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说明： Potent and selective BRD9 inhibitor
化学名： 5-Ethyl-4,5-dihydro-4-oxo-N-(tetrahydro-1,1-dioxido-2H-thiopyran-4-yl)-7-[3-(trifluoromethyl)phenyl]thieno[3,2-c]pyridine-2-carboximidamide
纯度： ≥98% (HPLC)
生物活性 for I-BRD9
I-BRD9 is a potent and selective BRD9 inhibitor (pIC50 = 7.3). Exhibits >70-fold selectivity for BRD9 over a panel of 34 other bromodomains and >700-fold selectivity over the BET family. Downregulates CLEC1, DUSP6, FES and SAMSN1 genes in Kasumi-1 cells.
许可信息
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the I-BRD9 probe summary on the SGC website.
External Portal Information for I-BRD9
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of I-BRD9 is reviewed on the chemical probes website.
化合物库 for I-BRD9
I-BRD9 is also offered as part of the Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
技术数据 for I-BRD9
| 分子量 | 497.55 |
| 公式 | C22H22F3N3O3S2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1714146-59-4 |
| PubChem ID | 91668541 |
| InChI Key | WRUWGLUCNBMGPS-UHFFFAOYSA-N |
| Smiles | O=C1C2=C(SC(C(NC3CCS(CC3)(=O)=O)=N)=C2)C(C4=CC=CC(C(F)(F)F)=C4)=CN1CC |
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 I-BRD9
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 49.76 | 100 |
制备储备液 for I-BRD9
以下数据基于产品分子量 497.55。 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 |
|---|---|---|---|
| 1 mM | 2.01 mL | 10.05 mL | 20.1 mL |
| 5 mM | 0.4 mL | 2.01 mL | 4.02 mL |
| 10 mM | 0.2 mL | 1 mL | 2.01 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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产品说明书 for I-BRD9
参考文献 for I-BRD9
参考文献是支持产品生物活性的出版物。
Theodoulou et al (2015) Discovery of I-BRD9, a selective cell active chemical probe for bromodomain containing protein 9 inhibition. J.Med.Chem 59 1425 PMID: 25856009
If you know of a relevant reference for I-BRD9, please let us know.
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关键词: I-BRD9, I-BRD9 supplier, bromodomains, containing, protein, extra, terminal, inhibits, inhibitors, potent, selective, downregulates, downregulation, sgc, structural, genomics, consortium, Bromodomains, 5591, Tocris Bioscience
5 篇 I-BRD9 的引用文献
引用文献是使用了 Tocris 产品的出版物。 I-BRD9 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
Yong et al (2020) The bromodomain containing protein BRD-9 orchestrates RAD51-RAD54 complex formation and regulates homologous recombination-mediated repair. Nat Commun 11 2639 PMID: 32457312
Yili et al (2023) BRD9-mediated chromatin remodeling suppresses osteoclastogenesis through negative feedback mechanism. Nat Commun 14 1413 PMID: 36918560
Wei et al (2018) Vitamin D switches BAF complexes to protect β cells. Cell 173 1135 PMID: 29754817
Brien et al (2018) Targeted degradation of BRD9 reverses oncogenic gene expression in synovial sarcoma. Elife 7 e41305 PMID: 30431433
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I-BRD9 的评论
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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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