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 Isoform Specific Products:

Epigenetic Reader Domain Isoform Comparison

Epigenetic Reader Domain Related Products (935)
Antibodies (109)
Epigenetic Reader Domain Isoform Comparison

By Effects:	Inhibitors (619)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-168234

PROTAC SMARCA2 degrader-31	Inhibitor
PROTAC SMARCA2-degrader-36 (compound 38) is a SMARCA2 degrader and can reach the the degradation rate of 99 % at the 100 nM in H929 cells. PROTAC SMARCA2-degrader-36 shows anti-proliferative activity and can be used for study of cancer(Structure Note: PINK SMARCA2 ligand HY-44012; Blue, VHL ligand (HY-112078); Black, linker HY-W014125).

HY-111575

DCB29	Inhibitor
DCB29 is a selective inhibitor of the BPTF bromodomain, with an IC₅₀ value of 13.2 μM. DCB29 can be used for the study of the BPTF-related diseases (such as bladder cancer, colorectal cancer, melanoma, leukemia, and other cancers).

HY-176449

PROTAC BRD4 Degrader-32	Inhibitor
PROTAC BRD4 Degrader-32 (Compound 22) is a BRD4 PROTAC degrader (DC₅₀: 0.20 nM). PROTAC BRD4 Degrader-32 connects the BRD4-binding domain and CRBN-binding domain through a unique carbon-carbon linked linker to form a ternary complex, inducing ubiquitination of BRD4 for proteasomal degradation. PROTAC BRD4 Degrader-32 is promising for research of BRD4-related cancers (such as hematological malignancies). (Pink: GSK1324726A (HY-13960); Black: linker (HY-176450); Blue: Lenalidomide-5-Br (HY-W072954)).

HY-159451

PROTAC SMARCA2 degrader-7	Inhibitor
PROTAC SMARCA2 degrader-7 (Compound I-428) is a PROTAC degrader for SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily A (SMARCA) SMARCA2. PROTAC SMARCA2 degrader-7 degrades SMARCA2 and SMARCA4 in MV411 with DC₅₀ of <100 and 100-500 nM. (Pink: Ligand for target protein (HY-159542); Black: Linker (HY-159538); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))

HY-172095

BRD4 Inhibitor-39	Inhibitor
BRD4 Inhibitor-39 (compound 12m) is an orally available BRD4 inhibitor with an IC₅₀ value of 0.02 μM. BRD4 Inhibitor-39 induces apoptosis. BRD4 Inhibitor-39 has anti-tumor activity.

HY-136794

SB-284851-BT	Inhibitor
SB-284851-BT is an inhibitor of BRD4/p38α/BRDT. SB-284851-BT inhibits BRD4-BD1 (IC₅₀=1.7 µM), p38α (K_d=0.47 nM), BRDT (1) (IC₅₀=18 µM) and BRD4 (1)(IC₅₀=3.7 µM). SB-284851-BT reduces IL-8 production by inhibiting p38α, as well as inhibiting BRD4 to down-regulates c-Myc and NF-κB gene pathways in cancer. SB-284851-BT can combined with the bromine domain and extra terminal (BET).

HY-W265951

3-Methylcarbostyril	Inhibitor
3-Methylcarbostyril (compound 5) is a BRD4 BD1 inhibitor with a pIC₅₀ of 4.4.

HY-168463

Y16524	Inhibitor
Y16524 is a potent inhibitor of CBP/p300 bromodomain , with the IC₅₀ of 0.01 μM. Y16524 has the potential for the research of acute myeloid leukemia (AML).

HY-173450

ZL0516	Inhibitor
ZL0516 is a potent, selective, and orally active BRD4 BD1 inhibitor. ZL0516 suppresses inflammatory bowel disease (IBD) by inhibiting BRD4/NF-κB signaling.

HY-177145

CDD-1132	Inhibitor
CDD-1132 (Compound 8) is a potent inhibitor of BRDT-BD2. CDD-1132 has an IC₅₀ of 13 nM against BRDT-BD2. CDD-1132 can be studied in research on nonhormonal contraceptive agent.

