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Epigenetic Reader Domain

Inhibitory Selectivity

Catalog No.Inhibitor Name Epigenetic Reader Domain
A12729(*)-JQ1
***
A11783I-BET151
*
A12545PFI-1
**
A11440I-BET-762
***
A13956RVX-208
*
A13227SGC-CBP30
****
A13163Bromosporine
****
A13890OTX015
****
A12948UNC1215
**
A13717UNC669
*
A14133GSK1324726A
***
A13749MS436
**
A13068CPI-203
***
A13957PFI-3

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

产品 51 到 81 共 81个

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  1. BRD7-IN-1 free base
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    BRD7-IN-1 free base

    Catalog No. A21530
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    BRD7-IN-1 free base, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC50s of 4.5 and 1.8 nM, respectively). 了解更多
  2. TPOP146
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    TPOP146

    Catalog No. A12655
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    CBP/P300 benzoxazepine bromodomain inhibitor
    TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4. 了解更多
  3. PF-CBP1
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    PF-CBP1

    Catalog No. A15876
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    CREBBP 抑制剂
    PF-CBP1是CREB结合蛋白（CREBBP）溴结构域的高度选择性抑制剂，它抑制CREBBP和p300溴结构域，IC50分别为125和363 nM。 了解更多
  4. BAZ2-ICR
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    BAZ2-ICR

    Catalog No. A15947
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    BAZ2 bromodomain 抑制剂
    BAZ2-ICR是用于体外和体内BAZ2溴结构域功能研究的出色化学探针。 了解更多
  5. OF-1
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    OF-1

    Catalog No. A16000
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    BRPF1B/BRPF2 bromodomain 抑制剂
    OF-1是BRPF溴结构域的化学探针。OF-1已显示以100 nM的KD（ITC）结合到BRPF1B，以500 nM的KD（ITC）结合到BRPF2和以2.4 uM的KD（ITC）结合到BRPF3。 了解更多
  6. PF-4
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    PF-4

    Catalog No. A13451
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    BRPF1 bromodomain 抑制剂
    PFI-4是一种有效的，选择性的且细胞可渗透的BRPF1溴结构域抑制剂（IC50 = 80 nM）。相对于包括BRPF2（BRD1），BRPF3和BRD4在内的其他溴结构域，BRPF1的选择性> 100倍。 了解更多
  7. CPI 0610
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    CPI 0610

    Catalog No. A16076
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    BET bromodomain 抑制剂
    CPI 0610是Bromodomain和Extra-Terminal（BET）蛋白家族的小分子抑制剂，具有潜在的抗肿瘤活性。 了解更多
  8. GSK 5959
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    GSK 5959

    Catalog No. A16092
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    BRPF1 bromodomain 抑制剂
    GSK 5959是一种有效的，选择性的且可透过细胞的BRPF1溴结构域抑制剂，IC50?80 nM。在35个其他溴结构域（包括BRPF2/3和BET家族溴结构域）中，对BRPF1的选择性超过100倍。 了解更多
  9. EML 425
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    EML 425

    Catalog No. A16180
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    CBP/p300 抑制剂
    EML 425是一种可逆且非竞争性的CBP/p300抑制剂，具有细胞渗透性（IC50值分别为1.1和2.9 uM）。 了解更多
  10. UNC 926 hydrochloride
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    UNC 926 hydrochloride

    Catalog No. A15367
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    MBT Domain (L3MBTL1) 抑制剂
    UNC 926 hydrochloride是甲基赖氨酸阅读器域抑制剂。 了解更多
  11. GSK6853
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    GSK6853

    Catalog No. A16330
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    BRPF1 bromodomain 抑制剂
    GSK6853是BRPF1溴结构域的有效和选择性抑制剂。与所有其他溴结构域相比，它显示出优异的BRPF1效能（pKd 9.5）和大于1600倍的选择性。 了解更多
  12. CeMMEC13
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    CeMMEC13

    Catalog No. A16355
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    TAF1 抑制剂
    CeMMEC13是一种异喹啉酮，可选择性抑制TAF1的第二个溴结构域（IC50 = 2.1μM）。 了解更多
  13. OXF BD 02
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    OXF BD 02

    Catalog No. A16366
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    BRD4 抑制剂
    OXF BD 02，BRD4第一个溴结构域的选择性抑制剂 (BRD4(1))( IC50 = 382 nM )。在CBP溴结构域上对BRD4(1)表现出2-3倍的选择性，并且对一系列其他溴结构域几乎没有亲和力。 了解更多
  14. GW841819X
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    GW841819X

    Catalog No. A16367
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    BET 抑制剂
    GW841819X是(+)-JQ1的类似物，是BET溴结构域的新型抑制剂。GW841819X是单个对映异构体，但在苯并二氮杂3.环3的4位具有不确定的手性。 了解更多
  15. BET-BAY 002
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    BET-BAY 002

    Catalog No. A16368
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    BET 抑制剂
    BET-BAY 002是一种有效的BET抑制剂，对多发性骨髓瘤模型有效。 了解更多
  16. CPI-637
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    CPI-637

