Dth
Dth (DFHBI-thalidomide) is an RNA aptamer-based PROTAC degrader. Dth can degrade a variety of endogenous proteins (such as mCherry, p50, p65 and E2F1) by replacing the 3′ module on the RNA scaffold with the RNA aptamer corresponding to the target protein. Dth upregulates IκB-α and Bax, and downregulates Bcl-2 and VEGF. Dth generates green fluorescence upon binding to the Broccoli RNA aptamer, enabling the tracing of RNA scaffolds. Dth can be used in cancer-related research.
(Pink: Ligands for Target Protein for PROTAC ligand (HY-176801); Blue: Cereblon ligand (HY-41547); Black: linker).
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- Fòrmula: C30H29F2N5O6
- Peso molecular:593.58
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Almacenamiento:
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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Actividad biológica
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Chemical Information
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Actividad biológica
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p50 |
p65 |
Dth (20 μM; 1.5 h) colocalizes with exogenous mCherry in HEK-293T cells via the Broccoli-MS2 RNA scaffold[1].
Dth (20 μM; 24 h) induces targeted degradation of exogenous mCherry in CHO cells via the Broccoli-MS2 RNA scaffold[1].
Dth (10-160 μM; 24 h) induces targeted degradation of endogenous p50 in MCF-7 cells via the Broccoli-p50 RNA scaffold[1].
Dth (20 μM; 24 h) induces degradation of endogenous p50 in MCF-7 cells expressing the B-20A-p50 RNA scaffold, thereby inhibiting NF-κB activity and altering the expression of downstream pathway proteins[1].
Dth (10-30 μM; 24 h) induces targeted degradation of endogenous p65 and E2F1 in MCF-7 cells via respective Broccoli-based RNA scaffolds[1].
Dth (10-30 μM; 24-48 h) can simultaneously induce targeted degradation of endogenous p50 and E2F1 in MCF-7 cells via the tri-aptamer p50-20A-E2F1 RNA scaffold, and its inhibitory effect on cell proliferation is stronger than that of single-target degradation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Chinese hamster ovary CHO cells (stably expressing MCP-mCherry and transfected with plasmids encoding Broccoli-MS2 RNA scaffolds with varying polyA linkers)
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Concentration:20 μM
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Incubation Time:24 h
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Result:Showed all RNA scaffold linker lengths induced partial mCherry degradation, with 10 polyA (10A) and 30 polyA (30A) linkers yielding better results.
Confirmed reduced red fluorescence signals corresponding to mCherry degradation via fluorescence microscopy.
Revealed thalidomide and DFHBI alone did not induce significant mCherry degradation.
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Cell Line:human breast cancer MCF-7 cells (transfected with plasmids encoding Broccoli-p50 RNA scaffolds with varying polyA linkers)
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Concentration:0, 10, 20, 40, 80, 160 μM
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Incubation Time:24 h
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Result:Showed RNA scaffolds with 5A, 10A, 20A, and 30A linkers induced partial p50 degradation, with 10A and 20A linkers yielding better results.
Revealed the best p50 degradation at 20 μM, with a hook effect observed at higher concentrations.
Exhibited no significant p50 degradation in cells expressing only the p50 aptamer or only Broccoli.
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Cell Line:human breast cancer MCF-7 cells (transfected with plasmids encoding B-20A-p50 RNA scaffold and NF-kB-driven GFP reporter cassette)
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Concentration:20 μM
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Incubation Time:24 h
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Result:Showed GFP fluorescence (driven by NF-kB activation) was significantly reduced in cells treated with TNF-α and Dth.
Revealed upregulated IkBα and proapoptotic Bax, and downregulated antiapoptotic Bcl-2 and angiogenesis-related VEGF via western blot.
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Cell Line:human breast cancer MCF-7 cells (transfected with plasmids encoding Broccoli-p65 or Broccoli-E2F1 RNA scaffolds with varying polyA linkers)
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Concentration:0, 10, 20, 30 μM
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Incubation Time:24 h
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Result:Showed for p65, RNA scaffolds with 20A linker yielded optimal degradation, and p65 levels decreased in a dose-dependent manner with Dth treatment.
Revealed for E2F1, RNA scaffolds with 30A linker yielded optimal degradation.
Confirmed pretreatment with MG132 blocked p65 degradation, and thalidomide/DFHBI alone did not induce degradation of either protein.
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Cell Line:human breast cancer MCF-7 cells (transfected with plasmids encoding triple-aptamer p50-Broccoli-E2F1 RNA scaffolds with varying polyA linkers)
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Concentration:0, 10, 20, 30 μM
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Incubation Time:24-48 h (24 h for western blot; 48 h for cell viability)
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Result:Showed RNA scaffolds with 5A, 10A, 20A, and 30A linkers induced significant degradation of both p50 and E2F1, with the 20A linker yielding the best results.
Revealed both proteins decreased in a dose-dependent manner with Dth treatment, reaching maximum degradation after 24 h.
Showed cell viability was significantly reduced compared to controls via CCK-8 assay, with simultaneous degradation of p50 and E2F1 inhibiting proliferation more strongly than single-target degradation.
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Cell Line:HEK-293T cells
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Concentration:20 μM
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Incubation Time:1.5 h
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Result:Colocalized with exogenous mCherry via the Broccoli-MS2 RNA scaffold.
Chemical Information
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Peso molecular 593.58
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Fòrmula C30H29F2N5O6
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SMILES
O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3NCCCCCCN(C(C)=N/C4=C\C5=CC(F)=C(O)C(F)=C5)C4=O)=O
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Synonyms
DFHBI-thalidomide
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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)
Dth Related Classifications
HY-175397 Related Classifications
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