dHTC3
dHTC3 is a selective BRD4 molecular glue degrader. dHTC3 selectively binds to BRD4 BD1 to form a BRD4-dHTC3 complex, which cooperatively recruits the SCFFBXO3 E3 ubiquitin ligase and mediates the degradation of BRD4 via the ubiquitin-proteasome pathway. dHTC3 induces proteasome- and CRL-dependent BRD4 degradation with no hook effect. dHTC3 can be used in related research on acute myeloid leukemia.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C31H42N6O4S2
- Peso molecular:626.83
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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
Descripciòn
IC50 & Target
[1]|
BRD4 (BD1) |
In Vitro
dHTC3 (1 nM-100 μM; 12-16 h) degrades BRD4 in MV4;11 BRD4-HiBiT cells, and pretreatment with JQ1 (HY-13030), MLN4924 (HY-70062), and Carfilzomib (HY-10455) blocks this degradation[1].
dHTC3 does not exhibit the hook effect in both BRD4 degradation and ternary complex formation assays[1].
dHTC3 (1 nM-100 μM; 1-16 h) selectively degrades BRD4 in MV4;11, HEK293T and NALM6 cells via SCFFBXO3 mediation, and its degradation activity is completely abolished after FBXO3 knockout[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Peso molecular 626.83
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Fòrmula C31H42N6O4S2
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SMILES
O=C(OC(C)(C)C)C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(NS(=O)(NCC5C(CC)(CC)C5)=O)C=C4)=N1
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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)
dHTC3 Related Classifications
HY-181976 Related Classifications
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