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))
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.92%
- CAS 番号: 2769753-47-9
- 分子式: C41H42N8O7S2
- 分子量:822.95
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
|
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.
化学情報
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CAS 番号 2769753-47-9
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性状 Solid
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分子量 822.95
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
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 |