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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C23H29N3O7
- 分子量:459.49
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
KLHDC2 0.36 μM (Kd) |
体外実験
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. Further protocols information, click here.
化学情報
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分子量 459.49
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分子式 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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別名
8SGE
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)