Histone modifications are essential for controlling both overall gene expression and stage-specific gene expression. While histones H3K9 and H3K27 are typically associated with gene repression, methylation on histones H3K4, H3K36, and H3K79 is typically associated with gene activation. Site-specific methyltransferases and demethylases dynamically control the methylation of histone lysines. The methylation of H3K27 in cells is carried out by EZH2 (the catalytic subunit of PRC2).
Inhibiting DOT1L, a histone H3 lysine 79 methyltransferase, improves the production of induced pluripotent stem cells (iPSCs). A powerful and specific DOT1L inhibitor, EPZ-5676.
The histone methyltransferase enhancer of zeste homolog 2 (EZH2) trimethylates histone 3's lysine 27 (H3K27me3), which results in chromatin condensation and transcriptional repression and is essential for PRC2 activity.
Structure | Cat No. | Product Name | CAS No. | Product Description |
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V3453 | UNC0321 | 1238673-32-9 | UNC0321 (UNC-0321) is a novel, potent and selective G9a histone methyltransferaseinhibitor with anticancer activity. |
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V0392 | UNC0379 | 1620401-82-2 | UNC0379 is a substrate competitive lysine methyltransferase SETD8 (KMT5A) inhibitorwith antineoplastic activity. |
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V0395 | UNC0631 | 1320288-19-4 | UNC0631 (UNC-0631) is a potent and selective inhibitor of histone methyltransferase G9a (KMT1C; EHMT2, IC50 = 4 nM)with antineoplastic activity. |
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V2603 | UNC0638 | 1255580-76-7 | UNC0638 (UNC-0638) is a selective and cell-permeable inhibitor of G9a histone methyltransferaseand GLP with IC50 of<15 nM and 19 nM, respectively. |
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V3137 | UNC0642 | 1481677-78-4 | UNC0642 (UNC-0642) is a novel, potent, selective, dual inhibitor ofG9a/GLP (histone methyltransferases) with antitumor activity. |
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V2057 | UNC0646 | 1320288-17-2 | UNC0646 is a novel, potent and selective histone methyltransferase G9a inhibitor with IC50 of 6 nM. |
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V0385 | UNC1999 | 1431612-23-5 | UNC1999 (UNC-1999) is an orally bioavailable, cell-permeable, selective, SAM-competitive and dual inhibitor of EZH2/EZH1 (Enhancer of zeste homolog) with antineoplastic activity. |
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V35160 | UNC2399 | 2412791-72-9 | UNC2399, a biotinylated UNC1999, is a selective EZH2 inhibitor (antagonist) with high in vitro potency against EZH2 with IC50 of 17 nM. |
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V2605 | UNC3866 | 1872382-47-2 | UNC3866 is a novel and potent antagonist of the methyllysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains with Kd of 100 nM as determined by AlphaScreen. |
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V94308 | UNC3866 TFA | 1872382-48-3 | UNC3866 TFA is a potent CBX7-H3 antagonist with IC50 of 66±1.2 nM. |
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V75864 | UNC4976 | 2920299-34-7 | UNC4976 is a nucleic acid-binding PAM (positive allosteric modulator) peptidomimetic of the CBX7 chromatin domain. |
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V76388 | UNC4976 TFA | UNC4976 TFA is a nucleic acid-binding PAM (positive allosteric modulator) peptidomimetic of the CBX7 chromatin domain. | |
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V40758 | UNC6852 | UNC6852 is a selective PRC2 degrader based on PROTAC technology. | |
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V35159 | UNC6852 | 2688842-08-0 | UNC6852 is a selective PRC2 degrader based on PROTAC technology. |
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V53045 | UNC6934 | 2561494-77-5 | UNC6934 is a chemical probe targeting the PWWP domain of NSD2, which localizes to the nucleolus. |
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V103441 | UNC7145 | 2561494-78-6 | UNC7145 is an inactive derivative of UNC6934 and serves as a negative control for the protein-protein inhibitory activity of UNC6934. |
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V93789 | UNC8153 | 2929304-60-7 | UNC8153 is a potent and selective nuclear receptor-binding SET domain 2 (NSD2) targeted degrader with Kd of 24 nM. |
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V75870 | UNC8153 TFA | 2929304-61-8 | UNC8153 TFA is a potent and specific nuclear receptor binding SET domain-containing 2 (NSD2) targeted degrader with a Kd of 24 nM. |
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V50975 | UZH2 | 2756566-45-5 | UZH2 is a potent and specific METTL3 inhibitor (antagonist) with IC50 of 5 nM. |
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V97159 | W4275 | 3051650-00-8 | W4275 (Compound 42) is an orally active and selective NSD2 inhibitor with IC50 of 17 nM. |