Epigenetic Reader Domain

Related Products

Epigenetic regulators of gene expression and chromatin state include so-called writers, erasers, and readers of chromatin modifications.Well-characterized examples of reader domains include bromodomains typically binding acetyllysine and chromatin organization modifier (chromo), malignant brain tumor (MBT), plant homeodomain (PHD), and Tudor domains generally associating with methyllysine. Research on epigenetic readers has been tremendously influenced by the discovery of selective inhibitors targeting the bromodomain and extraterminal motif (BET) family of acetyl-lysine readers. The human genome encodes 46 proteins containing 61 bromodomains clustered into eight families. Distinct experimental approaches are used to identify the first BET inhibitors, GSK 525762A and (+)-JQ-1.

The Polycomb group (PcG) protein, enhancer of zeste homologue 2 (EZH2), has an essential role in promoting histone H3 lysine 27 trimethylation (H3K27me3) and epigenetic gene silencing. This function of EZH2 is important for cell proliferation and inhibition of cell differentiation, and is implicated in cancer progression. Cyclin-dependent kinases regulate epigenetic gene silencing through phosphorylation of EZH2. In many types of cancers including lymphomas and leukemia, EZH2 is postulated to exert its oncogenic effects via aberrant histone and DNA methylation, causing silencing of tumor suppressor genes.

p300/CBP is not only a transcriptional adaptor but also a histone acetyltransferase.

Epigenetic Reader Domain Related Products (102):

By Effects:	Inhibitors (95)

Cat. No.	Product Name	Effect	Purity

HY-13030

(+)-JQ-1 Inhibitor 99.90%

(+)-JQ-1 is a BET bromodomain inhibitor, with IC₅₀s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)).
HY-13470

GSK126 Inhibitor 99.86%

GSK126 is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC₅₀ of 9.9 nM.
HY-13803

EPZ-6438 Inhibitor 99.63%

EPZ-6438 (Tazemetostat) is a potent, selective and orally available EZH2 inhibitor with K_i and IC₅₀ of 2.5 and 11 nM, respectively.
HY-15743

OTX-015 Inhibitor 99.81%

OTX-015 is a potent bromodomain (BRD2/3/4) inhibitor with IC₅₀s ranging from 92 to 112 nM.
HY-107455

A-485 Inhibitor 99.08%

A-485 is a potent and selective catalytic inhibitor of p300/CBP with IC₅₀s of 9.8 nM and 2.6 nM for p300 and CBP, respectively.
HY-112588

dBET6 Inhibitor 99.40%

dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC₅₀ of 14 nM, and has antitumor activity.
HY-103299

KG-501 Inhibitor 99.12%

KG-501 is a CREB inhibitor, with an IC₅₀ of 6.89 μM.
HY-101519

BETd-260 Inhibitor 98.04%

BETd-260 is a potent BET degrader based on PROTAC technology, with an IC₅₀ of 30 pM against BRD4 protein in RS4;11 leukemia cell line.

(+)-JQ-1	Inhibitor	99.90%
(+)-JQ-1 is a BET bromodomain inhibitor, with IC₅₀s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)).

GSK126	Inhibitor	99.86%
GSK126 is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC₅₀ of 9.9 nM.

EPZ-6438	Inhibitor	99.63%
EPZ-6438 (Tazemetostat) is a potent, selective and orally available EZH2 inhibitor with K_i and IC₅₀ of 2.5 and 11 nM, respectively.

OTX-015	Inhibitor	99.81%
OTX-015 is a potent bromodomain (BRD2/3/4) inhibitor with IC₅₀s ranging from 92 to 112 nM.

A-485	Inhibitor	99.08%
A-485 is a potent and selective catalytic inhibitor of p300/CBP with IC₅₀s of 9.8 nM and 2.6 nM for p300 and CBP, respectively.

dBET6	Inhibitor	99.40%
dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC₅₀ of 14 nM, and has antitumor activity.

KG-501	Inhibitor	99.12%
KG-501 is a CREB inhibitor, with an IC₅₀ of 6.89 μM.

BETd-260	Inhibitor	98.04%
BETd-260 is a potent BET degrader based on PROTAC technology, with an IC₅₀ of 30 pM against BRD4 protein in RS4;11 leukemia cell line.

HY-N0005

Curcumin	Inhibitor	99.66%
Curcumin is a natural phenolic compound with diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin is an inhibitor of p300 histone acetylatransferase ((HATs)) and also shows inhibitory effects on NF-κB and MAPKs.

HY-100972

ARV-771	Inhibitor	99.44%
ARV-771 is a potent bromodomain and extra-terminal (BET) proteins degrader based on PROTAC technology with K_d values of 4.7, 7.6, 7.6 nM against BRD2, BRD3 and BRD4, respectively.

HY-16954

ARV-825 Inhibitor 99.37%

ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 binds to BD1 and BD2 of BRD4 with K_ds of 90 and 28 nM, respectively.
HY-13032

GSK 525762A Inhibitor 99.85%

GSK 525762A is a BET bromodomain inhibitor with IC₅₀ of 32.5-42.5 nM.
HY-50698

BI 2536 Inhibitor 99.95%

BI 2536 is a dual PLK1 and BRD4 inhibitor with IC₅₀s of 0.83 and 25 nM, respectively.
HY-13500

GSK343 Inhibitor 98.49%

GSK343 is a highly potent and selective EZH2 inhibitor with an IC₅₀ of 4 nM.
HY-12186

3-Deazaneplanocin A hydrochloride Inhibitor 99.76%

3-Deazaneplanocin A hydrochloride is a potent histone methyltransferase EZH2 inhibitor.
HY-13823

C646 Inhibitor >98.0%

C646 is a selective and competitive histone acetyltransferase p300 inhibitor with K_i of 400 nM, and is less potent for other acetyltransferases.
HY-13235

I-BET151 Inhibitor 98.77%

I-BET151 is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC₅₀ of 6.1, 6.3, and 6.6, respectively.
HY-101120

666-15 Inhibitor 98.65%

666-15 is a potent and selective CREB inhibitor with an IC₅₀ of 81 nM.
HY-15646

UNC1999 Inhibitor 99.47%

UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH1/2 with IC₅₀s of 10 nM and 45 nM, repectively.
HY-100482

CPI-637 Inhibitor 99.94%

CPI-637 is a potent and selective CBP/EP300 bromodomains inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respectively.

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