    Catalog No. A16470
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    CBP/EP300 bromodomain 抑制剂
    CPI-637是一种选择性的，具有细胞活性的苯并二氮杂酮CBP/EP300溴结构域抑制剂。 了解更多
  17. ZL0420
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    ZL0420

    Catalog No. A16829
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    BRD4 抑制剂
    ZL0420是一种有效的选择性BRD4抑制剂，对BRD4 BD1的IC50值分别为27 nM，对BRD4 BD2的IC50值比相关BRD2同系物的选择性高。 了解更多
  18. A-485
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    A-485

    Catalog No. A16830
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    p300/CBP 抑制剂
    A-485是p300/CBP的强效选择性HAT抑制剂，在p300 TR-FRET分析中的IC50为10 nM，在CBP TR-FRET分析中的IC50为3 nM，选择性是紧密相关的HAT的1000倍以上。 了解更多
  19. ABBV-744
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    ABBV-744

    Catalog No. A16831
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    BET bromodomain 抑制剂
    ABBV-744是一种BDII选择性BET溴结构域抑制剂，正在研究中，用于治疗AML和对去势抵抗的前列腺癌。 了解更多
  20. BAY1238097
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    BAY1238097

    Catalog No. A16881
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    BET 抑制剂
    BAY1238097是一种有效的选择性BET抑制剂。BAY1238097与BET蛋白BRD上的乙酰化赖氨酸识别基序结合，从而防止BET蛋白与组蛋白之间的相互作用。 了解更多
  21. HJB-97
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    HJB-97

    Catalog No. A16872
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    BET bromodomian 抑制剂
    HJB-97是一种有效的BET溴甲烷抑制剂。它以BRD2/3/4 BD1和BD2为目标。 了解更多
  22. ARV-825
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    ARV-825

    Catalog No. A16859
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    BRD4 抑制剂
    ARV-825是一种异质双功能分子，由BRD4结合部分与E3连接酶脑结合部分组成，采用蛋白水解靶向嵌合体（PROTAC）技术连接。 了解更多
  23. dBET1
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    dBET1

    Catalog No. A16858
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    BRD4 protein degrader
    dBET1是基于PROTAC技术的有效BRD4蛋白降解剂，EC50为430 nM。 了解更多
  24. E-7386
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    E-7386

    Catalog No. A17089
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    CBP/beta-catenin modulator
    E-7386是一种活性CBP /β-catenin调节剂。 了解更多
  25. TP-472
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    TP-472

    Catalog No. A17180
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    BRD9/7 抑制剂
    TP-472是有效的BRD9/7抑制剂，Kd分别为33和340 nM。 了解更多
  26. CF53
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    CF53

    Catalog No. A17175
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    BET 抑制剂
    CF53是一种溴结构域和末端（BET）溴结构域抑制剂，IC50值为11.7 nM。 了解更多
  27. MZ1
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    • 最新产品

    MZ1

    Catalog No. A17014
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    BRD4 protein degrader
    MZ1是BRD2和BRD3上BRD4可逆，持久和选择性去除的有效诱导剂。 了解更多
  28. PLX51107
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    PLX51107

    Catalog No. A18345
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    selective BET inhibitor
    PLX51107 is a potent and selective BET inhibitor, with Kds 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; PLX51107 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range). 了解更多
  29. Mivebresib (ABBV-075)
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    • 最新产品

    Mivebresib (ABBV-075)

    Catalog No. A17226
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    BET inhibitor
    Mivebresib, also known as ABBV-075, is a potent BET inhibitor (bromodomain (BRD)-containing proteind) with potential antineoplastic activity. 了解更多
  30. MS402
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    MS402

    Catalog No. A18866
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    BRD inhibitor
    MS402 is a BD1-selective BET BrD inhibitor with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. 了解更多
  31. GNE-207
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    GNE-207

    Catalog No. A18844
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    CBP bromodomain inhibitor
    GNE-207 is a novel, potent, and orally bioavailable inhibitor of the bromodomain of CBP. GNE-207 has excellent CBP potency (CBP IC50?=?1?nM, MYC EC50?=?18?nM), and it exhibits a good pharmacokinetic profile. 了解更多

产品 51 到 81 共 81个

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作用机制
  1. Inhibitor (抑制剂) (70)
  2. Modulator (调节剂) (1)
  3. Degrader (降解剂) (7)
靶点
  1. BAZ2A (2)
  2. BAZ2B (2)
  3. BET (5)
  4. BRD2 (7)
  5. BRD3 (4)
  6. BRD4 (9)
  7. BRD7 (1)
  8. BRD9 (4)
  9. BRPF1 (4)
  10. BRPF2 (1)
  11. CECR2 (1)
  12. KAT5 (Tip60) (1)
  13. L3MBTL (2)
  14. L3MBTL1 (1)
  15. p300/CBP (7)
  16. PCAF (1)
  17. SMARCA4 (1)
  18. TAF1 (1)
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