Epigenetic Reader Domain

Angiogenesis

5-alpha Reductase ALK Bcr-Abl BTK EGFR FAK FLT3 HER-2 HIF Src Syk VDA VEGFR
Anti-infection

Antibiotic Arenavirus Bacterial CMV EBV Enterovirus Filovirus Fungal Gli HBV HCV HCV Protease HIV HSV Influenza Virus Parasite RABV Reverse Transcriptase RSV SARS-CoV TMV Virus Protease
Apoptosis

Apoptosis ASK Bcl-2 Caspase c-Myc c-RET Cytohesin DAPK Ferroptosis FKBP IAP Mdm2 p53 PD-1 PD-L1 PERK PKD Ras RIP kinase ROS Survivin Thymidylate Synthase TNF Receptor TNFa TRADD
Autophagy

Autophagy LRRK2 Mitophagy OGA ULK
Cell Cycle

Antifolate APC Aurora Kinase BMI-1 CDK Chk c-Myc Eukaryotic Initiation Factor G-quadruplex HDAC HSP Kinesin LIMK Mad2 Microtubule(Tubulin) Mps1 Nucleoside Antimetabolite/Analog Nur77 p21 PAK PERK PFKFB PLK PPAR Ras Rho ROCK SRPK TOPK Topoisomerase Wee1
Cytoskeletal Signaling

Arp2 3 Complex Bcr-Abl Cardiac Myosin Dynamin Gap Junction Protein HSP Integrin Kinesin Microtubule Associated MLCK Myosin PAK TACC3 Wntbeta-catenin
DNA Damage

ATM(ATR) CRISPR(Cas9) DNA alkylator DNA Stain DNA(RNA) Synthesis GAK HDAC HSP Nucleoside Antimetabolite(Analog) OGG1 p97 PARG PARP RAD51 RNR Sirtuin SMN Telomerase Topoisomerase
Endocrinology & Hormones

5-alpha Reductase ACE Adrenergic Receptor Androgen Receptor Aromatase Estrogenprogestogen Receptor Glucocorticoid Receptor GPR Mineralocorticoid Receptor RAAS THR TSH Receptor
Epigenetics

AMPK Aurora Kinase DNA Methyltransferase Epigenetic Reader Domain EZH1 2 HDAC HIF Histone Acetyltransferase Histone Demethylase Histone Methyltransferase JAK MAT MicroRNA MLL Pim PKC Protein Arginine Deiminase Sirtuin Small Interfering RNA (siRNA) SMYD
GPCR & G Protein

5-HT Receptor Adenosine Receptor Adenylate Cyclase Adrenergic Receptor Angiotensin Receptor APJ Bombesin Receptor Bradykinin Receptor cAMP Cannabinoid Receptor CaSR CCK receptor CCR CGRP Receptor CRFR CXCR Dopamine Receptor EBI2 Endothelin Receptor Formyl Peptide Receptor Free Fatty Acid Receptor G protein-coupled Bile Acid Receptor GCGR GHSR GLP Receptor Glucagon Receptor GnRH Receptor GPCR19 GPR GPR109A Guanylate Cyclase Hedgehog(Smoothened) ROCK Histamine Receptor ICMT Leukotriene Receptor LPA Receptor LPL Receptor LTR mAChR Melanocortin Receptor Melatonin Receptor mGluR Motilin Receptor MRGPR MT Receptor Neurokinin Receptor Neuropeptide Y Receptor Neurotensin Receptor NPY receptor Opioid Receptor OX Receptor Oxytocin Receptor P2Y Receptor PAFR PAR PKD PKG Prostaglandin Receptor Ras RGS Protein S1P Receptor SGLT Sigma Receptor Somatostatin Receptor TAAR TSH Receptor Urotensin Receptor Vasopressin Receptor

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Epigenetic Reader Domain

Epigenetic regulators of gene expression and chromatin state include so-called writers, erasers, and readers of chromatin modifications.The chromo and bromo domains, which typically bind acetyllysine, the malignant brain tumor (MBT), the plant homeodomain (PHD), and Tudor domains, which typically associate with methyllysine, are well-known examples of reader domains. The identification of selective inhibitors that specifically target members of the bromodomain and extraterminal motif (BET) family of acetyl-lysine readers has had a significant impact on research on epigenetic readers. 46 proteins, containing 61 bromodomains grouped into eight families, are encoded by the human genome. The first BET inhibitors, GSK 525762A and (+)-JQ-1, are discovered using various experimental methods.

