PROTAC DDa-1
PROTAC DDa-1 is a multi-targeted DCAF1-recruiting tyrosine kinase PROTAC degrader. PROTAC DDa-1 mediates the degradation of TNK2, CSK, LIMK2, TEC, and BTK, with a DC50 of 90 nM for BTK. PROTAC DDa-1 reduces the viability of BTK-dependent diffuse large B-cell lymphoma cells. PROTAC DDa-1 can be used for the research of diffuse large B-cell lymphoma.
(Pink: Bcr-Abl and Btk and Src ligand (HY-107447); Blue: Cereblon ligand (HY-149934); Black: linker).
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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。
- CAS 番号: 3036944-98-3
- 分子式: C60H77Cl2N13O3S
- 分子量:1131.31
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
DDa-1 (50-5000 nM; 6 h) mediates CRL- and proteasome-dependent degradation of CSK and LIMK2, but not LYN or ABL1, in HEK293T cells[1].
DDa-1 (5 µM; 6 h) reduces the abundance of CSK, LIMK2, TEC, and TNK2 proteins in HEK293T cells[1].
DDa-1 (62.5 nM-2000 nM; 24 h) potently degrades endogenous BTK with sub-µM potency in TMD8 diffuse large B-cell lymphoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells
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Concentration:50 nM, 500 nM, 5000 nM
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Incubation Time:6 h
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Result:Caused significant reduction in CSK and LIMK2 protein levels, but did not affect LYN or ABL1 levels.
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Cell Line:TMD8 diffuse large B-cell lymphoma cells
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Concentration:62.5 nM, 125 nM, 250 nM, 500 nM, 1000 nM, 2000 nM
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Incubation Time:24 h
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Result:Caused concentration-dependent reduction of endogenous BTK protein levels with sub-µM potency.
化学情報
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CAS 番号 3036944-98-3
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分子量 1131.31
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分子式 C60H77Cl2N13O3S
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SMILES
O=C(N1CCN(C2=CC=C3C(N=C(C4(C5=CC=C(Cl)C=C5)CCCCC4)N=C3NCCN)=C2)CC1)CCCCCCCN6CCC(OC7CCN(C8=CC(NC9=NC=C(C(NC%10=C(C)C=CC=C%10Cl)=O)S9)=NC(C)=N8)CC7)CC6
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
PROTAC DDa-1 関連分類
HY-156745 関連分類
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