DDB1 ligand-1
DDB1 ligand-1 is a DNA damage-binding protein 1 (DDB1) ligand. DDB1 ligand-1 binds to a unique pocket on the β propeller C (BPC) domain of DDB1, induces conformational changes, and blocks the canonical DCAF/HBx peptide binding site of DDB1. DDB1 ligand-1 engages full-length DDB1 in cellular settings and supports PROTAC development research.
For research use only. We do not sell to patients.
- Formula: C32H32F2N4O5
- Molecular Weight:590.62
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
Cereblon-DDB1 |
In Vitro
DDB1 ligand-1 (Compound 26) binds recombinant His-DDB1ΔB with high potency, as measured by TR-FRET displacement, with an EC50 of 40 nM[1].
DDB1 ligand-1 (0.1-100 μM) engages full-length DDB1 in AD293 cells stably expressing DDB1-HiBiT, stabilizing the protein with an EC50 of 3.55 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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Molecular Weight 590.62
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Formula C32H32F2N4O5
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SMILES
CNC([C@H]1C[C@H](CN(C1)C(C2=CC(OC(C)C)=C(C3=C2N(C=N3)C)C4=C5OC(F)(OC5=CC=C4)F)=O)C6=CC=CC=C6)=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.
Protocols
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Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DDB1 ligand-1 Related Classifications
HY-182983 Related Classifications
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