dBRD9
Based on 1 publication(s) in Google Scholar
dBRD9 is a BRD9 PROTAC degrader. dBRD9 reduces the binding of the ISGF3 complex to ISG promoters, decreases the level of ISG induction downstream of IFNAR signaling, and reduces the chromatin binding of BRD4 at BRD9 co-binding sites. dBRD9 can be used in research related to acute myeloid leukemia.
(Pink: BRD9 ligand (HY-100351); Blue: Cereblon ligand (HY-14658); Black: linker (HY-128833)).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.75%
- CAS. Nr.: 2170679-45-3
- Formel: C40H45N7O10
- Molecular Weight:783.83
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) dBRD9
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Biologische Aktivität
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BRD9 |
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Cell Line
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Type | Value | Description | References |
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| A204 | IC50 |
0.0898 μM
Compound: 21;dBRD9
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Antiproliferative activity against human A204 cells assessed as inhibition of cell growth incubated for 7 days by CellTiterGlo assay
Antiproliferative activity against human A204 cells assessed as inhibition of cell growth incubated for 7 days by CellTiterGlo assay
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[PMID: 30540463] |
dBRD9 (0.5-5000 nM; 4 h) induces dose-dependent degradation of BRD9 in MOLM-13 cells, with no off-target degradation of BRD4 or BRD7 detected[1].
dBRD9 (7 days potently inhibits the proliferation of EOL-1 and MOLM-13 acute myeloid leukemia (AML) cells, with an efficacy 10 to 100 times higher than that of non-degradable BRD9 probes[1].
dBRD9 (3 μM; 24 h) selectively reduces the induction of IFNAR-dependent secondary response genes (including interferon-stimulated genes) in Lipid A-stimulated mouse bone marrow-derived macrophages, without affecting primary response genes or IFN-β production[2].
dBRD9 (3 μM; 24 h) induces widespread loss of BRD9 chromatin binding as well as partial loss of BRD4 binding in Lipid A-stimulated mouse bone marrow-derived macrophages, which correlates with reduced ISGF3 complex binding and downregulation of interferon-stimulated genes[2].
dBRD9 (3 μM; 24 h) does not impair the induction of IRF9 and STAT2 proteins in Lipid A-stimulated mouse bone marrow-derived macrophages[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human acute myeloid leukemia (MOLM-13) cells
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Concentration:0.5, 5, 50, 500 and 5000 nM
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Incubation Time:4 h
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Result:Observed marked dose-dependent BRD9 loss across the tested concentrations.
Detected no off-target degradation of BRD4 or BRD7 at any tested concentration, unlike a comparator degrader.
Chemical Information
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CAS. Nr. 2170679-45-3
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Appearance Solid
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Molecular Weight 783.83
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Formel C40H45N7O10
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Color Light yellow to yellow
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SMILES
O=C(NCCOCCOCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CN(CC4=C(OC)C=C(C(C5=CC=NC=C65)=CN(C)C6=O)C=C4OC)C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
ARID1A loss drives gastric signet ring cell carcinoma by regulating mucin production and secretion. [Abstract]2026 Jun 2. PMID: 42230634
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (127.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Remillard D, et al. Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands. Angewandte Chemie (International ed. in English). 2017 May 15;56(21):5738-5743. [Content Brief]
[2]. Ahmed NS, et al. BRD9 regulates interferon-stimulated genes during macrophage activation via cooperation with BET protein BRD4. Proceedings of the National Academy of Sciences of the United States of America. 2022 Jan 04;119(1):e2110812119. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.2758 mL | 6.3789 mL | 12.7579 mL | 31.8947 mL |
| 5 mM | 0.2552 mL | 1.2758 mL | 2.5516 mL | 6.3789 mL | |
| 10 mM | 0.1276 mL | 0.6379 mL | 1.2758 mL | 3.1895 mL | |
| 15 mM | 0.0851 mL | 0.4253 mL | 0.8505 mL | 2.1263 mL | |
| 20 mM | 0.0638 mL | 0.3189 mL | 0.6379 mL | 1.5947 mL | |
| 25 mM | 0.0510 mL | 0.2552 mL | 0.5103 mL | 1.2758 mL | |
| 30 mM | 0.0425 mL | 0.2126 mL | 0.4253 mL | 1.0632 mL | |
| 40 mM | 0.0319 mL | 0.1595 mL | 0.3189 mL | 0.7974 mL | |
| 50 mM | 0.0255 mL | 0.1276 mL | 0.2552 mL | 0.6379 mL | |
| 60 mM | 0.0213 mL | 0.1063 mL | 0.2126 mL | 0.5316 mL | |
| 80 mM | 0.0159 mL | 0.0797 mL | 0.1595 mL | 0.3987 mL | |
| 100 mM | 0.0128 mL | 0.0638 mL | 0.1276 mL | 0.3189 mL |
dBRD9 Related Classifications
HY-117690 Related Classifications
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