GBD-9
Based on 1 Customer Validation
GBD-9 is a degrader based on the E3 ubiquitin ligase CRBN that targets BTK and the G1 to S phase transition protein GSPT1. GBD-9 has both PROTAC and molecular glue properties by inducing ubiquitination and proteasomal degradation of target proteins. GBD-9 can efficiently degrade wild-type and mutant BTK (such as C481S mutation) and GSPT1. GBD-9 significantly inhibits tumor cell proliferation by inducing G1 phase arrest in cancer cells, downregulating anti-apoptotic proteins (BCL-2, MCL-1) and activating Caspase-3 to induce apoptosis. GBD-9 is mainly used in the research of hematological tumors such as diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML).
(Pink: Btk ligand (HY-13036A); Blue: Cereblon ligand (HY-W023573); Black: linker (HY-N7057)).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.91%
- No. CAS: 2864408-92-2
- Fòrmula: C44H47N9O6
- Peso molecular:797.90
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Almacenamiento:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Ver todos los productos específicos de isoformas PROTACs
MoreVer todos los productos específicos de isoformas Eukaryotic Release Factor (eRF)
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Actividad biológica
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Cereblon |
eRF3a/GSPT1 |
GBD-9 (50 nM; 24 h) significantly degrades BTK and GSPT1 in DOHH2 cells, and the degradation could be blocked by 20 μM Ibrutinib (HY-10997) or Pomalidomide (HY-10984)[1].
GBD-9 (10-1000 nM; 72 h) inhibits the proliferation of DOHH2, WSU-NHL, HBL-1, THP-1, MV4-11 and other cells in a dose-dependent manner, with an IC50 of 133 nM for DOHH2 cells, which is significantly superior to Ibrutinib and single-target degraders[1].
GBD-9 (10-100 nM; 24 h) induces G1 arrest in DOHH2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DOHH2 (DLBCL cell line)
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Concentration:50 nM, 100 nM
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Incubation Time:24 h (50 nM), 4 h (100 nM)
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Result:Reduced BTK and GSPT1 protein levels to <20% of baseline at 50 μM, 4 h, with complete abrogation of BTK degradation when co-treated with Ibrutinib (20 μM), and loss of GSPT1 degradation when co-treated with pomalidomide (20 μM), confirming dependency on BTK binding and CRBN recruitment.
Chemical Information
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No. CAS 2864408-92-2
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Appearance Solid
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Peso molecular 797.90
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Fòrmula C44H47N9O6
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Color Light yellow to green yellow
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SMILES
O=C1N(C2CCC(NC2=O)=O)C(C(C1=C3)=CC=C3NCCCCCCCCC(N4CCC[C@@H](N5N=C(C6=CC=C(OC7=CC=CC=C7)C=C6)C8=C5N=CN=C8N)C4)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvente y solubilidad
DMSO : 100 mg/mL (125.33 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (276 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Mann MK, et al. Structure-Activity Relationship of USP5 Inhibitors [published correction appears in J Med Chem. 2022 Jan 13;65(1):889]. J Med Chem. 2021;64(20):15017-15036. [Content Brief]
[2]. Yang Z, et al. Merging PROTAC and molecular glue for degrading BTK and GSPT1 proteins concurrently. Cell Res. 2021 Dec;31(12):1315-1318. [Content Brief]
[3]. Zhao L, et al. Targeted protein degradation: mechanisms, strategies and application. Signal Transduct Target Ther. 2022 Apr 4;7(1):113. [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 (sealed storage, away from moisture and light). 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 | 1.2533 mL | 6.2664 mL | 12.5329 mL | 31.3322 mL |
| 5 mM | 0.2507 mL | 1.2533 mL | 2.5066 mL | 6.2664 mL | |
| 10 mM | 0.1253 mL | 0.6266 mL | 1.2533 mL | 3.1332 mL | |
| 15 mM | 0.0836 mL | 0.4178 mL | 0.8355 mL | 2.0888 mL | |
| 20 mM | 0.0627 mL | 0.3133 mL | 0.6266 mL | 1.5666 mL | |
| 25 mM | 0.0501 mL | 0.2507 mL | 0.5013 mL | 1.2533 mL | |
| 30 mM | 0.0418 mL | 0.2089 mL | 0.4178 mL | 1.0444 mL | |
| 40 mM | 0.0313 mL | 0.1567 mL | 0.3133 mL | 0.7833 mL | |
| 50 mM | 0.0251 mL | 0.1253 mL | 0.2507 mL | 0.6266 mL | |
| 60 mM | 0.0209 mL | 0.1044 mL | 0.2089 mL | 0.5222 mL | |
| 80 mM | 0.0157 mL | 0.0783 mL | 0.1567 mL | 0.3917 mL | |
| 100 mM | 0.0125 mL | 0.0627 mL | 0.1253 mL | 0.3133 mL |
GBD-9 Related Classifications
HY-153803 Related Classifications
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