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)

  • GC62144 structure
    GC62144653-47 hydrochloride
    CAS: 1224567-46-7
    纯度: >98.00%

    653-47 hydrochloride 是一种增强剂，能显著增强 666-15 的 cAMP 反应元件结合蛋白 (CREB) 抑制活性。653-47 hydrochloride 也是一种很弱的抑制剂，其 IC50 为 26.3 μM。

  • GC62211 structure
    GC62211dCBP-1
    CAS: 2484739-25-3
    纯度: >99.50%

    dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP by hijacking the E3 ubiquitin ligase CRBN, also is exceptionally potent at killing multiple myeloma cells and can abolish the enhancer that drives MYC oncogene expression.

  • GC62279 structure
    GC62279653-47
    CAS: 1224678-75-4

    653-47 是一种增强剂，能显著增强 666-15 的 cAMP 反应元件结合蛋白 (CREB) 抑制活性。653-47 也是一种很弱的抑制剂，其 IC50 为 26.3 μM。

  • GC62312 structure
    GC62312GSK620
    CAS: 2088410-46-0
    纯度: >99.50%

    GSK620是一种具有口服活性的泛溴结构域和末端外结构域蛋白第二溴结构域的（pan-BET BD2）选择性抑制剂。

  • GC62330 structure
    GC62330CC-90010
    CAS: 1706738-98-8
    纯度: >99.50%

    A BRD4 inhibitor

  • GC62405 structure
    GC62405UMB298
    CAS: 2266569-73-5

    UMB298 是一种有效的选择性 CBP/P300 溴域抑制剂。

  • GC62591 structure
    GC62591LT052
    CAS: 2543545-44-2
    纯度: >98.00%

    LT052 是一种高选择性 BET BD1 抑制剂，其 IC50 为 87.7 nM。LT052 表现出纳摩尔级别的 BRD4 BD1 的抑制活性，选择性是 BRD4 BD2 的 138 倍 (IC50=12.130 μM)。LT052 具有抗炎活性，可用于急性痛风性关节炎研究。

  • GC62606 structure
    GC62606PROTAC BRD4 Degrader-8
    纯度: >97.00%

    PROTAC BRD4 Degrader-8 是一种有效的 BRD4 抑制剂，对 BRD4 BD1 和 BD2 的 IC50 值分别为 1.1 nM 和 1.4 nM。PROTAC BRD4 Degrader-8 能够有效降解 PC3 前列腺癌细胞中的 BRD4 蛋白。

  • GC62620 structure
    GC62620NHWD-870
    CAS: 2115742-03-3
    纯度: >98.00%

    NHWD-870 inhibits CSF1 expression through suppressing BRD4 and its target HIF1α.

  • GC62654 structure
    GC62654GSK778
    CAS: 2451862-42-1
    纯度: >99.00%

    GSK778 (iBET-BD1) is a strong BD1 bromodomain inhibitor of the BET proteins, with IC50 value of 75 nM for BRD2 BD1, 41 nM for BRD3 BD1, 41 nM for BRD4 BD1, and 143 nM for BRDT BD1.

  • GC63064 structure
    GC63064Menin-MLL inhibitor 19
    CAS: 2360487-93-8
    纯度: >98.00%

    Menin-MLL inhibitor 19，一种有效的 menin-mll 相互作用的抑制剂，例如 A17，源于专利 WO2019120209A1。Menin-MLL inhibitor 19 可用于多种疾病的研究，例如癌症、骨髓增生异常综合征 (MDS) 和糖尿病。

  • GC63178 structure
    GC63178RVX-297
    CAS: 1044871-04-6
    纯度: >96.00%

    RVX-297 是一种高效、具有口服活性、对 BD2 有选择性的 BET 抑制剂。RVX-297 对 BRD2(BD2)，BRD3(BD2)，BRD4(BD2) 的 IC50 分别为 0.08、0.05、0.02 μM。RVX-297 抑制多种免疫细胞炎症基因的表达。RVX-297 对临床前模型急性炎症和自身免疫的有效。

