2. PROTAC Epigenetics Apoptosis
  3. PROTACs Epigenetic Reader Domain Apoptosis
  4. dBRD 9-A

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).

For research use only. We do not sell to patients.

dBRD 9-A

dBRD 9-A Chemical Structure

CAS No. : 2170679-42-0

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

dBRD 9-A Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

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

 

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.

dBRD 9-A Related Antibodies

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 (Foxn1nu) (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.
Molecular Weight

779.88

Formula

C42H49N7O8
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2822 mL 6.4112 mL 12.8225 mL
5 mM 0.2564 mL 1.2822 mL 2.5645 mL
View the 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.

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Purity & Documentation

Purity: 99.50%

SDS (252 KB)

COA (244 KB)

Handling Instructions (2659 KB)
References

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 1.2822 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 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

dBRD 9-A2170679-42-0PROTACsEpigenetic Reader DomainApoptosisGLTSCR1/1LGBAF complexBRD9super enhancersynovial sarcoma cellsBRD9 bromodomainSYO1SS18-SSXHSSYIICRBNInhibitorinhibitorinhibit

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