Art. -Nr.: HY-148739

dBRD 9-A

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dBRD 9-A is a selective BRD9 PROTAC degrader. dBRD 9-A induces near complete BRD9 degradation dependent on E3 ubiquitin ligase CRBN and BRD9 bromodomain engagement, and drives loss of BRD9 chromatin binding genome-wide. dBRD 9-A downregulates oncogenic SS18-SSX-driven transcriptional programs, super enhancer-associated gene expression, and SS18-SSX1 super enhancer binding, and depletes GBAF complex members GLTSCR1/1L from SS18-SSX complexes. dBRD 9-A induces cell cycle arrest and increases apoptosis in synovial sarcoma cells. dBRD 9-A can be used for the research of synovial sarcoma.
(Pink: BRD9 ligand (HY-107446); Blue: Cereblon ligand (HY-14658); Black: linker).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.07%
CAS. Nr.: 2170679-42-0
Formel: C₄₂H₄₉N₇O₈
Molecular Weight:779.88

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

dBRD 9-A Chemical Structure

CAS. Nr.: 2170679-42-0

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

dBRD 9-A is a selective BRD9 PROTAC degrader. dBRD 9-A induces near complete BRD9 degradation dependent on E3 ubiquitin ligase CRBN and BRD9 bromodomain engagement, and drives loss of BRD9 chromatin binding genome-wide. dBRD 9-A downregulates oncogenic SS18-SSX-driven transcriptional programs, super enhancer-associated gene expression, and SS18-SSX1 super enhancer binding, and depletes GBAF complex members GLTSCR1/1L from SS18-SSX complexes. dBRD 9-A induces cell cycle arrest and increases apoptosis in synovial sarcoma cells. dBRD 9-A can be used for the research of synovial sarcoma^[1]. (Pink: BRD9 ligand (HY-107446); Blue: Cereblon ligand (HY-14658); Black: linker).

IC₅₀ & Target^[1]

BRD9

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen :

In Vitro

dBRD9-A (100 nM; 6-72 h) induces near complete degradation of BRD9 in HSSYII and SYO1 synovial sarcoma cells^[1].
dBRD9-A (100 nM; 24 h) leads to a near-complete loss of BRD9 chromatin binding genome-wide in HSSYII synovial sarcoma cells^[1].
dBRD9-A (100 nM; 3-9 days) induces a progressive cell cycle arrest characterized by accumulation of G1/G0 phase cells and reduction of S phase cells in HSSYII and SYO1 synovial sarcoma cells^[1].
dBRD9-A (100 nM; 3-9 days) induces a progressive increase in apoptotic cells in HSSYII and SYO1 synovial sarcoma cells^[1].
dBRD9-A (100 nM; 6 h) primarily induces downregulation of gene expression, with preferential downregulation of genes associated with super enhancers in HSSYII synovial sarcoma cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

HSSYII, SYO1
Concentration:

100 nM
Incubation Time:

6 h, 12 h, 24 h, 48 h, 72 h
Result:

Elicited near complete BRD9 degradation across all tested time points in both HSSYII and SYO1 cell lines.

Cell Cycle Analysis^[1]

Cell Line:

HSSYII, SYO1
Concentration:

100 nM
Incubation Time:

3 days,6 days,9 days
Result:

Induced a progressive cell cycle arrest, with increases in G1/G0 phase cells and decreases in S phase cells over time in both cell lines.

Apoptosis Analysis^[1]

Cell Line:

HSSYII, SYO1
Concentration:

100 nM
Incubation Time:

3 days,6 days,9 days
Result:

Resulted in a progressive increase in Annexin-V positive (apoptotic) cells over time in both cell lines.

In Vivo

dBRD9-A (50 mg/kg; i.p.; once daily; 24 days) significantly inhibits synovial sarcoma tumor progression in a xenograft mouse model, with complete BRD9 degradation in tumor tissue and no overt toxicity^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c (Foxn1^nu) (female, 4-6 weeks old, subcutaneous xenograft model) injected with synovial sarcoma cells^[1]
Dosage:

50 mg/kg
Administration:

i.p.; once daily; 24 days
Result:

Inhibited tumor progression over 24 days, with a significant difference in tumor volume compared to vehicle control.
Confirmed near-complete degradation of BRD9 in tumor tissue via western blotting.
Retained normal body weight and blood counts, with no overt treatment-related side effects.

Chemical Information

CAS. Nr. 2170679-42-0
Appearance Solid
Molecular Weight 779.88
Formel C₄₂H₄₉N₇O₈
Color Light yellow to yellow
SMILES

O=C1C2=C(C(C3=CC(OC)=C(CN(CC(NCCCCCCCCNC4=CC=CC(C(N5C6C(NC(CC6)=O)=O)=O)=C4C5=O)=O)C)C(OC)=C3)=CN1C)C=CN=C2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (128.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.2822 mL

6.4112 mL

12.8225 mL

5 mM

0.2564 mL

1.2822 mL

2.5645 mL

10 mM

0.1282 mL

0.6411 mL

1.2822 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Brien GL, et al. Targeted degradation of BRD9 reverses oncogenic gene expression in synovial sarcoma. Elife. 2018;7:e41305. Published 2018 Nov 15. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	1.2822 mL	6.4112 mL	12.8225 mL	32.0562 mL
	5 mM	0.2564 mL	1.2822 mL	2.5645 mL	6.4112 mL
	10 mM	0.1282 mL	0.6411 mL	1.2822 mL	3.2056 mL
	15 mM	0.0855 mL	0.4274 mL	0.8548 mL	2.1371 mL
	20 mM	0.0641 mL	0.3206 mL	0.6411 mL	1.6028 mL
	25 mM	0.0513 mL	0.2564 mL	0.5129 mL	1.2822 mL
	30 mM	0.0427 mL	0.2137 mL	0.4274 mL	1.0685 mL
	40 mM	0.0321 mL	0.1603 mL	0.3206 mL	0.8014 mL
	50 mM	0.0256 mL	0.1282 mL	0.2564 mL	0.6411 mL
	60 mM	0.0214 mL	0.1069 mL	0.2137 mL	0.5343 mL
	80 mM	0.0160 mL	0.0801 mL	0.1603 mL	0.4007 mL
	100 mM	0.0128 mL	0.0641 mL	0.1282 mL	0.3206 mL

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dBRD 9-A

Apoptosis Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

PROTAC Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

dBRD 9-A

Apoptosis Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

PROTAC Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

dBRD 9-A Related Classifications

HY-148739 Related Classifications