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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V3187 | PLX51107 | 1627929-55-8 | PLX51107 is a novel, potent and selectiveBET (Bromodomain and Extra-Terminal motif) inhibitor, also called BRD4 (bromodomain and extra terminal domain) inhibitor withKdvalues of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; BRD4 is overexpressed in CLL and is enriched proximal to genes upregulated orde novoexpressed in CLL with known functions in disease pathogenesis and progression. |
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V52926 | PROTAC BET Degrader-10 | 1957234-97-7 | PROTAC BET Degrader-10 is an effective BET BRD4 degrader, which is connected by Cereblon ligand and BRD4 ligand. |
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V53078 | PROTAC BRD4 Degrader-10 | 2417370-49-9 | PROTAC BRD4 Degrader-10 (compound 8b) is a potent PROTAC linked to a von Hippel-Lindau ligand and a BRD4 ligand. |
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V76599 | PROTAC BRD4 Degrader-11 | PROTAC BRD4 Degrader-11 (compound 9a) is a potent PROTAC linked to a von Hippel-Lindau ligand and a BRD4 ligand. | |
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V53105 | PROTAC BRD4 Degrader-12 | 2417370-90-0 | PROTAC BRD4 Degrader-12 (compound 9c) is a PROTAC consisting of a von Hippel-Lindau ligand linked to a BRD4 ligand. |
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V54470 | PROTAC BRD4 Degrader-13 | 2417370-71-7 | PROTAC BRD4 Degrader-13 (compound 9d) is a PROTAC consisting of a von Hippel-Lindau ligand linked to a BRD4 ligand. |
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V81223 | PROTAC BRD4 Degrader-14 | PROTAC BRD4 Degrader-14 is a PROTAC linked to a von Hippel-Lindau ligand and a BRD4 ligand with IC50s of 1.8 nM and 1.7 nM for BRD4 BD1 and BD2, respectively. | |
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V40979 | PROTAC BRD4 Degrader-15 | 2417370-67-1 | PROTAC BRD4 Degrader-15 is a PROTAC linked to a von Hippel-Lindau ligand and a BRD4 ligand with IC50s of 7.2 nM and 8.1 nM for BRD4 BD1 and BD2, respectively. |
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V56154 | PROTAC BRD4 Degrader-19 | 2684292-71-3 | PROTAC BRD4 Degrader-19 (Compound 176) is a PROTAC that targets BRD4 protein for degradation. |
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V56152 | PROTAC BRD4 Degrader-20 | 2086300-61-8 | PROTAC BRD4 Degrader-20 (compound 195) is a bifunctional compound and a BRD4 degrader. |
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V56136 | PROTAC BRD4 Degrader-21 | 2503036-46-0 | PROTAC BRD4 Degrader-21 (Comp 74) is a BRD4 degrader. |
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V40976 | PROTAC BRD4 Degrader-7 | 2413382-30-4 | PROTAC BRD4 Degrader-7 is a potent bromodomain BRD4 degrader with IC50s of 15.5 and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively. |
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V76598 | PROTAC BRD4 Degrader-8 | PROTAC BRD4 Degrader-8 is a PROTAC linked to a von Hippel-Lindau ligand and a BRD4 ligand with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. | |
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V54464 | PROTAC BRD4 Degrader-9 | 2417370-42-2 | PROTAC BRD4 Degrader-9 (compound 8a) is a potent PROTAC consisting of a von Hippel-Lindau ligand linked to a BRD4 ligand. |
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V53118 | PROTAC BRD9 Degrader-6 | 2676211-62-2 | PROTAC BRD9 Degrader-6 is a potent BRD9 degrader (IC50=0.13 nM) and may be utilized in the study of BAF complex-related diseases. |
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V85034 | PROTAC BRM degrader-1 | 2378051-80-8 | |
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V40921 | PROTAC CBP/P300 Degrader-1 | 2484739-48-0 | PROTAC CBP/P300 Degrader-1 is an effective PROTAC CBP/P300 degrader. |
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V83620 | PROTAC SMARCA2 degrader-3 | 3024266-69-8 | |
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V0417 | SGC-CBP30 | 1613695-14-9 | SGC-CBP30 is a novel, potent and selective inhibitor of CREBBP (CBP/KAT3A) and its paralogue EP300 (KAT3B) with the potential to be used in neurodegenerative diseases (e. |
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V35970 | SJ1461 | 2924546-70-1 | SJ1461 is a potent orally bioactive BET inhibitor. |
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