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)

  • GC38474 structure
    GC38474MS645
    CAS: 2250091-96-2
    纯度: >98.00%

    MS645 是一种 BET bromodomains (BrD) 抑制剂，对于 BRD4-BD1/BD2 的 Ki 值为 18.4 nM。MS645 在空间上限制 BRD4 BrDs 的二价抑制，从而导致实体肿瘤细胞中 BRD4 转录活性的持续抑制。

  • GC39180 structure
    GC39180PROTAC BRD4 ligand-1
    CAS: 2313230-51-0
    纯度: >99.50%

    PROTAC BRD4 ligand-1 是一种有效的 BET 抑制剂，是靶向 BRD4 蛋白的配体。

  • GC39252 structure
    GC39252MS31 trihydrochloride
    纯度: >98.00%

    MS31 trihydrochloride 是一种高亲和性和选择性的，片段样的甲基赖氨酸读写蛋白 spindlin 1 (SPIN1) 抑制剂，有效破坏 SPIN1 与 H3K4me3 蛋白互相作用 (IC50=77 nM，AlphaLISA；243 nM，FP). MS31 trihydrochloride 选择性结合 SPIN1 的 Tudor 结构域 II (Kd=91 nM)。MS31 trihydrochloride 能有效抑制含三甲基赖氨酸肽与 SPIN1 的结合，对非肿瘤性细胞无毒。

  • GC39417 structure
    GC39417OXFBD04
    CAS: 2231747-03-6
    纯度: >99.00%

    OXFBD04 是一种有效的选择性 BRD4 抑制剂，IC50 为 166 nM。OXFBD04 是一种有效的 BET 溴结构域配体，对 CREBBP 溴结构域具有额外的适度亲和力。OXFBD04 具有抗癌活性。

  • GC40226 structure
    GC40226Curcumin-d6
    CAS: 1335198-02-1
    纯度: >99.00%

    An internal standard for the quantification of curcumin

  • GC40628 structure
    GC40628TP-472
    CAS: 2079895-62-6
    纯度: >98.00%

    A BRD9 inhibitor

  • GC43889 structure
    GC43889I-CBP112 (hydrochloride)
    CAS: 2147701-33-3
    纯度: >90.00%

    A p300 and CBP inhibitor

  • GC44250 structure
    GC44250MS351
    CAS: 472984-79-5
    纯度: >98.00%

    MS351 is an antagonist of chromobox 7 (CBX7) that acts by binding the CBX7 chromodomain.

  • GC44477 structure
    GC44477NVS-CECR2-1
    CAS: 1992047-61-6
    纯度: >99.00%

    A potent and selective CECR2 inhibitor

  • GC45503 structure
    GC45503L-Moses (hydrochloride)
    纯度: >98.00%

    A PCAF bromodomain inhibitor

  • GC45640 structure
    GC45640TP-238 (hydrochloride)
    CAS: 2415263-05-5
    纯度: >99.00%

    A chemical probe for the bromodomains of CECR2 and BPTF

  • GC50070 structure
    GC50070I-BET 151 dihydrochloride
    CAS: 1883545-47-8

    A BRD2, BRD3, and BRD4 inhibitor

  • GC50182 structure
    GC50182ent-LP 99
    CAS: 1808948-28-8

    ent-LP 99 是一种有效的选择性 BRD7 和 BRD9 抑制剂，对 BRD9 的 KD 为 99 nM。

  • GC50340 structure
    GC50340TC AC 28
    CAS: 1809296-92-1

    High affinity BET bromodomain ligand

  • GC50378 structure
    GC50378GSK 9311 hydrochloride
    CAS: 2253733-09-2

    GSK 9311 hydrochloride 是 GSK6853 活性较低的类似物，可用作阴性对照。 GSK 9311 hydrochloride 抑制 BRPF 溴结构域，对 BRPF1 和 BRPF2 的 pIC50 值分别为 6.0 和 4.3。

  • GC50395 structure
    GC50395L Moses dihydrochloride

    High affinity and selective PCAF bromodomain inhibitor

  • GC50542 structure
    GC50542TP 238
    CAS: 2415263-04-4

    A chemical probe for the bromodomains of CECR2 and BPTF

  • GC60182 structure
    GC60182GSK046
    CAS: 2474876-09-8
    纯度: >98.00%

    A BD2 bromodomain inhibitor

  • GC60184 structure
    GC60184GSK8814
    CAS: 1997369-78-4
    纯度: >98.50%

    GSK8814 是一种高效、选择性的 ATAD2/2B 溴代苯胺化学探针和抑制剂，结合常数pKd=8.1，在 BROMOscan 中的 pKi=8.9。GSK8814 分别以 7.3 和 4.6 的 pIC50 与 ATAD2 和 BRD4 BD1 结合。GSK8814 对 ATAD2 的选择性是 BRD4 BD1 的 500 倍。

  • GC60925 structure
    GC60925IACS-9571 hydrochloride
    CAS: 2319611-93-1
    纯度: >99.00%

    IACS-9571(ASIS-P040)hydrochloride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。

  • GC61212 structure
    GC61212PROTAC BRD4 Degrader-5
    CAS: 2409538-70-9
    纯度: >99.50%

    PROTACBRD4Degrader-5是一种基于PROTAC的BRD4降解剂，可有效降解HER2阳性和阴性乳腺癌细胞系中的BRD4。

  • GC61577 structure
    GC61577CBP/p300-IN-1
    CAS: 2443789-32-8
    纯度: >99.50%

    CBP/p300-IN-1是CBP/EP300溴结构域抑制剂。

  • GC61595 structure
    GC61595(+)-JQ-1-aldehyde
    纯度: >98.00%

    (+)-JQ-1-aldehyde是(+)-JQ1的醛形式。(+)-JQ-1-aldehyde可作为合成PROTACs的前体，靶向BET溴结构域.。

  • GC61841 structure
    GC61841Naphthol AS-E
    CAS: 92-78-4
    纯度: >98.00%

    Naphthol AS-E 是有效的，具有细胞渗透性的 KIX-KID 相互作用的抑制剂。Naphthol AS-E 直接结合 CBP 的 KIX 域 (Kd: 8.6 µM)，阻断 KIX 域和 KID 域的相互作用 (IC50: 2.26 µM)。Naphthol AS-E 可用于癌症研究。