dBRD9
- Product Name
- dBRD9
- CAS No.
- 2170679-45-3
- Chemical Name
- dBRD9
- Synonyms
- dBRD9;DBRD09;dBRD-9|||dBRD 9;dBRD9, 10 mM in DMSO;2-[[2,6-dimethoxy-4-(2-methyl-1-oxo-2,7-naphthyridin-4-yl)phenyl]methyl-methylamino]-N-[2-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]ethoxy]ethyl]acetamide;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;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;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]-
- CBNumber
- CB74667813
- Molecular Formula
- C40H45N7O10
- Formula Weight
- 783.84
- MOL File
- 2170679-45-3.mol
dBRD9 Property
- 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 Chemical Properties,Usage,Production
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
Raw materials
Preparation Products
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View Lastest Price from dBRD9 manufacturers
- Product
- dBRD9 2170679-45-3
- Price
- US $0.00-0.00/MG
- Min. Order
- 1MG
- Purity
- 98
- Supply Ability
- 100G
- Release date
- 2024-04-17