PROTAC BRD4 Degrader-28
PROTAC BRD4 Degrader-28 is a PROTAC degrader targeting BRD4, with a DC50 of 5.4 nM for BRD4 in HEK293 cells. PROTAC BRD4 Degrader-28 binds to the CRBN E3 ubiquitin ligase, forms a ternary complex with BRD4, and thereby mediates the ubiquitination and proteasomal degradation of BRD4. PROTAC BRD4 Degrader-28 can be used in cancer research.
(Pink: BRD4 ligand (HY-78695); Blue: Cereblon ligand (HY-115560); Black: linker).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C38H36ClN7O8S
- Peso molecular:786.25
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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
Descripciòn
IC50 & Target
[1]|
BRD4 5.4 nM (DC50) |
BRD4 BD1 2.3 nM (IC50) |
In Vitro
PROTAC BRD4 Degrader-28 (compound 4) (24 h) potently degrades endogenous BRD4 in HEK293 cells with a DC50 of 5.4 nM and a Dmax of 83%[1].
PROTAC BRD4 Degrader-28 (30 min, 3 h) binds directly to the BRD4-BD1 domain with an IC50 of 2.3 nM[1].
PROTAC BRD4 Degrader-28 (2 h, 30 min) engages CRBN in live HEK293 cells with an IC50 of 263.7 nM and in permeabilized cells with an IC50 of 68.8 nM, yielding an RBA of 2.4[1].
PROTAC BRD4 Degrader-28 1 h, 3 h) promotes BRD4-CRBN ternary complex formation with a KTF of 5.0 nM and an AUC of 158.5[1].
PROTAC BRD4 Degrader-28 (250 ns) forms stable interactions with the BRD4-BD1 domain, as demonstrated by consistent binding poses and low RMSF during 250 ns MD simulations[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 786.25
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Fòrmula C38H36ClN7O8S
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SMILES
O=C(OCCCCNC(COC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)=O)C[C@H]4C5=NN=C(C)N5C6=C(C(C)=C(C)S6)C(C7=CC=C(Cl)C=C7)=N4
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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 BRD4 Degrader-28 Related Classifications
HY-170808 Related Classifications
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