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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V53399 | Tazemetostat de(methylene morpholine)-O-C3-OC-COOH | 2750350-39-9 | Tazemetostat de(methylene morpholine)-O-C3-OC-COOH (Compound 21b) is an EZH2 degrader that may be utilized in lymphoma research. |
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V56077 | TNG-462 | 2760483-96-1 | TNG-462 (Compound 1143) is an orally bioavailable PRMT5 inhibitor for research into MTAP-deficient and/or MTA-accumulating cancers. |
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V51603 | TNG-908 | 2760481-53-4 | TNG908 is a MTAP-good PRMT5 that can pass the BBB (blood-brain barrier). |
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V16651 | TP-064 | 2080306-20-1 | TP-064 is a potent and specific protein arginine methyltransferase 4 (PRMT4; CARM1) inhibitor (IC50 <10 nM). |
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V56080 | Tulmimetostat (CPI-0209) | 2567686-02-4 | Tulmimetostat (CPI-0209) is an orally bioactive EZH1/EZH2 inhibitor. |
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V3452 | UNC0224 | 1197196-48-7 | UNC0224 (UNC-0224) is a novel, potent and selective G9a histone methyltransferase inhibitor with anticancer activity. |
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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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V0427 | UNC1215 | 1415800-43-9 | UNC1215 (UNC-1215) is a potent and selectiveantagonist of L3MBTL3, a member of the MBT (malignant brain tumor) family of methyllysine (Kme) reading domain, with potential antineoplastic activity. |
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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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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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