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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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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

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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

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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

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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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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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