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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.
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, Active, Degraders, Bromodomains, 6606, Tocris Bioscience
3 Citations for dBRD9
Citations are publications that use Tocris products. Selected citations for dBRD9 include:
Ma et al (2023) Engineered PROTAC-CID systems for mammalian inducible gene regulation J Am Chem Soc 145 1593 PMID: 3662658
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
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
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Targeted Protein Degradation Research Product GuideUpdated
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Epigenetics Scientific Review
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.
Epigenetics in Cancer Poster
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
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