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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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 | 2999742-92-4 | 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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V103479 | CCW 28-3 | 2361142-23-4 | CCW 28-3 is a BRD4 degrader based on PROTAC technology, and its mode of action is dependent on the proteasome and RNF4 (pink: JQ-1 (carboxylic acid); black: linker; blue: RNF4 ligand CCW16). |
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V102289 | CDC14A/B-IN-1 | 3048655-03-1 | CDC14A/B-IN-1 (Compound 15) is an orally available CDC14A/B phosphatase inhibitor with Ki of 57.4 nM (CDC14A) and 90.0 nM (CDC14B), respectively. |
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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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V94064 | CFT-1297 | CFT-1297 is a BET PROTAC degrader that degrades BRD4. | |
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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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V102516 | cis-MZ 1 hydrate | cis-MZ 1 hydrate is a negative control for PROTAC MZ 1 targeting BRD4. | |
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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. |
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V2609 | Pelabresib (CPI0610) | 1380087-89-7 | Pelabresib (CPI-0610; CPI0610) is a potent and selective benzoisoxazoloazepine BET (Bromodomain and Extra-Terminal) bromodomain inhibitor (IC50 = 39 nM) with anticancer effects. |
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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). |
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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. |
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V75498 | CREB-IN-1 TFA | 2912285-84-6 | CREB-IN-1 TFA is a potent, orally bioactive CREB inhibitor (IC50=0.18 µM). |
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V97409 | CW-3308 | 3055592-99-6 | CW-3308 is an orally available PROTAC that selectively targets BRD9 and has the potential to inhibit synovial sarcoma, rhabdoid tumors, and other BRD9-dependent human diseases. |
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V94909 | CZL-046 | 3032444-02-0 | CZL-046 (Compound 29) is an orally available p300 bromodomain inhibitor. |
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V104393 | dBAZ2 | dBAZ2 is a first-in-class PROTAC degrader targeting BAZ2A and BAZ2B, with DC50 values of 180 nM and 250 nM for BAZ2A and BAZ2B, respectively. | |
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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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