dBRD9 manufacturers
- dBRD9
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- $0.00 / 100MG
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2025-03-16
- CAS:2170679-45-3
- Min. Order: 1MG
- Purity: 98
- Supply Ability: 100G
- dBRD9
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- $131.00 / 1mg
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2024-11-15
- CAS:2170679-45-3
- Min. Order:
- Purity: 99.81%
- Supply Ability: 10g
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| Product Name: | dBRD9 | | Synonyms: | dBRD9;2-((2,6-Dimethoxy-4-(2-methyl-1-oxo-1,2-dihydro-2,7-naphthyridin-4-yl)benzyl)(methyl)amino)-N-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)ethoxy)ethyl)acetamide;Acetamide, 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]-;DBRD09;dBRD-9|||dBRD 9;2-({[2,6-dimethoxy-4-(2-methyl-1-oxo-1,2-dihydro-2,7-naphthyridin-4-yl)phenyl]methyl}(methyl)amino)-N-{2-[2-(2-{[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]amino}ethoxy)ethoxy]ethyl}acetamide;dBRD9, 10 mM in DMSO | | CAS: | 2170679-45-3 | | MF: | C40H45N7O10 | | MW: | 783.84 | | EINECS: | | | Product Categories: | | | Mol File: | 2170679-45-3.mol |  |
| | dBRD9 Chemical Properties |
| Boiling point | 1014.2±65.0 °C(Predicted) | | density | 1.357±0.06 g/cm3(Predicted) | | pka | 10.74±0.40(Predicted) | | form | Solid | | color | Light yellow to yellow | | InChIKey | AIOCFZJGGGEWDK-UHFFFAOYSA-N | | SMILES | O=C1N(C2CCC(=O)NC2=O)C(=O)C2=CC=CC(NCCOCCOCCNC(=O)CN(C)CC3C(=CC(C4=CN(C)C(=O)C5=CN=CC=C45)=CC=3OC)OC)=C12 |
| | dBRD9 Usage And Synthesis |
| Description | 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. Does not degrade BRD4 or BRD7 at concentrations up to 5 μM. Displays antiproliferative effects in human AML cell lines.
| | Uses | dBRD9,a PROTAC, can selective degrades BRD9. dBRD9 improves the bromine domain binding profile and reduces the binding activity of the whole BET family[1]. | | Biological Activity | dBRD9 is a PEG-linked pomalidomide conjugate and was found to prompt rapid BRD9 degradation over a broad range of concentrations. Besides, also shows an improved bromodomain engagement profile, with reduced binding activity across the BET family. Meanwhile, dBRD9 (0.5, 5, 50, 500, 5000 nM; 4 h) decreases the expression of BRD9 protein in MOLM-13 cells in a dose-dependent manner. However, it shows no significant effect on the expression of BRD4 and BRD7 proteins. Moreover, dBRD9 (100 nM; 2 h) shows selectivity for BRD9 degradation with a 5.5 median fold lower abundance in dBRD9 treated samples in MOLM-13 cells. However, the levels of other proteins were remarkably static between treatments, with 99% of proteins differing less than 0.30 fold. In addition, dBRD9 (0-100; 7 days) shows a potent anti-proliferative effect in EOL-1 and MOML-13 cells in a dose-dependent manner. All in all, dBRD9 is a PROTAC and can selectively degrade BRD9. | | IC 50 | BRD9 | | References | [1] Remillard D, et al. Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands. Angew Chem Int Ed Engl. 2017 May 15;56(21):5738-5743. DOI:10.1002/anie.201611281 |
| | dBRD9 Preparation Products And Raw materials |
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