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Histone Methyltransferase

Histone Methyltransferase

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.

Histone Methyltransferase related products

Structure Cat No. Product Name CAS No. Product Description
UNC0321 V3453 UNC0321 1238673-32-9 UNC0321 (UNC-0321) is a novel, potent and selective G9a histone methyltransferaseinhibitor with anticancer activity.
UNC0379 V0392 UNC0379 1620401-82-2 UNC0379 is a substrate competitive lysine methyltransferase SETD8 (KMT5A) inhibitorwith antineoplastic activity.
UNC0631 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.
UNC0638 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.
UNC0642 V3137 UNC0642 1481677-78-4 UNC0642 (UNC-0642) is a novel, potent, selective, dual inhibitor ofG9a/GLP (histone methyltransferases) with antitumor activity.
UNC0646 V2057 UNC0646 1320288-17-2 UNC0646 is a novel, potent and selective histone methyltransferase G9a inhibitor with IC50 of 6 nM.
UNC1999 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.
UNC2399 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.
UNC3866 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.
UNC3866 TFA V94308 UNC3866 TFA 1872382-48-3 UNC3866 TFA is a potent CBX7-H3 antagonist with IC50 of 66±1.2 nM.
UNC4976 V75864 UNC4976 2920299-34-7 UNC4976 is a nucleic acid-binding PAM (positive allosteric modulator) peptidomimetic of the CBX7 chromatin domain.
UNC4976 TFA V76388 UNC4976 TFA UNC4976 TFA is a nucleic acid-binding PAM (positive allosteric modulator) peptidomimetic of the CBX7 chromatin domain.
UNC6852 V40758 UNC6852 UNC6852 is a selective PRC2 degrader based on PROTAC technology.
UNC6852 V35159 UNC6852 2688842-08-0 UNC6852 is a selective PRC2 degrader based on PROTAC technology.
UNC6934 V53045 UNC6934 2561494-77-5 UNC6934 is a chemical probe targeting the PWWP domain of NSD2, which localizes to the nucleolus.
UNC7145 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.
UNC8153 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.
UNC8153 TFA 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.
UZH2 V50975 UZH2 2756566-45-5 UZH2 is a potent and specific METTL3 inhibitor (antagonist) with IC50 of 5 nM.
W4275 V97159 W4275 3051650-00-8 W4275 (Compound 42) is an orally active and selective NSD2 inhibitor with IC50 of 17 nM.
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