PROTAC BRD4 Degrader-14
PROTAC BRD4 Degrader-14 is a PROTAC-type BRD4 degrader, which is predicted to be a weak VHL binder and an inactive BRD4 degrader.
(Pink: BRD4 ligand (HY-129939); Blue: VHL ligand (HY-125845); Black: linker (HY-176368)).
For research use only. We do not sell to patients.
- CAS No.: 3026420-43-6
- Formula: C57H61F2N9O11S2
- Molecular Weight:1150.27
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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 |
PROTAC BRD4 Degrader-14 (compound 15) binds to BRD4 BD2 bromodomain with an IC50 of 8.1 nM[1].
PROTAC BRD4 Degrader-14 forms a ternary complex with BRD4 and VHL with a combined SPR half-life of 650 minutes[1].
PROTAC BRD4 Degrader-14 (4 hours) suppresses MYC gene transcript in MV4-11 AML cells with an IC50 of 15 nM and 98% maximum suppression at 4 hours[1].
PROTAC BRD4 Degrader-14 (4 hours) degrades BRD4 protein in EOL-1 cells with a DC50 of 2.1 nM and 98% maximum degradation at 4 hours[1].
PROTAC BRD4 Degrader-14 (6 days) inhibits EOL-1 cell proliferation with an IC50 of 91 nM at 6 days[1].
PROTAC BRD4 Degrader-14 (6 days) inhibits proliferation of PC3-S1 and LNCaP prostate cancer cells with an average IC50 of 64.5 nM at 6 days[1].
PROTAC BRD4 Degrader-14 (6 days) inhibits proliferation of HL-60 and EOL-1 AML cells with an average IC50 of 3.69 nM at 6 days[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3026420-43-6
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Molecular Weight 1150.27
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Formula C57H61F2N9O11S2
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SMILES
O[C@H](C[C@H]1C(NCC2=CC=C(C=C2)C3=C(N=CS3)C)=O)CN1C([C@@H](NC(COCCC4=CC(OCCNC(C5=CC(N(C6=NC=C(F)C=C6F)CC7=CNC8=C7C9=CN(C)C8=O)=C9C=C5CS(=O)(C)=O)=O)=CC(O)=C4)=O)C(C)(C)C)=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)