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Description: Potent and selective BRD9 Degrader (PROTAC®)
Chemical Name: 2-[[[4-(1,2-Dihydro-2-methyl-1-oxo-2,7-naphthyridin-4-yl)-2-6-dimethoxyphenyl]methyl]methylamino]-N-[2-[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]ethoxy]ethyl]acetamide dihydrochloride
Purity: ≥98% (HPLC)
Biological Activity for dBRD9
dBRD9 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.
Licensing Information
Sold under license from Dana-Farber Cancer Institute.
Technical Data for dBRD9
| M. Wt | 856.75 |
| Formula | C40H45N7O10.2HCl |
| Storage | Store at -20°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for dBRD9
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 17.14 | 20 | |
| DMSO | 42.84 | 50 |
Preparing Stock Solutions for dBRD9
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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 |
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Product Datasheets for dBRD9
References for dBRD9
References are publications that support the biological activity of the product.
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.
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Keywords: 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
3 Citations for dBRD9
Citations are publications that use Tocris products. Selected citations for dBRD9 include:
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
Do you know of a great paper that uses dBRD9 from Tocris? Please let us know.
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Literature in this Area
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TPD and Induced Proximity Research Product Guide
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
- Active Degraders
- TAG Degradation Platform
- Degrader Building Blocks
- Assays for Protein Degradation
- Induced Proximity Tools
Targeted Protein Degradation Poster
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