Enhancer of zeste homologue 2 (EZH2), a protein from the Polycomb group (PcG), is crucial for promoting histone H3 lysine 27 trimethylation (H3K27me3) and epigenetic gene silencing. This EZH2 function is crucial for cell proliferation, inhibits cell differentiation, and may contribute to the development of cancer. By phosphorylating EZH2, cyclin-dependent kinases control epigenetic gene silencing. Tumor suppressor genes are thought to be silenced by abnormal histone and DNA methylation caused by EZH2 in many cancer types, including lymphomas and leukemia.

In addition to acting as a transcriptional adaptor, p300/CBP also acts as a histone acetyltransferase.

Epigenetic Reader Domain related products

Cat No.	Product Name	CAS No.	Product Description
V35176	TP-238	2415263-04-4	TP-238 is a potent and specific CECR2/BPTF dual probe with IC50s of 30 nM and 350 nM respectively.
V35175	TP-238 hydrochloride	2415263-05-5	TP-238 HCl is an effective and selective CECR2/BPTF dual probe with IC50s of 30 nM and 350 nM respectively.
V40712	TP-472	2079895-62-6	TP-472 is a selective BRD9/7 inhibitor (antagonist) with Kds of 33 nM and 340 nM for BRD9 and BRD7, respectively.
V79846	TRIM24/BRPF1-IN-2		TRIM24/BRPF1-IN-2 (compound 20l) is a potent dual TRIM24/BRPF1 inhibitor (antagonist) with IC50s of 0.98 and 1.16 μM respectively.
V50954	Trotabresib (CC-90010; compound 1)	1706738-98-8	CC-90010 (compound 1) is a reversible, orally bioactive BET inhibitor.
V53254	Tz-Thalidomide	2087490-42-2	Tz-Thalidomide is a tetrazine-tagged Thalidomide , an E3 ligase ligand.
V35161	UMB298	2266569-73-5	UMB298 is a potent and specific CBP/P300 bromodomain inhibitor.
V0086	UNC-926	1184136-10-4	UNC-926 is apotent and selective inhibitor of the L3MBTL1 (Lethal(3)malignant brain tumor-like protein)domain (Kd = 3.9 μM), which is a methyl-lysine (Kme) reader domain.
V53393	UNC1021	1322591-19-4	UNC1021 is a selective L3MBTL3 inhibitor (antagonist) with IC50 of 0.048 μM.
V0426	UNC669	1314241-44-5	UNC669 (UNC-669) is a novel, potent and selective inhibitor of malignant brain tumor (MBT) with anticancer activity.
V35158	UNC926 hydrochloride	1782573-49-2	UNC926 HCl is a methyl-lysine (Kme) reader domain inhibitor that specifically inhibits L3MBTL1 with IC50 of 3.9 μM.
V56145	VinSpinIn	2380021-98-5	VinSpinIn is a Spindlin1 inhibitor (KD: 9.9 nM for SPIN149-262).
V35119	WWL0245	2869057-11-2	WWL0245 is a potent and specific BRD4 PROTAC.
V34727	XY-06-007	2757045-94-4	XY-06-007 is an effective and selective B&H-PROTAC BRD4BD1L94V degrader.
V35112	XY153	2933176-32-8	XY153 (compound 8l) is a BD2-selective BET inhibitor that selectively binds to BRD4 BD2.
V28340	Y06036	1832671-96-1	Y06036 is a potent BET Inhibitors for Potential Treatment of Castration-Resistant Prostate Cancer (CRPC).
V31521	Y06137	2226534-49-0	Y06137 (Y0-6137; Y0 6137)is a novel and potent bromodomain BET inhibitor (Kd= 81 nM.
V56153	Y08175	2223014-57-9	Y08175 is a potent CBP Bromodomain inhibitor.
V35022	Ziftomenib (KO-539)	2134675-36-6	Ziftomenib (KO-539) is an orally bioactive inhibitor of the menin-MLL interaction with anti-tumor activity (WO2017161028A1, compound 151).
V3857	ZL0420	2229039-45-4	ZL0420 (ZL-0420), an analog ofZL0454, is a novel potent and highly selective inhibitor of BRD4 (Bromodomain-Containing Protein 4) with anti-inflammatory activity.