PROTAC DNPH1 Degrader 1
PROTAC DNPH1 Degrader 1 is a potent PROTAC DNPH1 degrader with a DC50 of 28 nM. PROTAC DNPH1 Degrader 1 mediates proteasome- and VHL-dependent DNPH1 knockdown, drives DNPH1 ubiquitination and proteasomal degradation. PROTAC DNPH1 Degrader 1 can be used for the research of brca1 mutant cancer.
(Pink: DNPH1 ligand (HY-179303); Blue: VHL ligand (HY-150803); Black: linker).
For research use only. We do not sell to patients.
- Formula: C60H64F3N11O6S
- Molecular Weight:1124.28
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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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VHL |
DNPH1 28 nM (DC50) |
PROTAC DNPH1 Degrader 1 (compound 59) (0-500 nM; 18-168 h) potently and completely degrades DNPH1 in SUM149PT cells via a proteasome-dependent, VHL-recruiting mechanism[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SUM149PT cells, HiBit-tagged SUM149PT cells
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Concentration:0; 10; 50; 100; 300; 500 nM
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Incubation Time:18; 24; 48; 72; 120; 168 h
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Result:Achieved near-complete DNPH1 degradation with a DC50 of 28 nM and a Dmax of 100%.
Blocked degradation by cotreatment with proteasome inhibitors and neddylation inhibitor.
Inhibited degradation by competition with DNPH1 ligand 44 and VHL ligand VHL032.
Observed near-complete DNPH1 degradation via Western blot at concentrations as low as 20 nM in parental SUM149PT cells.
Chemical Information
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Molecular Weight 1124.28
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Formula C60H64F3N11O6S
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SMILES
CNC1=NC(NC2=C(C=C(C=C2)C(O)=O)C3=CC=CC(C(F)(F)F)=C3)=NC4=CC=C(C=C41)OC5=CC=C(C=C5)CN(CCCCCC6=CN([C@H](C(N7C[C@H](O)C[C@H]7C(N[C@@H](C)C8=CC=C(C9=C(C)N=CS9)C=C8)=O)=O)C(C)C)N=N6)C
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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)