PROTAC BRD4 Degrader-26
PROTAC BRD4 Degrader-26 is a light-regulated BRD4 PROTAC degrader. PROTAC BRD4 Degrader-26 induces targeted degradation of BRD4 via the ubiquitin-proteasome system. PROTAC BRD4 Degrader-26 is a degrader that can be inactivated in response to ultraviolet light. PROTAC BRD4 Degrader-26 can be used in breast cancer-related research.
(Pink: BRD4 ligand (HY-161651); Blue: Cereblon ligand (HY-41547); Black: linker (HY-161653)).
For research use only. We do not sell to patients.
- CAS No.: 3050769-37-1
- Formula: C46H45ClN10O10S
- Molecular Weight:965.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
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BRD4 |
Cereblon |
PROTAC BRD4 Degrader-26 (PROTAC-2) (0.01-10 µM; 6-24 h) induces concentration-dependent degradation of BRD4 in MCF-7 cells, reducing BRD4 levels by more than 80% after treatment with 1 µM for 24 h, and a hook effect is observed at 10 µM[1].
PROTAC BRD4 Degrader-26 (1 µM; 18 h) mediates the degradation of BRD4 in MCF-7 cells via a pathway dependent on the ubiquitin-proteasome system and requiring the activity of CRL-type E3 ligases[1].
PROTAC BRD4 Degrader-26 (0-120 min 365 nm UV exposure) undergoes rapid cleavage upon irradiation with 365 nm UV light, and complete degradation is observable within 30 min[1].
PROTAC BRD4 Degrader-26 (1 µM; 30 min 365 nm UV exposure, 24 h post-UV incubation) undergoes inactivation in MCF-7 cells upon immediate 365 nm UV irradiation for 30 minutes, which significantly impairs its ability to degrade BRD4[1].
PROTAC BRD4 Degrader-26 (1 µM; 6 h pre-incubation, 30 min 365 nm UV exposure, 24 h post-UV incubation) undergoes inactivation in MCF-7 cells upon 30 min of 365 nm UV irradiation at 6 h post-treatment, thereby reducing its BRD4 degradation efficacy[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human breast cancer MCF-7 cells
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Concentration:0.01, 0.1, 1, 10 µM
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Incubation Time:6 h; 24 h
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Result:Exhibited concentration-dependent BRD4 degradation at concentrations up to 1 µM, with a hook effect (diminished activity) observed at 10 µM.
Reduced BRD4 levels to 19% of control at 1 µM and 37% of control at 0.1 µM after 6 h treatment.
Reduced BRD4 levels to 22% of control at 1 µM and 93% of control at 0.01 µM after 24 h treatment.
Reduced BRD4 levels by more than 80% at 1 µM after 24 h treatment, making it the most potent BRD4 degrader among the synthesized PROTACs.
Chemical Information
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CAS No. 3050769-37-1
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Molecular Weight 965.43
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Formula C46H45ClN10O10S
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SMILES
O=C(C1=C(NCCCOC2=CC(COC(NCCCNC(C[C@H]3C4=NN=C(C)N4C(SC(C)=C5C)=C5C(C6=CC=C(Cl)C=C6)=N3)=O)=O)=C([N+]([O-])=O)C=C2)C=CC=C17)N(C8C(NC(CC8)=O)=O)C7=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)