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 (99):

By Effects:	Inhibitors (93)

Cat. No.	Product Name	Effect	Purity

HY-13030

(+)-JQ-1 Inhibitor 99.90%

(+)-JQ-1 is a BET bromodomain inhibitor, with IC₅₀ of 77 nM/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 activity with IC₅₀ of 9.9 nM.
HY-13803

EPZ-6438 Inhibitor 99.63%

EPZ-6438 inhibits the activity of human PRC2-containing wild-type EZH2 with K_i of 2.5±0.5 nM.
HY-15743

OTX-015 Inhibitor 99.81%

OTX-015 is a new potent BRD2/3/4 inhibitor for cell adhesion with IC₅₀ values 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-112090

ABBV-744 Inhibitor

ABBV-744 is a highly BDII-selective BET bromodomain inhibitor, used in the research of inflammatory diseases, cancer, and AIDS.

(+)-JQ-1	Inhibitor	99.90%
(+)-JQ-1 is a BET bromodomain inhibitor, with IC₅₀ of 77 nM/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 activity with IC₅₀ of 9.9 nM.

EPZ-6438	Inhibitor	99.63%
EPZ-6438 inhibits the activity of human PRC2-containing wild-type EZH2 with K_i of 2.5±0.5 nM.

OTX-015	Inhibitor	99.81%
OTX-015 is a new potent BRD2/3/4 inhibitor for cell adhesion with IC₅₀ values 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.

ABBV-744	Inhibitor
ABBV-744 is a highly BDII-selective BET bromodomain inhibitor, used in the research of inflammatory diseases, cancer, and AIDS.

HY-111422

PLX51107	Inhibitor	99.81%
PLX51107 is a potent and selective BET inhibitor, with K_ds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; PLX51107 also interacts with the bromodomains of CBP and EP300 (K_d, in the 100 nM range).

HY-103299

KG-501 Inhibitor 99.12%

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

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

HY-N0005

Curcumin	Inhibitor	99.66%
Curcumin is a natural phenolic compound with impressive antioxidant properties, acts as a p300/CREB-binding protein inhibitor of histone acetyltransferase activity, and also activates nuclear factor (erythroid-2 related) factor 2 (Nrf2).

HY-13032

GSK 525762A Inhibitor 99.85%

GSK 525762A is a BET bromodomain inhibitor with IC₅₀ of 32.5-42.5 nM.
HY-16954

ARV-825 Inhibitor 99.35%

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

GSK 525762A	Inhibitor	99.85%
GSK 525762A is a BET bromodomain inhibitor with IC₅₀ of 32.5-42.5 nM.

ARV-825	Inhibitor	99.35%
ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 shows affinity to BD1 and BD2 of BRD4 with K_ds of 90 and 28 nM, respectively.

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-13500

GSK343 Inhibitor 98.49%

GSK343 is a highly potent, selective, and cell-active EZH2 inhibitor with IC₅₀ of 4 nM.
HY-50698

BI 2536 Inhibitor 99.95%

BI 2536 is a potent and selective inhibitor of Plk1 with IC₅₀ of 0.83 nM, and is also a potent inhibitor of BRD4 with IC₅₀ of 25 nM.
HY-12186

3-Deazaneplanocin A hydrochloride Inhibitor 99.76%

3-Deazaneplanocin A hydrochloride is a potent histone methyltransferase EZH2 inhibitor.
HY-13235

I-BET151 Inhibitor 98.77%

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

GSK343	Inhibitor	98.49%
GSK343 is a highly potent, selective, and cell-active EZH2 inhibitor with IC₅₀ of 4 nM.

BI 2536	Inhibitor	99.95%
BI 2536 is a potent and selective inhibitor of Plk1 with IC₅₀ of 0.83 nM, and is also a potent inhibitor of BRD4 with IC₅₀ of 25 nM.

3-Deazaneplanocin A hydrochloride	Inhibitor	99.76%
3-Deazaneplanocin A hydrochloride is a potent histone methyltransferase EZH2 inhibitor.

I-BET151	Inhibitor	98.77%
I-BET151 is a BET bromodomain inhibitor, inhibits BRD4, BRD2, and BRD3 with pIC₅₀ of 6.1, 6.3, and 6.6, respectively.

HY-100015

Mivebresib	Inhibitor	99.28%
Mivebresib, a novel BET family inhibitor, disrupts critical transcription programs that drive prostate cancer growth to induce potent anti-tumor activity in vitro and in vivo. Also a potent inhibitor of MYC and the TMPRSS2-ETS fusion proteins.

HY-15646

UNC1999 Inhibitor 99.47%

UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH2 (IC₅₀<10 nM) and EZH1 (IC₅₀=45±3 nM).
HY-101120

666-15 Inhibitor 98.65%

666-15 is a potent and selective CREB inhibitor with an IC₅₀ of 81 nM.
HY-78695

JQ-1 carboxylic acid Inhibitor 99.59%

(+)-JQ1 carboxylic acid is the carboxylic acid form of (+)-JQ1 for derivative synthesis.

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