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
Description
IC50 & Target
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VHL |
DNPH1 28 nM (DC50) |
In Vitro
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. Further protocols information, click here.
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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.
Protocols
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RNA interference technology
RNA interference (RNAi) is a cellular mechanism that inhibits gene expression by suppressing gene transcription or activating RNA degradation. This mechanism was discovered in plants in 1998 by Andrew Fire and Craig Mello. Today, this phenomenon can be observed in almost all eukaryotes, including protozoa, flies, nematodes, insects, parasites, and mammals.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)