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.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V75494 | ZL0420 | 2230496-80-5 | ZL0420 is a potent and specific BET bromodomain 4 (BRD4) inhibitor (antagonist) with IC50s of 27 nM and 32 nM for BRD4 BD1 and BRD4 BD2, respectively. |
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V3860 | ZL0454 | 2229042-77-5 | ZL0454 (ZL-0454), an analog of ZL0420, is a novel potent and highly selective inhibitor of BRD4 (Bromodomain-Containing Protein 4) with nanomolar binding affinities to bromodomains (BDs) of BRD4. |
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V53367 | ZL0590 | 2230496-99-6 | ZL0590 is a potent, orally bioactive BRD4 BD1 selective inhibitor (antagonist) with IC50 of 90 nM for human BRD4 BD1. |
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V56130 | ZLD2218 | 2713974-32-2 | Inhibiting BRD4 can improve renal damage and fibrosis. |
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