  • GC63528 structure
    GC63528BET bromodomain inhibitor 1
    CAS: 2411226-02-1
    纯度: >95.00%

    BET bromodomain inhibitor 1 是一种具有口服活性的，选择性 BET 溴结构域抑制剂，对 BRD4 的 IC50 为 2.6 nM。BET bromodomain inhibitor 1 与 BRD2(2)，BRD3(2)，BRD4(1)，BRD4(2) 和 BRDT(2) 高亲和力结合 (Kd 值分别为 1.3 nM、1.0 nM、3.0 nM、1.6 nM、2.1 nM)。BET bromodomain inhibitor 1 具有抗癌活性。

  • GC63538 structure
    GC63538Menin-MLL inhibitor 20
    CAS: 2448173-47-3

    Menin-MLL inhibitor 20 是一种不可逆的 menin-MLL 相互作用的抑制剂，具有抗肿瘤活性 (WO2020142557A1, compound 6)。

  • GC63694 structure
    GC63694BAZ1A-IN-1
    CAS: 941521-45-5

    BAZ1A-IN-1 is a potent inhibitor of BAZ1A (bromodomain-containing protein), exerting a Kd value of 0.52 μM against BAZ1A bromodomain, shows good anti-viability activity against cancer cell lines expressing a high level of BAZ1A, but weak or no activity against cancer cells with a low expression level of BAZ1A.

  • GC63887 structure
    GC63887SGC-SMARCA-BRDVIII
    CAS: 1997319-84-2
    纯度: >99.00%

    SGC-SMARCA-BRDVIII is a potent and selective SMARCA2/4 BRD inhibitor.

  • GC64040 structure
    GC64040VTP50469 fumarate
    CAS: 2169919-29-1
    纯度: >98.00%

    VTP50469 fumarate 是一种有效的，高选择性和口服活性的 Menin-MLL 相互作用抑制剂，Ki 为 104 pM。VTP50469 fumarate 具有高效的抗白血病活性。

  • GC64271 structure
    GC64271AU-15330
    CAS: 2380274-50-8
    纯度: >99.00%

    AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4, which can induce potent inhibition of tumor growth in xenograft models of prostate cancer.

  • GC64297 structure
    GC64297I-BET567
    CAS: 1887237-54-8

    I-BET567 是一种有效、具有口服活性 pan-BET 候选抑制剂，对 BRD4 BD1 和 BD2 的 pIC50s 分别为 6.9 和 7.2。I-BET567 已在肿瘤和炎症小鼠模型中已被证明有效。

  • GC64518 structure
    GC64518Ziftomenib
    CAS: 2134675-36-6
    纯度: >98.00% / >99.50%

    Ziftomenib是一种高选择性具口服活性的Menin-MLL（混合谱系白血病）相互作用抑制剂，用于治疗复发或难治性急性髓系白血病（AML）。

  • GC64529 structure
    GC64529ZL0590
    CAS: 2230496-99-6

    ZL0590 是一种有效的，具有口服活性 BRD4 BD1 选择性抑制剂，对人 BRD4 BD1的 IC50 为 90 nM。ZL0590 具有显著的抗炎活性。

  • GC64538 structure
    GC64538BPTF-IN-BZ1
    纯度: >97.00%

    BPTF-IN-BZ1 是一种 BPTF 抑制剂，具有高效价（Kd = 6.3 nM）。

  • GC64541 structure
    GC64541BRM/BRG1 ATP Inhibitor-2
    CAS: 2368900-77-8
    纯度: >99.50%

    BRM/BRG1 ATP Inhibitor-2 是一种 BRG1/BRM ATP 酶抑制剂，治疗 BAF 相关疾病。

  • GC64696 structure
    GC64696CBP/p300-IN-12
    CAS: 2738688-57-6
    纯度: >99.00%

    CBP/p300-IN-12 是一种有效的选择性共价组蛋白乙酰转移酶 p300 (IC50 为 166 nM) 和 CBP 抑制剂。CBP/p300-IN-12 降低 PC-3 细胞的 H3K27Ac 水平 (EC50 为 37 nM)。CBP/p300-IN-12 可与 C1450 形成共价加合物。