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Epigenetic Reader Domain

Epigenetic Reader Domain

Epigenetic regulators of gene expression and chromatin state include so-called writers, erasers, and readers of chromatin modifications.The chromo and bromo domains, which typically bind acetyllysine, the malignant brain tumor (MBT), the plant homeodomain (PHD), and Tudor domains, which typically associate with methyllysine, are well-known examples of reader domains. The identification of selective inhibitors that specifically target members of the bromodomain and extraterminal motif (BET) family of acetyl-lysine readers has had a significant impact on research on epigenetic readers. 46 proteins, containing 61 bromodomains grouped into eight families, are encoded by the human genome. The first BET inhibitors, GSK 525762A and (+)-JQ-1, are discovered using various experimental methods.

Enhancer of zeste homologue 2 (EZH2), a protein from the Polycomb group (PcG), is crucial for promoting histone H3 lysine 27 trimethylation (H3K27me3) and epigenetic gene silencing. This EZH2 function is crucial for cell proliferation, inhibits cell differentiation, and may contribute to the development of cancer. By phosphorylating EZH2, cyclin-dependent kinases control epigenetic gene silencing. Tumor suppressor genes are thought to be silenced by abnormal histone and DNA methylation caused by EZH2 in many cancer types, including lymphomas and leukemia.

In addition to acting as a transcriptional adaptor, p300/CBP also acts as a histone acetyltransferase.

Epigenetic Reader Domain related products

Structure Cat No. Product Name CAS No. Product Description
(+)-JQ-1-aldehyde V53049 (+)-JQ-1-aldehyde 2634778-37-1 (+)-JQ-1-aldehyde is the aldehyde form of (+)-JQ1.
(+)-JQ1 V0411 (+)-JQ1 1268524-70-4 (+)-JQ1 is a novel, potent and highly specific BET (Bromodomain and extra terminal domain) bromodomain inhibitor with antineoplastic activity.
(+)-JQ1 PA V3741 (+)-JQ1 PA 2115701-93-2 (+)-JQ1 PA (also known as (+)-JQ1 propargyl amide) is a novel propargyl amide derivative of (+)-JQ1 with IC50of 10.4 nM for Bromodomain and extra-terminal(BET).
(1s,4s)-Menin-MLL inhibitor-23 V77414 (1s,4s)-Menin-MLL inhibitor-23 (1s,4s)-Menin-MLL inhibitor-23 is the enantiomer of Menin-MLL inhibitor-23.
(6s)-4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-f][1,2,4]噻唑并[4,3-a][1,4]二氮杂卓-6-乙酸 V3740 (+)-JQ1 carboxylic acid 202592-23-2 (+)-JQ1 carboxylic acid is the free carboxylic acid (COOH) form of (+)-JQ1 (tert-Butyl ester form-COOtBu).
(R)-BAY1238097 V4201 (R)-BAY1238097 1564269-85-7 R)-BAY1238097 is the R-isomer of BAY-1238097 with lower activity than BAY1238097.
(S)-Bleximenib oxalate ((S)-Menin-MLL inhibitor 24 oxalate) V77361 (S)-Bleximenib oxalate ((S)-Menin-MLL inhibitor 24 oxalate) (S)-Bleximenib ((S)-Menin-MLL inhibitor 24) oxalate is the S-enantiomer of (S)-Menin-MLL inhibitor 24 oxalate.
(S)-GNE-987 V56124 (S)-GNE-987 2738533-33-8 (S)-GNE-987 (compound 4), the hydroxyproline epimer of GNE-987 (BET degrader), can eliminate the binding to von Hippel-Lindau and cannot degrade BRD4 protein.
(S,R)-CFT8634 V56138 (S,R)-CFT8634 2704617-95-6 (S,R)-CFT8634 is a selective and orally bioactive BRD9 protein degrader.
(Z)-JQ1-TCO V88857 (Z)-JQ1-TCO JQ1-TCO (JQ1-trans-cycloctene) is a derivative of the BET inhibitor JQ1.
(±)-JQ1 V101132 (±)-JQ1 1268524-69-1 (±)-JQ1 is the racemate of (+)-JQ-1.
3-Methylcarbostyril V89507 3-Methylcarbostyril 2721-59-7 3-Mmethylcarbostyril (compound 5) is a BRD4 BD1 inhibitor with pIC50 of 4.4.
6-O-Isobutyrylbritannilactone V52483 6-O-Isobutyrylbritannilactone 1259933-02-2 6-O-Isobutyrylbritannilactone is a natural melanogenesis inhibitor.
653-47 V52488 653-47 1224678-75-4 653-47 is an enhancer that significantly enhances the cAMP response element binding protein (CREB) inhibitory activity of 666-15.
653-47 hydrochloride V52487 653-47 hydrochloride 1224567-46-7 653-47 HCl is an enhancer that significantly enhances the cAMP response element binding protein (CREB) inhibitory activity of 666-15.
666-15 V5228 666-15 1433286-70-4 666-15 is a novel, cell-permeable, potent and selective inhibitor ofCREB (cAMP-response element binding protein)-mediated gene transcription with IC50 of 81 nM.
7-O-Methylaloesinol V81843 7-O-Methylaloesinol 105317-69-9 7-O-Methylaloesinol is a pigment analogue.
ABBV-744 V4567 ABBV-744 2138861-99-9 ABBV-744 (ABBV744) is a novel, potent and highlyBDII-selective BET bromodomaininhibitor with anticancer and anti-inflammatory activity.
ACBI2 V52455 ACBI2 2913161-19-8 ACBI2 is a potent and orally bioactive VHL PROTAC SMARCA2 degrader (EC50= 7 nM) that degrades SMARCA2 (DC50= 1 nM in RKO cells).
Amredobresib (BI894999) V56120 Amredobresib (BI894999) 1610044-98-8 Amredobresib is a potent BET inhibitor.
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