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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- CAS No.: 3036944-98-3
- Formule: C60H77Cl2N13O3S
- Masse moléculaire:1131.31
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
In Vitro
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. Further protocols information, click here.
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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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CAS No. 3036944-98-3
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Masse moléculaire 1131.31
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC DDa-1 Related Classifications
HY-156745 Related Classifications
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