PROTAC BLIMP-1 degrader-1
Based on 1 Customer Validation
PROTAC BLIMP-1 degrader-1 is an orally active BLIMP-1 PROTAC degrader with an EC50 of 13.1 nM. PROTAC BLIMP-1 degrader-1 recruits the neprilysin (CRBN) E3 ligase to mediate ubiquitination and subsequent degradation of BLIMP-1α via the 26S proteasome, without affecting the BLIMP-1β isoform. PROTAC BLIMP-1 degrader-1 inhibits cancer cell proliferation and tumor growth. It can be used in research related to multiple myeloma.
(Pink: BLIMP-1 ligand (HY-180178); Blue: Ligands for E3 Ligase and Cereblon ligand (HY-W442918); Black: linker (HY-180180)).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 98.49%
- Formule: C41H47BrN8O4
- Masse moléculaire:795.77
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
BLIMP-1 13.1 nM (EC50) |
In Vitro
PROTAC BLIMP-1 degrader-1 (Compound 49) (2 h) potently induces BLIMP-1 degradation in BLIMP-1-overexpressing HEK293 cells with an EC50 of 13.1 nM, while exhibiting high human liver microsomal stability, moderate permeability, and low efflux potential[1].
PROTAC BLIMP-1 degrader-1 (0.01-10.0 μM; 24 h) induces dose-dependent depletion of endogenous BLIMP-1α (but not BLIMP-1β) in OPM2 and MM1.s multiple myeloma cell lines[1].
PROTAC BLIMP-1 degrader-1 (log10 μM from -4 to 1; 5 days) drives CRBN-dependent cytostatic antiproliferative activity in OPM2 multiple myeloma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:OPM2, MM1.s multiple myeloma cell lines
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Concentration:0.01, 0.02, 0.04, 0.08, 0.16, 0.32, 0.63, 1.26, 2.5, 5 and 10.0 μM
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Incubation Time:24 h
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Result:Dose-dependently depleted endogenous BLIMP-1α protein in both OPM2 and MM1.s cell lines.
Spares the shorter BLIMP-1β isoform.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG mice[1]
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Dosage:200 mg/kg
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Administration:p.o.; twice daily; 3 days
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Result:Achieved 54% BLIMP-1 degradation at 6 hours post last dose.
Sustained 60% BLIMP-1 degradation at 14 hours post last dose.
Chemical Information
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Appearance Solid
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Masse moléculaire 795.77
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Formule C41H47BrN8O4
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Color White to off-white
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SMILES
CC1=CC(Br)=CC=C1[C@@H](C(N)=O)N2CCN3N=C(C=C3C2)CNC(C4=NC(C)=C([C@H]5CC[C@@H](CC5)CNC6=CC=C(C7CCC(NC7=O)=O)C=C6)C=C4)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (62.83 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). 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). 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)
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2659 KB)
Références
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). 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 | 1.2566 mL | 6.2832 mL | 12.5664 mL | 31.4161 mL |
| 5 mM | 0.2513 mL | 1.2566 mL | 2.5133 mL | 6.2832 mL | |
| 10 mM | 0.1257 mL | 0.6283 mL | 1.2566 mL | 3.1416 mL | |
| 15 mM | 0.0838 mL | 0.4189 mL | 0.8378 mL | 2.0944 mL | |
| 20 mM | 0.0628 mL | 0.3142 mL | 0.6283 mL | 1.5708 mL | |
| 25 mM | 0.0503 mL | 0.2513 mL | 0.5027 mL | 1.2566 mL | |
| 30 mM | 0.0419 mL | 0.2094 mL | 0.4189 mL | 1.0472 mL | |
| 40 mM | 0.0314 mL | 0.1571 mL | 0.3142 mL | 0.7854 mL | |
| 50 mM | 0.0251 mL | 0.1257 mL | 0.2513 mL | 0.6283 mL | |
| 60 mM | 0.0209 mL | 0.1047 mL | 0.2094 mL | 0.5236 mL |
PROTAC BLIMP-1 degrader-1 Related Classifications
HY-180177 Related Classifications
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