Hyp-dBET1
Hyp-dBET1 is a hypoxia-activated BRD4 PROTAC degrader. The IC50 of Hyp-dBET1 for reducing cell viability under hypoxic conditions is approximately 153 nM to 192 nM, while it shows low activity under normoxic conditions (IC50 of approximately 2.8 μM to 3.8 μM). Hyp-dBET1 induces BRD4 degradation under hypoxic conditions, converts to dBET1 in hypoxic environments, and downregulates the expression level of ZFP-91. Hyp-dBET1 can be used in studies related to breast cancer, cervical cancer and solid tumors.
(Pink: BRD4 ligand (HY-78695); Blue: Cereblon ligand (HY-103597); Black: linker (HY-178091)).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C45H42ClN9O9S
- Peso molecular:920.39
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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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BRD4 |
Hyp-dBET1 (0.05-5.0 μM; 24 h) significantly degrades BRD4 protein in MDA-MB-231 cells under hypoxic conditions, while it exerts no obvious BRD4-degrading effect but downregulates the expression of downstream protein ZFP-91 under normoxic conditions[1].
Hyp-dBET1 (0.1-100 μM; 72 h) exerts a concentration-dependent effect on reducing cell viability in MDA-MB-231 (with an IC50 value of 3.4 μM under normoxia), HeLa (with IC50 values of 3815 nM and 192 nM under normoxia and hypoxia, respectively), and HEK-293 (with IC50 values of 2870 nM and 153 nM under normoxia and hypoxia, respectively) cells under either hypoxic or normoxic conditions[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:0.05, 0.1, 0.2, 0.5, 1.0, 2.0, 5.0 μM
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Incubation Time:24 h
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Result:Significantly degraded the target protein BRD4 under hypoxic conditions.
Failed to effectively degrade the target protein BRD4 under normoxic conditions.
Non-specifically downregulated the expression of the downstream protein ZFP-91 under normoxic conditions.
Chemical Information
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Peso molecular 920.39
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Fòrmula C45H42ClN9O9S
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SMILES
CC1=C(C)C(C(C2=CC=C(Cl)C=C2)=N[C@H]3CC(N(CC4=CC=C([N+]([O-])=O)C=C4)CCCCNC(COC5=C6C(C(N(C7C(NC(CC7)=O)=O)C6=O)=O)=CC=C5)=O)=O)=C(S1)N8C3=NN=C8C
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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)
Hyp-dBET1 Related Classifications
HY-173256 Related Classifications
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