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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- No. CAS: 3036944-98-3
- Fòrmula: C60H77Cl2N13O3S
- Peso molecular:1131.31
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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.
Chemical Information
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No. CAS 3036944-98-3
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Peso molecular 1131.31
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC DDa-1 Related Classifications
HY-156745 Related Classifications
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