KDRLKZ-1
KDRLKZ-1 (8SGE) is a small-molecule ligand of KLHDC2 E3 ligase (Kd = 0.36 μM), with an IC50 of 0.21 μM and 0.31 μM in alphaLISA and TR-FRET assays, respectively. KDRLKZ-1 binds to the substrate-binding pocket of the KLHDC2 kelch domain, mimics the interaction of natural substrates and displaces them. KDRLKZ-1 acts as an oligomer disruptor, regulates the oligomerization of the KLHDC2-EloB-EloC complex, and induces the dissociation of tetramers into smaller components. KDRLKZ-1 can be used in scaffold ligand research for PROTAC degraders targeting KLHDC2.
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- 화학식: C23H29N3O7
- 분자량:459.49
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보관:
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
- 순도&문서
- References
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Help & FAQs
Biological Activity
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KLHDC2 0.36 μM (Kd) |
KDRLKZ-1 binds to the purified KLHDC2 kelch domain, with a Kd value of 0.36 µM, a 1:1 binding mode, and a half-life of 76 seconds[1].
KDRLKZ-1 (15 min) can specifically displace the SelK peptide substrate from the purified KLHDC2 kelch domain, with an IC50 of 0.21 µM, and shows no activity against VHL[1].
KDRLKZ-1 (80 min) displaces the SelK peptide substrate from the purified KLHDC2 kelch domain in TR-FRET assays, with an IC50 of 0.31 µM[1].
Excessive KDRLKZ-1 competes with the natural USP1 peptide substrate for binding to the purified full-length KLHDC2-EloB-EloC complex, thereby inhibiting the ubiquitination modification of USP1[1].
KDRLKZ-1 induces the dissociation of purified full-length KLHDC2-EloB-EloC tetramers into smaller oligomers[1].
Excessive KDRLKZ-1 competitively inhibits the interaction between endogenous KLHDC2 and biotin-conjugated KLHDC2 ligand in HEK293 cell extracts[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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분자량 459.49
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화학식 C23H29N3O7
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SMILES
O=C(O)CN1C=C(N2C(C(CC(C)C)=CC3=C2CN(C(OCCOC)=O)CC3)=O)C=CC1=O
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Synonyms
8SGE
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KDRLKZ-1 Related Classifications
HY-157558 Related Classifications
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