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Submit ReviewdBRD9 is a potent and selective Degrader (PROTAC®) of BRD9 (IC50 = 56.6 nM in MOLM-13 cells). dBRD9 is composed of the BRD9 inhibitor BI 7273 conjugated to the cereblon E3 ligase ligand pomalidomide (Cat. No. 6302). Does not degrade BRD4 or BRD7 at concentrations up to 5 μM. Displays antiproliferative effects in human AML cell lines. BRD9 antibody validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # NBP3-14730.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Sold under license from Dana-Farber Cancer Institute.
分子量 | 856.75 |
公式 | C40H45N7O10.2HCl |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 2341840-98-8 |
PubChem ID | 135397681 |
InChI Key | AIOCFZJGGGEWDK-UHFFFAOYSA-N |
Smiles | COC1=CC(C2=CN(C(C3=CN=CC=C23)=O)C)=CC(OC)=C1CN(CC(NCCOCCOCCNC4=C5C(N(C(C5=CC=C4)=O)C6CCC(NC6=O)=O)=O)=O)C.Cl.Cl |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 17.14 | 20 | |
DMSO | 42.84 | 50 |
以下数据基于产品分子量 856.75。 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 |
---|---|---|---|
0.5 mM | 2.33 mL | 11.67 mL | 23.34 mL |
2.5 mM | 0.47 mL | 2.33 mL | 4.67 mL |
5 mM | 0.23 mL | 1.17 mL | 2.33 mL |
25 mM | 0.05 mL | 0.23 mL | 0.47 mL |
参考文献是支持产品生物活性的出版物。
Remillard et al (2017) Degradation of the BAF complex factor BRD9 by heterobifunctional ligands. Angew.Chem.Int.Ed.Engl. 56 5738 PMID: 28418626
If you know of a relevant reference for dBRD9, please let us know.
关键词: dBRD9, dBRD9 supplier, 2170679-45-3, BRD9, degrading, active, degraders, PROTAC, PROTACs, Proteolysis, Targeting, Chimeras, targeted, protein, degradation, tpd, BAF, complex, factor, bromodomains, cereblon, e3, ligase, potent, selective, Bromodomains, Bromodomain, (BRD), Degraders, 6606, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 dBRD9 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
Ma et al (2023) Engineered PROTAC-CID systems for mammalian inducible gene regulation J Am Chem Soc 145 1593 PMID: 3662658
Loo et al (2020) A Genome-wide CRISPR Screen Reveals a Role for the Non-canonical Nucleosome-Remodeling BAF Complex in Foxp3 Expression and Regulatory T Cell Function Immunity 53 143 PMID: 32640256
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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。
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia