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 (176):

By Effects:	Inhibitors (164) Antagonists (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 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 histone acetyltransferase (HAT), respectively.

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 histone acetyltransferase (HAT), respectively.

HY-N0005

Curcumin	Inhibitor
Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities.

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 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively.

HY-114162

VTP50469 Inhibitor 99.41%

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	99.41%
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-136175

SNDX-5613	Inhibitor	99.62%
SNDX-5613 is a potent and specific Menin-MLL inhibitor with a binding K_i of 0.149 nM and a cell based IC₅₀ of 10-20 nM. SNDX-5613 can be used for the research of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML).

HY-126428

ZL0580	Modulator	99.48%
ZL0580, a structurally close analog of ZL0590, induces epigenetic suppression of HIV via selectively binding to BD1 domain of BRD4. ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter.

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.
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.

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.

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-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 NSC 527179 (HY-14658) with a linker.

HY-13032

Molibresib Inhibitor 99.85%

Molibresib (I-BET762; GSK525762) 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-101120

666-15 Inhibitor 99.63%

666-15 is a potent and selective CREB inhibitor with an IC₅₀ of 81 nM. 666-15 suppresses tumor growth in a breast cancer xenograft model.

Molibresib	Inhibitor	99.85%
Molibresib (I-BET762; GSK525762) 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.

666-15	Inhibitor	99.63%
666-15 is a potent and selective CREB inhibitor with an IC₅₀ of 81 nM. 666-15 suppresses tumor growth in a breast cancer xenograft model.

HY-107425

MZ 1	Inhibitor	98.87%
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-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.
HY-112090

ABBV-744 Inhibitor 99.48%

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

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.

ABBV-744	Inhibitor	99.48%
ABBV-744 is a highly BDII-selective BET bromodomain inhibitor, used in the research of inflammatory diseases, cancer, and AIDS.

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-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.

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