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 (163):

By Effects:	Inhibitors (152) Activators (1) Modulators (1)

Cat. No.	Product Name	Effect	Purity

HY-13030

(+)-JQ-1	Inhibitor	99.90%
(+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC₅₀s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy.

HY-107455

A-485 Inhibitor >98.0%

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 histone acetyltransferase (HAT), respectively.

A-485	Inhibitor	>98.0%
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 histone acetyltransferase (HAT), respectively.

HY-N0005

Curcumin	Inhibitor
Curcumin (Diferuloylmethane) 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-15743

Birabresib Inhibitor 99.81%

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

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

HY-100972

ARV-771	Inhibitor	99.82%
ARV-771 is a potent BET degrader based on PROTAC technology with K_ds of 34, 4.7, 8.3, 7.6, 9.6, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively.

HY-114162

VTP50469 Inhibitor

VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a K_i of 104 pM. VTP50469 has potently anti-leukemia activity.

VTP50469	Inhibitor
VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a K_i of 104 pM. VTP50469 has potently anti-leukemia activity.

HY-114421

FKBP12 PROTAC dTAG-13	Inhibitor	>98.0%
FKBP12 PROTAC dTAG-13 (dTAG-13) is a PROTAC-based heterobifunctional degrader. FKBP12 PROTAC dTAG-13 (dTAG-13) is a degrader of FKBP12^F36V with expression of FKBP12^F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 (dTAG-13) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN.

HY-125837A

MS31 trihydrochloride	Inhibitor	>98.0%
MS31 trihydrochloride is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 trihydrochloride potently inhibits the interactions between SPIN1 and H3K4me3 (IC₅₀=77 nM, AlphaLISA; 243 nM, FP). MS31 trihydrochloride selectively binds Tudor domain II of SPIN1 (K_d=91 nM). MS31 trihydrochloride potently inhibits binding of trimethyllysine-containing peptides to SPIN1, and is not toxic to nontumorigenic cells.

HY-16954

ARV-825 Inhibitor 99.37%

ARV-825 is a BRD4 degrader based on PROTAC technology. ARV-825 binds to BD1 and BD2 of BRD4 with K_ds of 90 and 28 nM, respectively.
HY-112588

dBET6 Inhibitor 99.40%

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

ARV-825	Inhibitor	99.37%
ARV-825 is a BRD4 degrader based on PROTAC technology. ARV-825 binds to BD1 and BD2 of BRD4 with K_ds of 90 and 28 nM, respectively.

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

HY-101838

dBET1	Inhibitor	99.24%
dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC₅₀ of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to Thalidomide (HY-14658) with a linker.

HY-13032

Molibresib Inhibitor 99.85%

Molibresib (GSK 525762A; I-BET 762) 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. BI-2536 suppresses IFNB (encoding IFN-β) gene transcription.
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-101120

666-15 Inhibitor 99.63%

666-15 is a potent and selective CREB inhibitor with an IC₅₀ of 81 nM.
HY-13235

I-BET151 Inhibitor 99.37%

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

Molibresib	Inhibitor	99.85%
Molibresib (GSK 525762A; I-BET 762) is a BET bromodomain inhibitor with IC₅₀ of 32.5-42.5 nM.

BI 2536	Inhibitor	99.95%
BI 2536 is a dual PLK1 and BRD4 inhibitor with IC₅₀s of 0.83 and 25 nM, respectively. BI-2536 suppresses IFNB (encoding IFN-β) gene transcription.

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.

666-15	Inhibitor	99.63%
666-15 is a potent and selective CREB inhibitor with an IC₅₀ of 81 nM.

I-BET151	Inhibitor	99.37%
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-78695

JQ-1 (carboxylic acid)	Inhibitor	99.59%
JQ-1 carboxylic acid is a (+)-JQ1 derivative (a BET bromodomain inhibitor). JQ-1 carboxylic acid can be uesd as a precursor to synthesize PROTACs, which targets BET bromodomains.

HY-107425

MZ 1	Inhibitor	98.51%
MZ 1 is a PROTAC BRD4 degrader. MZ 1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4 over BRD2 and BRD3. K_ds of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively.

HY-100482

CPI-637	Inhibitor	99.94%
CPI-637 is a selective and potent CBP/EP300 bromodomain inhibitor with IC₅₀ values of 0.03 μM, 0.051 μM and 11.0 μM for CBP, EP300 and BRD4 BD-1, respectively, and an EC₅₀ of 0.3 μM for CBP.

HY-112090

ABBV-744 Inhibitor 99.14%

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

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