HY-176822

SGC-BRDVIII-NC	Inhibitor
SGC-BRDVIII-NC (Compound 35) is a negative control compound of SMARCA2/4 and PB1 bromodomain (BRD) inhibitor. SGC-BRDVIII-NC completely abolishes protein-ligand binding capacity with the methylation of the phenolic hydroxyl moiety. SGC-BRDVIII-NC can be used for adipogenesis research.

HY-176929

BET-IN-29	Inhibitor
BET-IN-29 (Compound 1) is a bromodomain and the terminal motif (BET) inhibitor. BET-IN-29 can be used for the study of cancer, inflammation, metabolism, neurological diseases, and infectious diseases.

HY-142674

BRD4-BD1/2-IN-1	Inhibitor
BRD4-BD1/2-IN-1 is a potent BRD4 inhibitor with IC₅₀s of <100 nM for BRD4 BD-1 and BRD4 BD-2, respectively (US20150148375A1, compound 5).

HY-15222A

Menin-MLL inhibitor MI-2 dihydrochloride	Inhibitor
Menin-MLL inhibitor MI-2 dihydrochloride is a competitive and selective Menin-MLL interaction inhibitor with an IC₅₀ value of 446 nM and a K_i value of 158 nM. Menin-MLL inhibitor MI-2 dihydrochloride downregulates the expression of target genes such as HOXA9 and MEIS1, inhibits proliferation of leukemia cells and induces apoptosis and differentiation. Menin-MLL inhibitor MI-2 dihydrochloride is proming for rasearch of MLL-rearranged acute leukemias (e.g., AML, ALL).

HY-153945

BET-IN-15	Inhibitor
BET-IN-15 (compound 1) is a potent and orally active BET inhibitor with IC₅₀ values of 0.64，0.25 nM for BRD4-BD1，BRD4-BD2，respectively. BET-IN-15 shows antiproliferative activity.

HY-168635

SJ46420	Inhibitor
SJ46420, a SJ46421 (HY-168634) pro-drug variant, is a potent and selective BRD3 PROTAC degrader. SJ46420 degrads BRD3 in a KLHDC2-dependent manner, thereby partially reducing the levels of BRD2 or BRD4 (Pink: ligand for target protein (HY-13030); Black: linker (HY-20797); Blue: E3 ligase ligand (HY-159973)).

HY-149806

Bromodomain IN-2	Inhibitor
BD-IN-1 is a pan bromodomain (BD) inhibitor with K_D values of 250, 420, 130, 430, 67, 240, 970 nM for BRD4(1), CBP, BRPF1B, BRD7, BRD9, BRDT(1), CECR2 respectively. BD-IN-1 shows antiproliferative activity.

HY-151366

HDAC8/BRPF1-IN-1	Inhibitor
HDAC8/BRPF1-IN-1 (Compound 23a) is a dual inhibitor of HDAC8 and BRPF1 with an IC₅₀ of 443 nM against human HDAC8 and a K_d of 67 nM against human BRPF1. HDAC8/BRPF1-IN-1 shows low in vitro activity against HDAC1 and 6.

HY-132128

BRD4 Inhibitor-12	Inhibitor	99.34%
BRD4 Inhibitor-12 (Compound 9) is a BRD4 ligand, and can be used for research of cancer, infammation.

HY-145909

BRD4 Inhibitor-17	Inhibitor
BRD4 Inhibitor-17 (Compound 5i) is a potent inhibitor of BRD4 with an IC₅₀ of 0.33 μM. BRD4 Inhibitor-17 plays crucial role in regulating transcription of inflammatory, proliferation and cell cycle genes. BRD4 Inhibitor-17 serves as potential antidotes for arsenicals.

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Epigenetic Reader Domain

Epigenetic Reader Domain

Epigenetic Reader Domain Isoform Specific Products:

Epigenetic Reader Domain Isoform Specific Products:

Epigenetic Reader Domain Related Products (935)

Antibodies (109)

Epigenetic Reader Domain Isoform Comparison

Epigenetic Reader Domain Related Products (935):