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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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. |
|
V52976 | CBP/p300-IN-1 | 2443789-32-8 | CBP/p300-IN-1 is a CBP/EP300 bromodomain inhibitor. |
|
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. |
|
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). |
|
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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V52263 | CEM114 | 2279062-54-1 | CEM114 is a potent chemical epigenetic modifier (CEM) that recruits endogenous chromatin machinery through the CRISPR-Cas9 system. |
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V56131 | cis-MZ 1 | 1797406-72-4 | cis-MZ 1 is the negative control (NC) of MZ 1. |
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V0424 | CPI-203 (RO-6870810, TEN-010, JQ2, and RG-6146) | 1446144-04-2 | CPI-203 (RO6870810, JQ-2,TEN010, RG6146) is a novel, selective, cell permeable and orally bioavailable BET bromodomain inhibitor with anticancer activity. |
|
V18762 | CPI-268456 | 1380087-86-4 | CPI-268456 is an inhibitor ofbromodomain-containing protein 4 (BRD4), binding to BRD4 (IC50 =<0.5 µM in a cell-free assay) and inhibiting LPS-induced IL-6 secretion in THP-1 cells (IC50 = <0.5 µM). |
|
V2608 | CPI-637 | 1884712-47-3 | CPI-637 is a novel, potent, selective and cell-bioactive benzodiazepinone analog that acts as a CBP/EP300 bromodomain inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respectively. |
|
V75498 | CREB-IN-1 TFA | 2912285-84-6 | CREB-IN-1 TFA is a potent, orally bioactive CREB inhibitor (IC50=0.18 µM). |
|
V19243 | dBET57 | 1883863-52-2 | dBET57 is a novel BRD4 heterobifunctional small-molecule ligand (PROTAC) which exhibits significant and selective degradation of BRD4 BD1 but is inactive on BRD4 BD2. |
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V79029 | DBr-1 | DBr-1 is a potent BRD9 degrader. | |
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V84538 | dBRD 9-A | 2170679-42-0 | |
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V52198 | dBRD4-BD1 | 2839318-19-1 | dBRD4-BD1 is a selective and persistent BRD4 degrader with DC50 of 280 nM (Dmax=77%). |
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V56122 | DC-BPi-03 | 2758411-46-8 | DC-BPi-03 is a potent BPTF-BRD inhibitor (antagonist) with IC50 of 698.3 nM and Kd of 2.81 μM. |
|
V52196 | DC-BPi-11 | 2758411-61-7 | DC-BPi-11 is an inhibitor (blocker/antagonist) of bromodomain PHD finger transcription factor (BPTF) with IC50 of 698 nM. |
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