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Epigenetic Reader Domain

Epigenetic Reader Domain

Inhibitory Selectivity

Catalog No.	Inhibitor Name	Epigenetic Reader Domain
A12729	(*)-JQ1	***
A11783	I-BET151	*
A12545	PFI-1	**
A11440	I-BET-762	***
A13956	RVX-208	*
A13227	SGC-CBP30	****
A13163	Bromosporine	****
A13890	OTX015	****
A12948	UNC1215	**
A13717	UNC669	*
A14133	GSK1324726A	***
A13749	MS436	**
A13068	CPI-203	***
A13957	PFI-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.

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AZD5153 6-Hydroxy-2-naphthoic acid

Catalog No. A21852
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BET/BRD4 bromodomain inhibitor

AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM. 了解更多

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Molibresib besylate

Catalog No. A21855
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BET bromodomain inhibitor

Molibresib besylate (GSK 525762C; I-BET 762 besylate) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM. 了解更多

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GSK 1210151A (I-BET151)

Catalog No. A11783
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BET Bromodomain 抑制剂

GSK 1210151A (I-BET151)是溴结构域和额外末端（BET）家族蛋白BRD2，BRD3和BRD4的新型选择性抑制剂。了解更多

Product Citations (1)

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- Momeny M, .et al. Inhibition of bromodomain and extraterminal domain reduces growth and invasive characteristics of chemoresistant ovarian carcinoma cells, Anticancer Drugs, 2018, Nov;29(10):1011-1020 PMID: 30096128
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PFI-1

Catalog No. A12545
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BET 抑制剂

PFI-1是BET溴结构域抑制剂，对BRD2和BRD4表现出抑制活性。了解更多

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GSK 525762A (I-BET-762)

Catalog No. A11440
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BET 抑制剂

GSK 525762A (I-BET-762)是BET(溴域和末端外)家族的小分子抑制剂。了解更多

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CPI-203

Catalog No. A13068
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BET bromodomain 抑制剂

CPI203是溴结构域和额外末端（BET）家族蛋白BRD4的新型有效，选择性和细胞渗透性抑制剂，IC50为?37 nM（BRD4α筛选试验）。了解更多

Product Citations (1)

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- Derenzini E, .et al. BET Inhibition-Induced GSK3β Feedback Enhances Lymphoma Vulnerability to PI3K Inhibitors, Cell Rep, 2018, Aug 21;24(8):2155-2166 PMID: 30134175
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Bromosporine

Catalog No. A13163
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bromodomain 抑制剂

Bromosporine是一种针对溴结构域的广谱抑制剂，对于BRD2，BRD4，BRD9和CECR2的IC50分别为0.41μM，0.29μM，0.122μM和0.017μM。了解更多

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UNC 669

Catalog No. A13717
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L3MBTL 抑制剂

UNC669是L3MBTL1和L3MBTL3的抑制剂,对L3MBTL1和L3MBTL3具有选择性（IC50分别为4.2μM和3.1μM）。了解更多

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(+)-JQ1

Catalog No. A12729
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BET 抑制剂

(+)-JQ1是有效的，高亲和力的选择性BET溴结构域抑制剂。了解更多

Product Citations (8)

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- Gerald Thiel, .et al. TRPM3-Induced Gene Transcription Is under Epigenetic Control, Pharmaceuticals (Basel), 2022, Jul 10;15(7):846 PMID: 35890145
- Selase D Deletsu, .et al. Identification and characterization of Stathmin 1 as a host factor involved in HIV-1 latency, Biochem Biophys Res Commun, 2021, Aug 27;567:106-111 PMID: 34146904
- Cole Schonhofer, .et al. Flavonoid-based inhibition of cyclin-dependent kinase 9 without concomitant inhibition of histone deacetylases durably reinforces HIV latency, Biochem Pharmacol, 2021, Apr;186:114462 PMID: 33577894
- Nandini Verma, .et al. Synthetic lethal combination targeting BET uncovered intrinsic susceptibility of TNBC to ferroptosis, Sci Adv, 2020, 6 : eaba8968
- Kuo MT, .et al. Collaboration Between RSK-EphA2 and Gas6-Axl RTK Signaling in Arginine Starvation Response That Confers Resistance to EGFR Inhibitors, Transl Oncol, 2020, 13(2):355-364 PMID: 31887630
- Rao Z, .et al. Vacuolar (H+)-ATPase Critically Regulates Specialized Proresolving Mediator Pathways in Human M2-like Monocyte-Derived Macrophages and Has a Crucial Role in Resolution of Inflammation, J Immunol, 2019, Aug 15;203(4):1031-1043 PMID: 31300512
- A Carrer, .et al. Acetyl-CoA metabolism supports multi-step pancreatic tumorigenesis, Cancer Discov, 2019, Jan 9. pii: CD-18-0567 PMID: 30626590
- Clocchiatti A, .et al. Androgen receptor functions as transcriptional repressor of cancer-associated fibroblast activation, J Clin Invest, 2018, Dec 3;128(12):5531-5548 PMID: 30395538
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SGC-CBP30

Catalog No. A13227
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CBP/p300 bromodomain 抑制剂

SGC-CBP30是一种有效且选择性的CREBBP（CBP）和EP300抑制剂，无细胞试验中IC50分别为21 nM和38 nM。它们是一般的转录共激活因子。了解更多

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OTX015

Catalog No. A13890
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BET 抑制剂

OTX015是口服可生物利用的BRD2，BRD3和BRD4的小分子抑制剂（EC50s = 10-19 nM）。了解更多

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UNC1215

Catalog No. A12948
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L3MBTL3 抑制剂

UNC1215是具有细胞活性的L3MBTL3的强效选择性拮抗剂。了解更多

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I-CBP112

Catalog No. A13165
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CBP/p300 bromodomain 抑制剂

I-CBP112是一种高效且选择性的p300/CBP溴结构域抑制剂（对于CBP，IC50为?0.14-0.17 uM，对于p300为?0.625 uM）。了解更多

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MS436

Catalog No. A13749
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BRD4 抑制剂

MS436是用于BRD4溴结构域的重氮基小分子抑制剂，Ki值为30-50 nM。了解更多

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I-BRD9

Catalog No. A15872
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Selective BRD9 抑制剂

I-BRD9是一种有效的选择性BRD9抑制剂，pIC50为7.3，而对BRD4的pIC50为5.3。了解更多

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BI-7273

Catalog No. A16068
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BRD9 BD 抑制剂

BI-7273是一种选择性的，细胞可渗透的BRD9 BD抑制剂。了解更多

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BI-9564

Catalog No. A16196
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BRD7/9 抑制剂

BI-9564是BRD9和BRD7溴结构域的有效和选择性抑制剂（Kds分别为14.1和239 nM；IC50分别为75 nM和3.4 uM）。了解更多

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(E)-ZL0420

Catalog No. A20136
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BRD4 inhibitor

ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2. 了解更多

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ZL0454

Catalog No. A20123
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BRD4 inhibitor

ZL0454 is a potent and selective Bromodomain-containing protein 4 (BRD4) inhibitor with an IC50 of 49 and 32 nM for BD1 and BD2. 了解更多

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BMS-986158

Catalog No. A19442
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Bromodomain inhibitor

BMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) proteins. 了解更多

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