Epigenetic Reader Domain

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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 (677)
Antibodies (109)

By Effects:	Controls (10) Inhibitors (506) Agonists (2) Degraders (96) Antagonist (1) Activators (3) Modulators (3) Chemical (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-137573

Trotabresib	Inhibitor	99.53%
CC-90010 (compound 1) is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors.

HY-129937A

GNE-987	Inhibitor	99.91%
GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC₅₀=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC₅₀=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC).

HY-103100

SB-699551	Activator	99.53%
SB-699551 is a potent and selective 5-HT5A antagonist with a K_i value of 5.1 μM. SB-699551 increases the phosphorylation levels of CREB and ATF1, and decreases the phosphorylation levels of AKT, PRAS40, P70S6K, FOXO1, and S6RP. SB-699551 improves drug-induced cognitive deficits. SB-699551 improves social withdrawal and forgetfulness. SB-699551 inhibits breast cancer.

HY-117690

dBRD9	Degrader	99.89%
dBRD9,a PROTAC, can selective degrades BRD9. dBRD9 improves the bromine domain binding profile and reduces the binding activity of the whole BET family.

HY-19999A

PF-CBP1 hydrochloride	Inhibitor	99.96%
PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). PF-CBP1 inhibits CREBBP and EP300 bromodomains with?IC₅₀?of 125 nM and 363 nM respectively. PF-CBP1 hydrochloride reduces LPS-induced inflammatory cytokines expression (IL-1β,?IL-6?and?IFN-β) in primary macrophages. PF-CBP1 hydrochloride also downregulates?RGS4?expression cortical neurons and can be used for the research of neurological disorders, including epilepsy and parkinson's disease, et al.

HY-19541

I-CBP112	Inhibitor	98.20%
I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor, that inhibits the CBP/p300 bromodomains, enhances acetylation by p300.

HY-137892

GSK620	Inhibitor	99.79%
GSK620 is a potent and orally active pan-BD2 inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood.

HY-100352

BI-9564	Inhibitor	98.73%
BI-9564 is a potent, selective and cell-permeable BRD9/BRD7 bromodomains inhibitor, with IC₅₀s of 75 nM and 3.4 μM and K_ds of 14 nM and 239 nM, respectively. BI-9564 has an IC₅₀ of > 100 μM for BET family.

HY-129939

PROTAC BRD4 ligand-1	Inhibitor	99.85%
PROTAC BRD4 ligand-1 is a potent BET inhibitor and a ligand for target BRD4 protein for PROTACT GNE-987 (HY-129937A).

HY-112789

(+)-JQ1 PA	Inhibitor	98.45%
(+)-JQ1 PA is a derivative of the Bromodomain and extra-terminal (BET) inhibitor JQ1, with an IC₅₀ of 10.4 nM. (+)-JQ1 PA is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-134463

NHWD-870	Inhibitor	99.36%
NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC₅₀=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation.

HY-13960

GSK1324726A	Inhibitor	99.75%
GSK1324726A is a novel, potent, and selective inhibitor of BET proteins with high affinity to BRD2 (IC₅₀=41 nM), BRD3 (IC₅₀=31 nM), and BRD4 (IC₅₀=22 nM).

HY-148669A

Bleximenib oxalate	Inhibitor	≥98.0%
Bleximenib (JNJ-75276617; Menin-MLL inhibitor 24) oxalate is a potent, selective and orally active menin-KMT2A protein-protein interaction inhibitor with IC₅₀ values of 0.1, 0.045, ≤0.066 nM for human, mouse, dog, respectively. Bleximenib oxalate shows antiproliferative activity and induces apoptosis. Bleximenib oxalate has the potential for the research of Acute myeloid leukemia (AML).

HY-120028

GNE-207	Inhibitor	99.94%
GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC₅₀ of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC₅₀ of 18 nM for MYC expression in MV-4-11 cells.

HY-19809

MI-463	Inhibitor	99.66%
MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.

HY-16586

PFI-1	Inhibitor	99.87%
PFI-1 is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC₅₀ of 0.22 μM in a cell-free assay.

HY-15846

CPI-203	Inhibitor	98.98%
CPI-203 is a novel potent, selective and cell permeable inhibitor of BET bromodomain, with an IC₅₀ value of appr 37 nM (BRD4 α-screen assay).

HY-149026

GNE-064	Inhibitor	99.65%
GNE-064 (compound 5) is a selective, orally active and highly soluble inhibitor of SMARCA4, SMARCA2 and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC₅₀ of 0.035 μM and inhibits SMARCA2 with an EC₅₀ of 0.10 μM. GNE-064 possess K_ds with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of agent synthesis.

HY-136521

AZ13824374	Inhibitor	98.86%
AZ13824374 is a highly potent and selective ATAD2 bromodomain inhibitor which shows cellular target engagement and antiproliferative activity in a range of breast cancer models. AZ13824374 inhibits ATAD2 with pIC₅₀s of 8.2 and 6.2 in ATAD2 FRET assay and ATAD2 NanoBRET assay, respectively.

HY-145550

Amredobresib	Inhibitor	98.97%
Amredobresib is a potent inhibitor of BET. Amredobresib inhibits the binding of bromodomains to acetylated lysines on histone H3 and H4 and thus acts as important regulators of gene transcription. Amredobresib is useful for the research of acute myeloid leukemia (AML) and cancer (extracted from patent WO2019145410A1 and WO2021175824A1).

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Epigenetic Reader Domain

Epigenetic Reader Domain

Epigenetic Reader Domain Related Products (677)

Antibodies (109)

Epigenetic Reader Domain Related Products (677):