KDRLKZ-2
KDRLKZ-2 is a small-molecule ligand of KLHDC2 E3 ligase (Kd = 95 nM), with an IC50 of 68 nM and 0.1 μM in alphaLISA and TR-FRET assays, respectively. KDRLKZ-2 binds to the substrate-binding pocket of the kelch domain of KLHDC2, mimics the interaction of natural substrates and displaces them. KDRLKZ-2 acts as an oligomer disruptor, regulates the oligomerization of the KLHDC2-EloB-EloC complex, and induces the dissociation of tetramers into smaller components. KDRLKZ-2 can be used in scaffold ligand studies of PROTAC degraders targeting KLHDC2.
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- Formule: C23H29N3O7
- Masse moléculaire:459.49
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
KDRLKZ-2 competes with the native SelK peptide substrate for binding to purified KLHDC2 in alphaLISA displacement assays, with an IC50 of 0.068 μM[1].
KDRLKZ-2 competes with the native SelK peptide substrate for binding to purified KLHDC2 in TR-FRET displacement assays, with an IC50 of 0.1 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Masse moléculaire 459.49
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Formule C23H29N3O7
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SMILES
O=C(O)CN1C=C(N2C(C(C(C)CC)=CC3=C2CN(C(OCCOC)=O)CC3)=O)C=CC1=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)