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 (925)
Antibodies (109)

By Effects:	Inhibitors (621)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-145226

XY-06-007	Inhibitor	98.9%
XY-06-007 is a selective and potent bump-and-hole (B&H)-PROTAC BRD4_BD1L94V degrader. XY-06-007 shows a DC_{50, 6 h} of 10 nM against BRD4_BD1L94V with no degradation of off-targets. XY-06-007 demonstrates suitable pharmacokinetics for in vivo studies.

HY-111503

Y06137	Inhibitor	99.90%
Y06137 is a potent and selective BET inhibitor for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the BRD4(1) bromodomain with a K_d of 81 nM.

HY-125837

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

HY-139076

Menin-MLL inhibitor 19	Inhibitor	98.07%
Menin-MLL inhibitor 19, a potent exo-aza spiro inhibitor of menin-mll interaction, example A17, extracted from patent WO2019120209A1. Menin-MLL inhibitor 19 can be used for the reseaech of various diseases, such as cancer, myelodysplastic syndrome (MDS) and diabetes.

HY-156794A

Enzomenib enantiomer	Inhibitor	98.01%
Enzomenib enantiomer (DSP-5336 enantiomer) is an enantiomer of Enzomenib (HY-156794). Enzomenib (DSP-5336) is an orally active Menin inhibitor (IC₅₀=1.4 nM, K_d=6.0 nM). Enzomenib disrupts the interaction between Menin and KMT2A/MLL fusion proteins, specifically inhibits the expression of leukemia driver genes such as HOX/MEIS1, and upregulates ITGAM. Enzomenib effectively induces cell differentiation, inhibits tumor cell proliferation, and suppresses primitive cell colony formation. Enzomenib reduces disease burden and prolongs survival, but causes adverse reactions including differentiation syndrome and QTc interval prolongation. Enzomenib is used for research on relapsed/refractory acute myeloid leukemia, acute lymphoblastic leukemia, and other hematologic malignancies with mixed lineage leukemia (MLL) rearrangements or NPM1 mutations.

HY-136175B

cis-Revumenib	Inhibitor	98.92%
cis-Revumenib (cis-SNDX-5613) is an isomer of Revumenib (HY-136175). Revumenib (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. Revumenib can be used for the research of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML).

HY-153226

BET-IN-14	Inhibitor	98.87%
BET-IN-14 is an orally active pan BET inhibitor (IC₅₀: 5.35 nM). BET-IN-14 has anti-cancer activity.

HY-18372

UNC1021	Inhibitor	99.85%
UNC1021 is a selective L3MBTL3 inhibitor with an IC₅₀ of 0.048 μM.

HY-170380

XY221	Inhibitor
XY221 (Compound 16o) selectively inhibits BRD4 BD2, with an IC₅₀ of 5.8 nM. XY221 demonstrates high pan-BD2 selectivity (667-fold over BRD4 BD1) and BRD4 BD2 domain selectivity (9−32-fold over BRD2/3/T BD2). XY221 induce Apoptosis in MV4-11 cells and shows anticancer activity .

HY-126299

NVS-BPTF-1	Inhibitor	99.6%
NVS-BPTF-1, a chemical probe, is a selective inhibitor for bromodomain and PHD finger containing transcription factor (BPTF), with K_D of 71 nM.

HY-151812

CBP/p300-IN-20	Inhibitor	98.03%
CBP/p300-IN-20 is a potent and selective p300/CBP inhibitor, with a pIC₅₀ of 10.1 for p300. CBP/p300-IN-20 can be used for the research of cancer.

HY-147046

ET-JQ1-OH	Inhibitor
ET-JQ1-OH is an allele-specific BET inhibitor. ET-JQ1-OH can serve as a Ligand for Target Protein for PROTAC, and is used for the development and design of PROTAC Brd4 degraders, such as AB3145 (HY-180923).

HY-107425B

cis-MZ 1 hydrate	Inhibitor	99.0%
cis-MZ 1 hydrate is a negative control for BRD4-targeted PROTAC MZ 1 (HY-107425). cis-MZ 1 or MZ 1 is a combination of the von Hippel-Lindau ligand (red part in the structural formula) and the BRD4 ligand (blue part in the structural formula). The K_d of MZ 1 for BRD4 BD1/2 was 382 nM and 120 nM, respectively.

HY-176521A

AR/BRD4 RIPTAC-1 TFA	Inhibitor	99.61%
AR/BRD4 RIPTAC-1 (Compound II-5) TFA is an orally active Regulatory-inducible proximity-targeting chimera (RIPTAC). AR/BRD4 RIPTAC-1 TFA induces the formation of a stable ternary complex between the androgen receptor (AR) and BRD4, thereby blocking BRD4 function. AR/BRD4 RIPTAC-1 TFA inhibits the growth and proliferation of tumor cells. AR/BRD4 RIPTAC-1 TFA holds promise for use in prostate cancer research.

HY-162739

SMARCA2-IN-1	Inhibitor
SMARCA2-IN-1 (Compound I-19) is an inhibitor for SWI/SNF chromatin remodeling complexe SMARCA2 with IC₅₀ >1000 nM in H1299.

HY-147202

BRD4 Inhibitor-24	Inhibitor	99.27%
BRD4 Inhibitor-24 (compound 3U) is a potent BRD4 inhibitor, BRD4 Inhibitor-24 shows antitumor activity against MCF7 and K652 cells, with IC₅₀ values of 33.7 and 45.9 μM, respectively (extracted from patent CN107721975A).

HY-147868

DC-CPin711	Inhibitor	99.09%
DC-CPin711 is a potent and selective inhibitor of CREB-binding protein (CBP) bromodomain with an IC₅₀ of 0.0626 μM. DC-CPin711 arrests cell cycle at G1 phase and induces apoptosis.

HY-117948

ML399	Inhibitor	98.20%
ML399 is a Menin-Mixed Lineage Leukemia (MLL) protein-protein interaction inhibitor.

HY-151594A

iBRD4-BD1 diTFA	Inhibitor	99.52%
iBRD4-BD1 diTFA is selective BRD4 bromodomain inhibitor. iBRD4-BD1 diTFA has inhibition activity for BRD4 bromodomain with an IC₅₀ value of 12 nM. iBRD4-BD1 diTFA can be used for the research of inflammation and oncology.

HY-111977

ZEN-3219	Inhibitor	99.75%
ZEN-3219 is a BET inhibitor with IC₅₀s of 0.48, 0.16 and 0.47 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3219 can be used to form PROTACs to induce degradation of BRD4.

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Epigenetic Reader Domain

Epigenetic Reader Domain

Epigenetic Reader Domain Related Products (925)

Antibodies (109)

Epigenetic Reader Domain Related Products (925):