By inhibiting these enzymes, UNC0642 can lead to enhanced activity of H3-K9-HMTase, which may regulate genes associated with H3K9 methylation. | ||||||
EPZ6438 | 1403254-99-8 | sc-507456 | 1 mg | $66.00 | ||
EPZ-6438 is an inhibitor of the histone methyltransferase EZH2. By inhibiting EZH2, which also targets H3K9 for methylation, EPZ-6438 can lead to enhanced activity of H3-K9-HMTase, thereby promoting the transcription of genes regulated by this histone modification. | ||||||
GSK126 | 1346574-57-9 | sc-490133 sc-490133A sc-490133B | 1 mg 5 mg 10 mg | $92.00 $243.00 $306.00 | ||
GSK126 is a highly selective EZH2 methyltransferase inhibitor. By inhibiting EZH2, GSK126 can enhance the activity of H3-K9-HMTase, leading to the regulation of genes associated with H3K9 methylation. | ||||||
UNC1999 | 1431612-23-5 | sc-475314 | 5 mg | $142.00 | 1 | |
UNC1999 is a potent, selective and cell-penetrant chemical probe for EZH2 and EZH1 histone methyltransferases. By inhibiting these enzymes, UNC1999 can lead to enhanced activity of H3-K9-HMTase, thereby promoting the transcription of genes regulated by this modification. | ||||||