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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 1 到 50 共 81个

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  1. 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
  2. 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
  3. 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
  4. 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
  5. 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
  6. 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
  7. 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
  8. MZ1
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    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
  9. 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
  10. 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
  11. 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
  12. 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
  13. 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
  14. 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
  15. 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
  16. 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
  17. 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
  18. 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
  19. 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
  20. 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
  21. 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
  22. 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
  23. 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
  24. 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
  25. GNE-049
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    GNE-049

    Catalog No. A20206
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    CBP inhibitor
    GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively. 了解更多
  26. SF1126
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    SF1126

    Catalog No. A12704
    Pan PI3K 抑制剂
    SF1126是一种水溶性小分子前药，包含泛PI3K/mTOR抑制剂LY294002/SF1101与含RGD的四肽SF1174共轭，具有潜在的抗肿瘤和抗血管生成活性。 了解更多
  27. C646
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    C646

    Catalog No. A12815
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    p300/CBP 抑制剂
    C646是选择性的p300/CREB结合蛋白（CBP）抑制剂（Ki = 400 nM）。 了解更多
  28. BRD-IN-3
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    BRD-IN-3

    Catalog No. A18454
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    BRD inhibitor
    BRD-IN-3 ((R,R)-36n) is a highly potent PCAF bromodomain (BRD) inhibitor, with an IC50 of 7 nM. BRD-IN-3 also exhibits activity against GCN5 and FALZ. 了解更多
  29. 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
  30. 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
  31. P300/CBP-IN-3
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    P300/CBP-IN-3

    Catalog No. A18544
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    p300/CBP histone acetyltransferase inhibitor
    P300/CBP-IN-3, a p300/CBP histone acetyltransferase inhibitor. 了解更多
  32. ZEN-3219
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    ZEN-3219

    Catalog No. A19367
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    BET inhibitor
    ZEN-3219 is a BET inhibitor with IC50s of 0.48, 0.16 and 0.47 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3219 can be used to form PROTACs to induce degradation of BRD4. 了解更多
  33. A1874
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    A1874

    Catalog No. A18735
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    BRD4-degrading PROTAC
    A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation. 了解更多
  34. 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
  35. GSK2801
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    GSK2801

    Catalog No. A14015
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    BAZ2A and BAZ2B 抑制剂
    GSK2801是BAZ2家族含溴结构域蛋白的强效抑制剂。 了解更多
  36. 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
  37. (-)-JQ1
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    (-)-JQ1

    Catalog No. A14160
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    BET bromodomain 抑制剂
    (-)-JQ1蛋白家族蛋白质的溴结构域和额外末端结构域（BET）家族，包括BRD2，BRD3和BRD4，在许多细胞过程中起着关键作用，包括炎症基因表达，有丝分裂和病毒/宿主相互作用，这是通过控制组蛋白乙酰化的过程来实现的。依赖的染色质复合物。 了解更多
  38. GSK1324726A (I-BET726)
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    GSK1324726A (I-BET726)

    Catalog No. A14133
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    BET 抑制剂
    GSK1324726A (I-BET726)是一种新型、高效、选择性的BET蛋白小分子抑制剂，对BRD2（IC50 = 41 nM）、BRD3（IC50 = 31 nM）和BRD4（IC50 = 22 nM）具有高度的亲和力。 了解更多
  39. GSK 525768A
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    GSK 525768A

    Catalog No. A14134
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    GSK 525768A是GSK 525762A的对映体化合物，GSK 525762A是一种有效的小分子抑制剂，可破坏溴多糖BET家族（Brd2、Brd3和Brd4）的功能；GSK 525768A对BET没有活性。 了解更多
  40. Anacardic Acid
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    Anacardic Acid

    Catalog No. A14226
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    KAT5 (Tip60), p300/PCAF 抑制剂
    Anacardic Acid是p300和p300/CBP相关因子组蛋白乙酰转移酶的有效抑制剂。 了解更多
  41. PFI-3
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    PFI-3

    Catalog No. A13957
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    SMARCA bromodomains probe
    PFI-3是SMARCA溴结构域的选择性化学探针。 了解更多
  42. Apabetalone (RVX-208)
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    Apabetalone (RVX-208)

    Catalog No. A13956
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    BET bromodomain 抑制剂
    RVX-208是一种有效的BET溴结构域抑制剂，对BD2的IC50为0.510 uM，是BD1选择性的170倍。 了解更多
  43. 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
  44. 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
  45. 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
  46. MZP-55
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    MZP-55

    Catalog No. A19415
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    BRD3/4 degrader
    MZP-55 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 8 nM for Brd4BD2. 了解更多
  47. MZP-54
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    MZP-54

    Catalog No. A19426
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    BRD3/4 degrader
    MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 4 nM for Brd4BD2. 了解更多
  48. MS417
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    MS417

    Catalog No. A19433
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    BRD4 inhibitor
    MS417 is a BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC50, 32.7 μM). 了解更多
  49. dBET57
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    dBET57

    Catalog No. A19133
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    BRD4BD1degrader
    dBET57 is a potent and selective degrader of BRD4BD1 based on the PROTAC technology. 了解更多
  50. CD235
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    CD235

    Catalog No. A19115
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    BET bromodomain inhibitor
    CD235 is a structurally similar analogue of CD161. CD161 is a potent and orally bioavailable BET bromodomain inhibitor. 了解更多

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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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