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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V41034 | PBRM1-BD2-IN-5 | 2819989-61-0 | PBRM1-BD2-IN-5 is a potent PBRM1 bromodomain inhibitor (antagonist) with Kd of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and IC50 of 0.26 μM for PBRM1-BD2. |
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V41033 | PBRM1-BD2-IN-6 | 2819989-67-6 | PBRM1-BD2-IN-6 is a potent inhibitor of the PBRM1 bromodomain with IC50 of 0.22 µM. |
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V41032 | PBRM1-BD2-IN-7 | 2819989-68-7 | PBRM1-BD2-IN-7 is a selective and cellularly active PBRM1 bromodomain inhibitor. |
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V41031 | PBRM1-BD2-IN-8 | 2819989-75-6 | PBRM1-BD2-IN-8 (compound 34) is a potent PBRM1 Bromodomain inhibitor (PBRM1-BD2 Kd=4.4 μM, PBRM1-BD2 IC50=0.16 μM; PBRM1-BD5 Kd=25 μM), which has anti- cancer 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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V2348 | PF-CBP1 | 1962928-21-7 | PF-CBP1 is a selective inhibitor of the bromodomain of CREB-binding protein. |
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V3409 | PF-CBP1 | 962928-21-7 | PF-CBP1 (also known as PF-06670910) is a novel, potent and highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). |
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V2049 | PF-CBP1 HCl | 2070014-93-4 | PF-CBP1 HCl (also known as PF-06670910 HCl) is a novel, potent and highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). |
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V0413 | PFI-1 (PF-6405761) | 1403764-72-6 | PFI-1(PF6405761) is a novel, highly potent and selective BET (bromodomain-containing protein) inhibitor with antineoplastic activity. |
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V0423 | PFI-3 | 1819363-80-8 | PFI-3 (PFI3) isa potent, selective, acetyl-lysine-competitive, and cell-permeable inhibitor of SMARCA bromodomains (SMARCA2/4 and PB1(5)) with antineoplastic activity. |
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V0416 | PFI-4 | 900305-37-5 | PFI-4 is a novel, potent,cell permeableand selective inhibitor of bromodomain and PHD finger-containing protein 1 (BRPF1) with antineoplastic activity. |
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V56144 | Phoenixin-20 (PNX-20) | 1415039-77-8 | Phoenixin-20 (PNX-20) is a biologically active peptide with hormone-like effects in vertebrates, which can stimulate hypothalamic-pituitary-gonadal hormones and regulate mammalian reproductive processes. |
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V81121 | Phoenixin-20 TFA (PNX-20 TFA) | PPhoenixin-20 (TFA) (PNX-20 (TFA)) is a biologically active peptide with hormone-like effects in vertebrates, stimulating hypothalamic-pituitary-gonadal hormones and regulating mammalian reproductive processes. | |
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V41008 | Physachenolide C | 791117-61-8 | Physachenolide C is an effective and selective BET inhibitor that can cause apoptosis and arrest the cell cycle in the G0-G1 phase, and has anti-tumor activity. |
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V41006 | PI3K/Akt/CREB activator 1 | 2708177-73-3 | PI3K/Akt/CREB activator 1 (compound AE-18) is an orally bioavailable activator of PI3K/Akt/CREB. |
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V78461 | PLK1-IN-6 | PLK1-IN-6 is a potent and specific inhibitor of PLK1 with IC50 of 0.45 nM. | |
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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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