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Submit ReviewBI 9564
说明： Potent and selective BRD9 and BRD7 inhibitor; orally active
化学名： 4-[4-[(Dimethylamino)methyl]-2,5-dimethoxyphenyl]-2-methyl-1,2-dihydro-2,7-naphthyridin-1-one
纯度： ≥98% (HPLC)
生物活性 for BI 9564
BI 9564 is a potent and selective BRD9 and BRD7 inhibitor (Kd values are 14 and 239 nM, respectively). Exhibits selectivity for BRD9/7 over 48 other bromodomains, 324 kinases and 55 GPCRs. Inhibits proliferation of AML cell lines in vitro and reduces AML tumor xenograft growth in vivo. Cell permeable and orally active.
许可信息
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the BI 9564 probe summary on the SGC website.
External Portal Information for BI 9564
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of BI-9564 is reviewed on the chemical probes website.
化合物库 for BI 9564
BI 9564 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
技术数据 for BI 9564
| 分子量 | 353.41 |
| 公式 | C20H23N3O3 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1883429-22-8 |
| PubChem ID | 117072549 |
| InChI Key | BJFSUDWKXGMUKA-UHFFFAOYSA-N |
| Smiles | O=C(N(C)C=C1C2=CC(OC)=C(CN(C)C)C=C2OC)C3=C1C=CN=C3 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for BI 9564
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 7.07 | 20 | |
| 1eq. HCl | 3.53 | 10 温和加热 |
制备储备液 for BI 9564
以下数据基于产品分子量 353.41。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 14.15 mL | 70.74 mL | 141.48 mL |
| 1 mM | 2.83 mL | 14.15 mL | 28.3 mL |
| 2 mM | 1.41 mL | 7.07 mL | 14.15 mL |
| 10 mM | 0.28 mL | 1.41 mL | 2.83 mL |
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产品说明书 for BI 9564
参考文献 for BI 9564
参考文献是支持产品生物活性的出版物。
Martin et al (2016) Structure-based design of an in vivo active selective BRD9 inhibitor J.Med.Chem. 59 4462 PMID: 26914985
Karim and Schönbrunn (2016) An Advanced Tool To Interrogate BRD9. J.Med.Chem. 59 4459 PMID: 27120693
If you know of a relevant reference for BI 9564, please let us know.
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关键词: BI 9564, BI 9564 supplier, BI9564, BRD9, BRD7, potent, selective, inhibitors, inhibits, bromodomains, orally, active, Bromodomains, 5590, Tocris Bioscience
1 篇 BI 9564 的引用文献
引用文献是使用了 Tocris 产品的出版物。 BI 9564 的部分引用包括：
Nasun et al (2022) BRD9 regulates interferon-stimulated genes during macrophage activation via cooperation with BET protein BRD4. Proc Natl Acad Sci U S A 119 PMID: 34983841
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
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Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.