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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
SRG-II-19F (dCym-JQ1) V81433 SRG-II-19F (dCym-JQ1) SRG-II-19F (dCym-JQ1) is a BRDT bromodomain1 (BRDTBD1) PROTAC degrader.
SRX3177 V55083 SRX3177 2241237-51-2 SRX3177 is a triple inhibitor of CDK4/6, PI3K and BRD4, with IC50 of 33 nM (BRD4 BD1), 89 nM (BRD4 BD2), 79 nM (PI3Kα), 83 nM (PI3Kδ), 3.18 μM (PI3Kγ), < 2.5 nM (CDK4), 3.3 nM (CDK6).
TCIP 1 V76446 TCIP 1 TCIP 1 is a transcriptional/epigenetic CIP (TCIP) small molecule, consisting of small molecules covalently linked to BCL6 and BRD4, respectively.
Thalidomide-NH-C4-NH-Boc V40173 Thalidomide-NH-C4-NH-Boc 2093388-52-2 Thalidomide-NH-C4-NH-Boc (compound 15) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
Thalidomide-NH-CBP/p300 ligand 2 V53334 Thalidomide-NH-CBP/p300 ligand 2 2484739-21-9 Thalidomide-NH-CBP/p300 ligand 2 (P-007) is a PROTAC protein degrader of CBP and p300.
TMX1 V76407 TMX1 TMX1 is a BRD4 covalent molecular glue degrader.
TP-238 V35176 TP-238 2415263-04-4 TP-238 is a potent and specific CECR2/BPTF dual probe with IC50s of 30 nM and 350 nM respectively.
TP-238 hydrochloride V35175 TP-238 hydrochloride 2415263-05-5 TP-238 HCl is an effective and selective CECR2/BPTF dual probe with IC50s of 30 nM and 350 nM respectively.
TP-472 V40712 TP-472 2079895-62-6 TP-472 is a selective BRD9/7 inhibitor (antagonist) with Kds of 33 nM and 340 nM for BRD9 and BRD7, respectively.
TRIM24/BRPF1-IN-2 V79846 TRIM24/BRPF1-IN-2 TRIM24/BRPF1-IN-2 (compound 20l) is a potent dual TRIM24/BRPF1 inhibitor (antagonist) with IC50s of 0.98 and 1.16 μM respectively.
Trotabresib (CC-90010; compound 1) V50954 Trotabresib (CC-90010; compound 1) 1706738-98-8 CC-90010 (compound 1) is a reversible, orally bioactive BET inhibitor.
Tz-Thalidomide V53254 Tz-Thalidomide 2087490-42-2 Tz-Thalidomide is a tetrazine-tagged Thalidomide , an E3 ligase ligand.
UMB298 V35161 UMB298 2266569-73-5 UMB298 is a potent and specific CBP/P300 bromodomain inhibitor.
UNC-926 V0086 UNC-926 1184136-10-4 UNC-926 is apotent and selective inhibitor of the L3MBTL1 (Lethal(3)malignant brain tumor-like protein)domain (Kd = 3.9 μM), which is a methyl-lysine (Kme) reader domain.
UNC1021 V53393 UNC1021 1322591-19-4 UNC1021 is a selective L3MBTL3 inhibitor (antagonist) with IC50 of 0.048 μM.
UNC669 V0426 UNC669 1314241-44-5 UNC669 (UNC-669) is a novel, potent and selective inhibitor of malignant brain tumor (MBT) with anticancer activity.
UNC926 hydrochloride V35158 UNC926 hydrochloride 1782573-49-2 UNC926 HCl is a methyl-lysine (Kme) reader domain inhibitor that specifically inhibits L3MBTL1 with IC50 of 3.9 μM.
VinSpinIn V56145 VinSpinIn 2380021-98-5 VinSpinIn is a Spindlin1 inhibitor (KD: 9.9 nM for SPIN149-262).
WWL0245 V35119 WWL0245 2869057-11-2 WWL0245 is a potent and specific BRD4 PROTAC.
XL-126 V83729 XL-126
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