Epigenetic Reader Domain
Epigenetic Reader Domain(表观识别蛋白结构域)
Epigenetic regulators of gene expression and chromatin state include so-called writers, erasers, and readers of chromatin modifications.Well-characterized examples of reader domains include bromodomains typically binding acetyllysine and chromatin organization modifier (chromo), malignant brain tumor (MBT), plant homeodomain (PHD), and Tudor domains generally associating with methyllysine. Research on epigenetic readers has been tremendously influenced by the discovery of selective inhibitors targeting the bromodomain and extraterminal motif (BET) family of acetyl-lysine readers. The human genome encodes 46 proteins containing 61 bromodomains clustered into eight families. Distinct experimental approaches are used to identify the first BET inhibitors, GSK 525762A and (+)-JQ-1.
The Polycomb group (PcG) protein, enhancer of zeste homologue 2 (EZH2), has an essential role in promoting histone H3 lysine 27 trimethylation (H3K27me3) and epigenetic gene silencing. This function of EZH2 is important for cell proliferation and inhibition of cell differentiation, and is implicated in cancer progression. Cyclin-dependent kinases regulate epigenetic gene silencing through phosphorylation of EZH2. In many types of cancers including lymphomas and leukemia, EZH2 is postulated to exert its oncogenic effects via aberrant histone and DNA methylation, causing silencing of tumor suppressor genes.
p300/CBP is not only a transcriptional adaptor but also a histone acetyltransferase.
Epigenetic Reader Domain 相关产品(242)
- GC16299BET bromodomain inhibitorCAS: 1380087-89-7纯度: >99.50%
BET 溴结构域抑制剂是从专利 WO/2015/153871A2 化合物实施例 11 中提取的一种有效的 BET 抑制剂。
- GC16531Bromodomain Inhibitor, (+)-JQ1CAS: 1268524-70-4纯度: >99.50%
A selective inhibitor of BET bromodomains
- GC17973OTX-015CAS: 202590-98-5纯度: >99.50%
OTX-015 以浓度依赖性方式抑制 BRD2、BRD3 和 BRD4 与乙酰化组蛋白 4 的结合，IC50 值为 92-112nM .OTX-015 在九个 AML 细胞系中的六个和所有四个 ALL 细胞系中测量到显着的生长抑制:HEL IC50 值为 248 nM，NB4 IC50值为 233 nM，NOMO-1 IC50 值为 229 nM，KG1 IC50 值为 198 nM，OCI-AML3 IC50 值为Kasumi IC50 值为 60 nM，Kasumi IC50 值为 17 nM，JURKAT IC50 值为 249 nM，BV-173 IC50 值为 161 nM , TOM-1 IC50 值为 133 nM, RS4-11 IC50 值为 34 nM。
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC15789 | GSK2801 | 1619994-68-1 | >99.50% | |
A probe for BAZ2A/B bromodomains | ||||
| GC16299 | BET bromodomain inhibitor | 1380087-89-7 | >99.50% | |
BET 溴结构域抑制剂是从专利 WO/2015/153871A2 化合物实施例 11 中提取的一种有效的 BET 抑制剂。 | ||||
| GC16531 | Bromodomain Inhibitor, (+)-JQ1 | 1268524-70-4 | >99.50% | |
A selective inhibitor of BET bromodomains | ||||
| GC16599 | CPI-169 | 1450655-76-1 | >98.00% | |
A selective EZH2 inhibitor | ||||
| GC16726 | BI-7273 | 1883429-21-7 | >99.50% | |
A potent BRD9 bromodomain inhibitor | ||||
| GC16763 | NI-57 | 1883548-89-7 | >99.50% | |
A BRPF bromodomain inhibitor | ||||
| GC16817 | BI-9564 | 1883429-22-8 | >99.50% | |
A selective BRD9/7 bromodomain inhibitor | ||||
| GC17073 | I-BET-762 | 1260907-17-2 | >99.00% | |
Inhibitor of BET proteins | ||||
| GC17284 | Anacardic acid | 16611-84-0 | >98.00% | |
A histone acetyltransferase inhibitor | ||||
| GC17482 | OF-1 | 919973-83-4 | >98.00% | |
A bromodomain probe for BRPF proteins | ||||
| GC17973 | OTX-015 | 202590-98-5 | >99.50% | |
OTX-015 以浓度依赖性方式抑制 BRD2、BRD3 和 BRD4 与乙酰化组蛋白 4 的结合，IC50 值为 92-112nM .OTX-015 在九个 AML 细胞系中的六个和所有四个 ALL 细胞系中测量到显着的生长抑制:HEL IC50 值为 248 nM，NB4 IC50值为 233 nM，NOMO-1 IC50 值为 229 nM，KG1 IC50 值为 198 nM，OCI-AML3 IC50 值为Kasumi IC50 值为 60 nM，Kasumi IC50 值为 17 nM，JURKAT IC50 值为 249 nM，BV-173 IC50 值为 161 nM , TOM-1 IC50 值为 133 nM, RS4-11 IC50 值为 34 nM。 | ||||
| GC18508 | BAY-299 | 2080306-23-4 | >99.00% | |
A potent and selective BRD1 inhibitor | ||||
| GC18729 | MZ1 | 1797406-69-9 | >99.00% | |
A PROTAC that drives BRD4 degradation | ||||
| GC18731 | LP99 | 1808951-93-0 | >98.50% / >99.50% | |
A selective inhibitor of BRD7/9 | ||||
| GC18750 | NEO2734 | 2081072-29-7 | >99.50% | |
NEO2734 (EP31670) 是一种口服有效的双重 p300/CBP 和 BET 溴结构域选择性抑制剂，对 p300/CBP 和 BET 溴结构域的 IC50 值均 <30 nM。 NEO2734 在 SPOP 突变型和野生型前列腺癌中具有活性。 | ||||
| GC19038 | ARV-825 | 1818885-28-7 | >99.00% | |
A BRD4 inhibitor that drives BRD4 degradation | ||||
| GC19098 | CeMMEC1 | 440662-09-9 | >99.50% | |
A selective TAF1 bromodomain 2 inhibitor | ||||
| GC19119 | dBET1 | 1799711-21-9 | >98.00% | |
A hybrid molecule containing (+)-JQ-1 and thalidomide | ||||
| GC19200 | INCB-057643 | 1820889-23-3 | >98.00% | |
A BET family protein inhibitor | ||||
| GC19210 | JQ-1 carboxylic acid | 202592-23-2 | >99.00% | |
A selective inhibitor of BET bromodomains | ||||
| GC19246 | MI-463 | 1628317-18-9 | >99.50% | |
An inhibitor of menin-MLL fusion protein interactions | ||||
| GC19247 | MI-503 | 1857417-13-0 | >99.50% | |
MI-503 是一种高效且具有口服生物利用度的 menin-mLL 相互作用的小分子抑制剂。 | ||||
| GC19248 | Mivebresib | 1445993-26-9 | >99.00% | |
A BRD2, BRD4, and BRDT inhibitor | ||||
| GC19298 | PLX51107 | 1627929-55-8 | >99.50% | |
A BET family protein inhibitor | ||||