KLHL12 ligand-1
KLHL12 ligand-1 is a KLHL12 Kelch domain ligand with a Ki of 0.33 μM, Ka of 0.33 μM, submicromolar binding affinity, and selective binding over KEAP1/KLHL19. KLHL12 ligand-1 binds in the substrate cleft of KLHL12, with its 4-methyl group forming a CH-π interaction with Tyr334. KLHL12 ligand-1 binds to cellular KLHL12 in permeabilized and intact cells, and has solvent-exposed positions suitable for modification to create PROTACs. KLHL12 ligand-1 can be used for the research of cancer.
For research use only. We do not sell to patients.
- Formula: C16H13Cl3N4O
- Molecular Weight:383.66
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
KLHL12 ligand-1 (compound 7k) potently binds purified KLHL12 Kelch domain with an FPA-determined Ki of 0.33 μM[1].
KLHL12 ligand-1 (15 min) engages KLHL12-NanoLuc in digitonin-permeabilized HEK293 cells with an IC50 of 0.62 μM[1].
KLHL12 ligand-1 (2 h) engages KLHL12-NanoLuc in intact HEK293 cells with an IC50 of 0.14 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 383.66
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Formula C16H13Cl3N4O
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SMILES
CC1=CC=CC2=C1N=C(N2CC(NC3=C(Cl)C=C(Cl)C=C3Cl)=O)N
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)