DB0614
Based on 1 Customer Validation
DB0614 is a PROTAC based on Cereblon ligand, which is a selective and potent targeted protein degrader of NEK9 inhibitor. DB0614 can degrade ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2 and ULK1. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity.(Blue: Thalidomide-4-OH (HY-103596), Black: linker, Pink: FLT3-IN-17 (HY-148070))
For research use only. We do not sell to patients.
- Purity: 96.07%
- CAS No.: 2769753-47-9
- Formula: C41H42N8O7S2
- Molecular Weight:822.95
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
|
CDK6 |
CDK16/Cyclin Y |
ULK1 |
Aurora Kinase |
SIK2 |
LIMK2 |
DB0614 (1 μM, 5 h) is E3-ligase dependent on the degradation of the protein mitosis A-related kinase 9 (NEK9) in Cereblon (CRBN)-/- MOLT-4 cells[1].
DB0614 (1 μM, 6 h) shows high levels of degradation but not full loss in NEK9 which is dependent on the proteasome, neddylation, E1 inhibition and CRBN binding in HCT116 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLT4 cells
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Concentration:0-10000 nM
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Incubation Time:5 h
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Result:Degradated the protein NEK9 maximamly at 125 nM in MOLT4 cells.
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Cell Line:HCT116 cells
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Concentration:0-10 μM
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Incubation Time:6 h
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Result:Showed high levels of degradation but not full loss in NEK9 levels in HCT116 cells.
Chemical Information
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CAS No. 2769753-47-9
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Appearance Solid
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Molecular Weight 822.95
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Formula C41H42N8O7S2
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Color Light yellow to yellow
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SMILES
O=C1C2=C(C(N1C3C(NC(CC3)=O)=O)=O)C(OCCCCCN4CCN(CC4)C5=CC=C(NC6=NC7=C(SC=C7C8=CC(NS(=O)(C)=O)=CC=C8)C=N6)C=C5)=CC=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 2.78 mg/mL (3.38 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 60°C; 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (273 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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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 | 1.2151 mL | 6.0757 mL | 12.1514 mL | 30.3785 mL |
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