GlpBio

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)

  • GC34437 structure
    GC34437IACS-9571 Hydrochloride (ASIS-P040 Hydrochloride)

    IACS-9571Hydrochloride是溴结构域蛋白TRIM24和BRPF1的抑制剂，对TRIM24的IC50和Kd值分别为8nM和31nM，对BRPF1的Kd值为14nM。

  • GC34443 structure
    GC34443(R)-BAY1238097
    CAS: 1564269-85-7
    纯度: >99.50%

    (R)-BAY1238097是BAY1238097的低活性R型异构体。BAY1238097是一种有效的、BET与组蛋白结合的选择性抑制剂，通过下调c-Myc水平及下游转录组，在AML(急性髓性白血病)和MM(多发性骨髓瘤)模型中表现出较强的抗增殖活性。

  • GC34446 structure
    GC34446(rac)-BAY1238097
    CAS: 1564268-19-4
    纯度: >98.50%

    (rac)-BAY1238097是一种BET抑制剂，对BRD4的IC50值为1.02μM。用于癌症研究。

  • GC34505 structure
    GC34505BRD7-IN-1
    CAS: 2448414-48-8
    纯度: >99.00%

    BRD7-IN-1是一种修饰的BI7273衍生物(BRD7/9抑制剂)，通过与VHL配体连接形成PROTACVZ185(VZ185抑制BRD7/9的DC50分别是4.5nM、1.8nM)。

  • GC34517 structure
    GC34517CBP-IN-1
    CAS: 2222941-37-7
    纯度: >99.50%

    A p300 and CBP inhibitor

  • GC34675 structure
    GC34675Molibresib besylate
    CAS: 1895049-20-3
    纯度: >98.50%

    Molibresibbesylate(GSK525762C;I-BET762besylate)是BET溴结构域抑制剂，IC50为32.5-42.5nM。

  • GC34778 structure
    GC34778SGC-iMLLT
    CAS: 2255338-25-9

    An inhibitor of MLLT1 and MLLT3 YEATS domains

  • GC34958 structure
    GC34958(+)-JQ1 PA
    CAS: 2115701-93-2
    纯度: >98.50%

    A clickable form of (+)-JQ1

  • GC35175 structure
    GC351756-Demethoxytangeretin
    CAS: 6601-66-7
    纯度: >99.00%

    6-?Demethoxytangeretin 6-去甲氧基三苯甲基黄嘌呤是从柑橘 (Citrus depressa) 分离的黄酮。 6-Demethoxytangeretin 具有抗炎和抗过敏活性，通过间变性淋巴瘤激酶 (ALK) 和丝裂原活化蛋白激酶 (MAPK) 途径抑制人肥大细胞中 IL-6 的产生和基因表达。6-?Demethoxytangeretin 促进 CRE 介导的转录 (与海马神经元的学习和记忆相关)。

  • GC35227 structure
    GC35227ACBI1
    CAS: 2375564-55-7
    纯度: >98.00%

    ACBI1 is a potent and cooperative PROTAC degrader of SMARCA2, SMARCA4 and PBRM1 with DC50 of 6 nM, 11 nM and 32 nM for SMARCA2, SMARCA4 and PBRM1 in MV-4-11 cells, respectively. ACBI1 is composed of a bromodomain ligand, a linker, and the E3 ubiquitin ligase VHL. ACBI1 induces anti-proliferative effects and apoptosis.

  • GC35297 structure
    GC35297Alobresib
    CAS: 1637771-14-2
    纯度: >98.00%

    A BET bromodomain inhibitor

  • GC35448 structure
    GC35448AZD5153 6-Hydroxy-2-naphthoic acid
    CAS: 1869912-40-2
    纯度: >99.50%

    AZD-5153 6-hydroxy-2-naphthoic acid (HNT salt) is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor with pKi of 8.3 for BRD4. AZD-5153 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes. NSD3, via H3K36me2, acts as an epigenetic deregulator to facilitate the expression of oncogenesis-promoting genes.

  • GC35505 structure
    GC35505BET-BAY 002
    CAS: 1588521-78-1
    纯度: >99.50%

    BET-BAY 002是BET小分子抑制剂，对多发性骨髓瘤模型有效。

  • GC35506 structure
    GC35506BET-BAY 002 S enantiomer
    CAS: 2070009-49-1

    BET-BAY 002 S enantiomer 是 BET-BAY 002 的 S 型对映异构体。BET-BAY 002 是 BET 抑制剂。

  • GC35552 structure
    GC35552BRD-IN-3
    CAS: 2351938-32-2

    BRD-IN-3 ((R,R)-36n) 是一个强效的P300/CBP 相关因子溴端结构域 (PCAF BRD) 的抑制剂，其IC50 值为 7 nM。BRD-IN-3 也能抑制GCN5 和FALZ。

  • GC35557 structure
    GC35557Bromodomain IN-1
    CAS: 1914120-48-1

    Bromodomain IN-1 是一种有效的选择性 Bromodomain 抑制剂，详细信息请参考专利文献 WO2016069578A1 中的化合物 4。

  • GC35558 structure
    GC35558Bromodomain inhibitor-8
    CAS: 1300031-70-2
    纯度: >98.00%

    Bromodomain inhibitor-8 (Intermediate 21) 是BET 溴端结构域 的抑制剂，可用于治疗自身免疫性和炎症类疾病。

  • GC35815 structure
    GC35815dBET57
    CAS: 1883863-52-2
    纯度: >99.50%

    A PROTAC that drives BRD4 degradation

  • GC35904 structure
    GC35904dTRIM24
    CAS: 2170695-14-2
    纯度: >99.50%

    dTRIM24 是一种选择性的双功能基于 PROTAC 技术的 TRIM24 降解剂。

  • GC36521 structure
    GC36521M89
    CAS: 2363165-42-6
    纯度: >98.50%

    M-89 强效的、特异性的menin 的抑制剂，结合到menin 的Kd 值为1.4 nM。M-89 可抑制Menin-MLL 蛋白之间的相互作用，有治疗混合谱系白血病的潜力。

  • GC36734 structure
    GC36734NI-42
    CAS: 1884640-99-6
    纯度: >99.50%

    An inhibitor of the BRPF1 bromodomain

  • GC36887 structure
    GC36887PF-CBP1 hydrochloride
    CAS: 2070014-93-4

    An inhibitor of the CBP and p300 bromodomains

  • GC36943 structure
    GC36943PNZ5
    CAS: 1629277-36-6

    PNZ5 是一个有效的、异恶唑类的、BET 的广泛抑制剂，有着类似(+)-JQ1 的高选择性和强效作用，其对BRD4(1) 的KD 值为 5.43 nM。

  • GC38049 structure
    GC38049GSK8573
    CAS: 1693766-04-9
    纯度: >98.00%

    GSK8573 是 GSK2801 的非活性对照化合物。GSK8573 与 BRD9 具有结合活性，Kd 值为 1.04 μM，并且对 BAZ2A/B 和其他溴结构域家族无抑制活性。