LO-4-25
LO-4-25 is a CUL4DCAF16 based covalent PROTAC-like degrader. LO-4-25 induces degradation of the androgen receptor (AR) and androgen receptor truncation variant AR-V7. LO-4-25 covalently targets cysteine residues on CUL4DCAF16 to mediate degradation of neo-substrates. LO-4-25 triggers proteasome-dependent degradation of target proteins via CUL4DCAF16-mediated ubiquitination. LO-4-25 can be used for the research of androgen-independent prostate cancer.
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- Formule: C32H37ClN6O5S
- Masse moléculaire:653.19
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
LO-4-25 (1-10 μM; 24 h) potently degrades both AR and AR-V7 in 22Rv1 cells in a CUL4DCAF16-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:22Rv1 androgen-independent prostate cancer cells
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Concentration:1 μM, 10 μM
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Incubation Time:24 h
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Result:Induced robust degradation of both AR and AR-V7 in 22Rv1 cells.
Completely attenuated degradation of AR and AR-V7 in 22Rv1 cells with DCAF16 knockdown via siRNA transfection.
Chemical Information
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Masse moléculaire 653.19
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Formule C32H37ClN6O5S
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SMILES
O=C(NC1=CC(Cl)=CN=C1)/C=C/C(N2CCN(CC2)C(CCCCCOC3=CC=C(C=C3)C4=CSC(N5CCOCC5)=N4)=O)=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)