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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V56150 | BRD4-IN-4 | 304685-40-3 | BRD4-IN-4 (Compound 1) is a BRD4 inhibitor (IC50=6.83 μM). |
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V75493 | BRD7-IN-1 | 2448414-48-8 | BRD7-IN-1 is a modified BI7273 analogue (BRD7/9 inhibitor), which forms PROTAC VZ185 by connecting with VHL ligand (the DC50 of VZ185 inhibiting BRD7/9 is 4.5 nM and 1.8 nM respectively). |
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V80142 | BRD7-IN-2 | BRD7-IN-2 (compound 2-77) is a potent bromodomain-containing protein 7 (BRD7) inhibitor targeting prostate cancer cells. | |
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V80145 | BRD7-IN-3 | BRD7-IN-3 (compound 1-78) is a dual (bifunctional) inhibitor of bromodomain-containing proteins BRD7/BRD9 with IC50s of 1.6 μM and 2.7 μM respectively. | |
|
V78547 | BRD9 Degrader-1 | BRD9 Degrader-1 is a BRD9 degrader. | |
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V2478 | BRM/BRG1 ATP Inhibitor-1 | 2270879-17-7 | BRM/BRG1 ATP Inhibitor-1 is an orally bioactive inhibitor of Brahma Homolog (BRM)/SMARCA2 ATPase with anticancer activity and has potential to be used for the treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers. |
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V52322 | BRM/BRG1 ATP Inhibitor-3 | 2368901-31-7 | BRM/BRG1 ATP Inhibitor-3 is a BRG1/BRM inhibitor. |
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V56127 | BRM/BRG1 ATP Inhibitor-4 | 2422030-94-0 | BRM/BRG1 ATP Inhibitor-4 is a BRG1/BRM inhibitor. |
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V52353 | Bromodomain IN-2 | 2445335-77-1 | BD-IN-1 is a pan-bromodomain (BD) inhibitor (antagonist) with Kds of 250, 420, and 420 for BRD4(1), CBP, BRPF1B, BRD7, BRD9, BRDT(1), and CECR2 respectively. |
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V56143 | Bromodomain inhibitor-12 | 2010124-06-6 | Bromodomain inhibitor-12 (example 303) is a bromodomain inhibitor that may be utilized in study/research of autoimmune and inflammatory diseases. |
|
V56129 | Bromodomain inhibitor-12 (edisylate) | 2010124-27-1 | Bromodomain inhibitor-12 edisylate (example 303) is a bromodomain inhibitor that may be utilized in the research of autoimmune and inflammatory diseases. |
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V33302 | Bromodomain inhibitor-8 | 1300031-70-2 | Bromodomain inhibitor-8 is a novel and potent BET bromodomain inhibitor with the potential to be used in the treatment of autoimmune and inflammatory diseases. |
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V0418 | Bromosporine | 1619994-69-2 | Bromosporine is a novel, potent and broad spectrum inhibitor against BET bromodomains with potential use as a chemical probe for bromodomain functional assays. |
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V56141 | CBP-IN-1 | 1936431-44-5 | CBP-IN-1 (compound 12) is a potent CBP inhibitor (antagonist) with IC50 of 1.5 nM. |
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V52976 | CBP/p300-IN-1 | 2443789-32-8 | CBP/p300-IN-1 is a CBP/EP300 bromodomain inhibitor. |
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V52295 | CBP/p300-IN-12 | 2738688-57-6 | CBP/p300-IN-12 is a potent and specific covalent inhibitor of histone acetyltransferase p300 (IC50 of 166 nM) and CBP. |
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V56065 | CBP/p300-IN-14 | 2725036-10-0 | CBP/p300-IN-14 is a potent CBP/EP300 (lysine acetyltransferase) inhibitor (antagonist) with IC50 of 3.3 nM (disclosed in patent WO2021213521A1, compound 27). |
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V78676 | CBP/p300-IN-20 | CBP/p300-IN-20 is a potent and specific inhibitor of p300/CBP with pIC50 of 10.1 for p300. | |
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V56064 | CBP/p300-IN-21 | 1065581-69-2 | CBP/p300-IN-21 (Compound 5d) is a selective CBP/p300 inhibitor (IC50= IC50s for p300 and CBP are 0.07 and 1.755 μM, respectively). |
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V53145 | CBP/p300-IN-8 | 2304416-91-7 | CBP/p300-IN-8 is a potent inhibitor of the CBP/P300 bromodomain family. |
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